Alisertib | MLN 8237 | Aurora A Kinase Inhibitor | AmBeed-信号通路专用抑制剂

规格	价格	会员价	库存	数量
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产品名称	Aurora A ↓ ↑	Aurora B ↓ ↑	Aurora C ↓ ↑	其他靶点	纯度
BI-847325	++ Aurora A (Human), IC50: 25 nM	++++ Aurora B (Xenopus laevis), IC50: 3 nM	++ Aurora C (Human), IC50: 15 nM		99%+
CCT 137690	++ Aurora A, IC50: 15 nM	++ Aurora B, IC50: 25 nM	++ Aurora C, IC50: 19 nM		99%+
MK-5108	++++ Aurora A, IC50: 0.064 nM				99%+
KW-2449	+ Aurora A, IC50: 48 nM			FLT3	99%+
Tozasertib	++++ Aurora A, Ki app: 0.6 nM	++ Aurora B, Ki app: 18 nM	+++ Aurora C, Ki app: 4.6 nM	Bcr-Abl,FLT3	99%+
AT9283	++++ Aurora A, IC50: ~3.0 nM	++++ Aurora B, IC50: ~3.0 nM			99%+
MLN8054	+++ Aurora A, IC50: 4 nM	+ Aurora B, IC50: 172 nM			99%+
ZM-447439	+ Aurora A, IC50: 110 nM	+ Aurora B, IC50: 130 nM		Src	99%+
TCS7010	++++ Aurora A, IC50: 3.4 nM				99%+
TAK-901	++ Aurora A-TPX2, IC50: 21 nM	++ Aurora B-INCENP, IC50: 15 nM			99%+
Danusertib	+++ Aurora A, IC50: 13 nM	+ Aurora B, IC50: 79 nM	+ Aurora C, IC50: 61 nM	RET	99%+
MK-8745	++++ Aurora A, IC50: 0.6 nM				99+%
PHA-680632	++ Aurora A, IC50: 27 nM	+ Aurora B, IC50: 135 nM	+ Aurora C, IC50: 120 nM	FLT3	99%+
AMG 900	+++ Aurora A, IC50: 5 nM	+++ Aurora B, IC50: 4 nM	++++ Aurora C, IC50: 1 nM		99%+
Alisertib	++++ Aurora A, IC50: 1.2 nM				99%+
ENMD-2076	+++ Aurora A, IC50: 14 nM	+ Aurora B, IC50: 350 nM		RET,FLT3	98%
JNJ-7706621	+++ Aurora A, IC50: 11 nM	++ Aurora B, IC50: 15 nM			99%+
CYC-116	+++ Aurora A, Ki: 8 nM	+++ Aurora B, Ki: 9 nM		FLT3	99%+
Reversine	+++ Aurora A, IC50: 12 nM	+++ Aurora B, IC50: 13 nM	++ Aurora C, IC50: 20 nM		98%
CCT129202	++ Aurora A, IC50: 42 nM	+ Aurora B, IC50: 198 nM	+ Aurora C, IC50: 227 nM		98%
SNS-314 mesylate	+++ Aurora A, IC50: 9 nM	++ Aurora B, IC50: 31 nM	++++ Aurora C, IC50: 3 nM		99%+
Barasertib-HQPA		++++ Aurora B, IC50: 0.37 nM			99%+
Hesperadin		+ Aurora B (human), IC50: 250 nM			98%
GSK-1070916		++++ Aurora B-INCENP, IC50: 3.5 nM	+++ Aurora C-INCENP, IC50: 6.5 nM	Tie-2,SIK	99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Cell Line ROSAKIT D816V cells HMC-1 cells CAMA-1 T47D MCF7 GB169 neurosphere cells GB30 neurosphere cells GB9 neurosphere cells A549 lung cancer cells Hs294T cells SK-Mel5 cells DLD-1 HCT116 BCL cell lines (LY10, SU-DHL6, LY7, Jeko-1) TCL cell lines (C5MJ, DND41, H9, HH) MDA-MB-231 cells MDA-MB-231 cells	Concentration	Treated Time	Description	References
ROSAKIT D816V cells	500 nM	24 h	To evaluate the induction of apoptosis by Alisertib in ROSAKIT D816V cells, results showed that Alisertib significantly induced apoptosis at submicromolar doses.	Biomark Res. 2023 Mar 10;11(1):29.
HMC-1 cells	500 nM	24 h	To evaluate the induction of apoptosis by Alisertib in HMC-1 cells, results showed that Alisertib significantly induced apoptosis at submicromolar doses.	Biomark Res. 2023 Mar 10;11(1):29.
CAMA-1	200 nM	72 h	To investigate the cytotoxic effect of Alisertib on RB-deficient cells, results showed that RB-deficient cells were more sensitive to Alisertib, leading to apoptosis.	Oncogene. 2022 Jul;41(27):3524-3538.
T47D	200 nM	72 h	To investigate the cytotoxic effect of Alisertib on RB-deficient cells, results showed that RB-deficient cells were more sensitive to Alisertib, leading to apoptosis.	Oncogene. 2022 Jul;41(27):3524-3538.
MCF7	200 nM	72 h	To investigate the cytotoxic effect of Alisertib on RB-deficient cells, results showed that RB-deficient cells were more sensitive to Alisertib, leading to apoptosis.	Oncogene. 2022 Jul;41(27):3524-3538.
GB169 neurosphere cells	200 nM	12 days	Induced apoptosis and senescence, reduced tumor cell proliferation	Cancer Res. 2014 Oct 1;74(19):5364-70.
GB30 neurosphere cells	200 nM	12 days	Induced apoptosis and senescence, reduced tumor cell proliferation	Cancer Res. 2014 Oct 1;74(19):5364-70.
GB9 neurosphere cells	200 nM	12 days	Induced apoptosis and senescence, reduced tumor cell proliferation	Cancer Res. 2014 Oct 1;74(19):5364-70.
A549 lung cancer cells	500 nM	7 days	Induced cellular senescence, enhanced SA-β-gal activity, and inhibited clonogenic capacity	Nutrients. 2022 Sep 2;14(17):3636.
Hs294T cells	1 μM	3 days	Investigated the effect of Alisertib on DNA damage, finding that Alisertib increased the expression of the DNA damage marker γH2AX.	EBioMedicine. 2017 Oct;24:43-55.
SK-Mel5 cells	1 μM	3 days	Investigated the effect of Alisertib on DNA damage, finding that Alisertib increased the expression of the DNA damage marker γH2AX.	EBioMedicine. 2017 Oct;24:43-55.
DLD-1	0.05 µM, 0.1 µM, 0.2 µM	72 h	To evaluate the anti-proliferative effects of Alisertib and TAK-733 alone and in combination, it was found that the combination showed stronger synergistic effects in KRAS/PIK3CA double-mutant cell lines.	Front Pharmacol. 2015 Jun 16;6:120.
HCT116	0.05 µM, 0.1 µM, 0.2 µM	72 h	To evaluate the anti-proliferative effects of Alisertib and TAK-733 alone and in combination, it was found that the combination showed stronger synergistic effects in KRAS/PIK3CA double-mutant cell lines.	Front Pharmacol. 2015 Jun 16;6:120.
BCL cell lines (LY10, SU-DHL6, LY7, Jeko-1)	10 to 1000 nM	72 h	To evaluate the cytotoxic effect of Alisertib in BCL cell lines, results showed concentration-dependent cytotoxicity in BCL cell lines.	Clin Cancer Res. 2015 Sep 15;21(18):4097-109.
TCL cell lines (C5MJ, DND41, H9, HH)	10 to 1000 nM	72 h	To evaluate the cytotoxic effect of Alisertib in TCL cell lines, results showed concentration-dependent cytotoxicity in TCL cell lines.	Clin Cancer Res. 2015 Sep 15;21(18):4097-109.
MDA-MB-231 cells	100 nM	2 h	To investigate the effect of Alisertib on the ATP/ADP ratio in mitotic cells, results showed that Alisertib treatment significantly reduced the ATP/ADP ratio.	Cell Death Dis. 2021 Sep 30;12(10):893.
MDA-MB-231 cells	100 nM	6 h	To investigate the effect of Alisertib on oxidative phosphorylation (OXPHOS) in cells, results showed that Alisertib treatment significantly reduced intracellular ATP levels.	Cell Death Dis. 2021 Sep 30;12(10):893.

Species Mice Nude mice Mice Nude mice Nude mice SCID mice BALB/c mice	Animal Model MCF7 xenograft model Intracranial GB neurosphere xenograft model MYC-driven SCLC mouse model Hs294T xenograft model Colorectal cancer cell line xenograft models TCL xenograft model 4T1 xenograft model	Administration	Dosage	Frequency	Description	References
Mice	MCF7 xenograft model	Oral	10 mg/kg	6 days a week for 3 weeks	To evaluate the therapeutic effect of Alisertib on RB-deficient tumors in vivo, results showed that Alisertib significantly inhibited the growth of RB-deficient tumors.	Oncogene. 2022 Jul;41(27):3524-3538.
Nude mice	Intracranial GB neurosphere xenograft model	Oral	20 mg/kg	Twice daily, 5 days/week for 2 weeks	Extended median survival of mice, reduced tumor cell proliferation	Cancer Res. 2014 Oct 1;74(19):5364-70.
Mice	MYC-driven SCLC mouse model	Oral gavage	20 mg/kg	5 days on, 2 days off weekly, continuous treatment	To evaluate the effect of Alisertib in combination with CHK1 inhibitor Prexasertib on the survival of MYC-driven SCLC mouse model, results showed that the combination therapy significantly prolonged the survival of mice.	Nat Commun. 2019 Aug 2;10(1):3485
Nude mice	Hs294T xenograft model	Subcutaneous injection	30 mg/kg	Once daily for 3 weeks	Investigated the effect of Alisertib on tumor growth, finding that Alisertib significantly inhibited tumor growth.	EBioMedicine. 2017 Oct;24:43-55.
Nude mice	Colorectal cancer cell line xenograft models	Oral	3 mg/kg	Once daily for 22 days	To evaluate the anti-tumor activity of Alisertib and TAK-733 alone and in combination in colorectal cancer cell line xenograft models, it was found that the combination showed synergistic effects in the HCT116 xenograft model.	Front Pharmacol. 2015 Jun 16;6:120.
SCID mice	TCL xenograft model	Alisertib oral, Romidepsin intraperitoneal	20 mg/kg	Alisertib daily for 21 days; Romidepsin on days 1, 9, 16	To evaluate the synergistic effect of Alisertib and Romidepsin combination therapy in a TCL xenograft model, results showed significant tumor growth inhibition and improved survival.	Clin Cancer Res. 2015 Sep 15;21(18):4097-109.
BALB/c mice	4T1 xenograft model	Oral	15 mg/kg	Once daily for 17 days	To investigate the tumor suppressive effect of Alisertib in combination with metformin, results showed that the combination treatment significantly inhibited tumor growth.	Cell Death Dis. 2021 Sep 30;12(10):893.

细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源

2884	100 μM	Growth Inhibition Assay	72 h	Attenuates cell growth	23328114
2885	100 μM	Growth Inhibition Assay	72 h	Attenuates cell growth	23328114
A172	100 μM	Cytotoxic Assay	24 h	IC50=0.120 μM	22274399
A-673	10 μM	Growth Inhibition Assay	96 h	IC50=0.032 μM	21448591
AGS	25 μM	Growth Inhibition Assay	24 h	IC50=19.09 μM	25609923
AGS	5 μM	Apoptosis Assay	24 h	Induces apoptosis	25609923
AGS	5 μM	Function Assay	24 h	Induces the autophagy	25609923
AGS	0.5 μM	Cytotoxic Assay	24 h	Decreases cell survival	22972611
BT-12	10 μM	Growth Inhibition Assay	96 h	IC50=0.060 μM	20108338
BxPC-3	50 μM	Growth Inhibition Assay	24 h	IC50=6.8 μM	25632225
BxPC-3	5 μM	Function Assay	24 h	Induces cell cycle arrest in G2/M phase	25632225
BxPC-3	5 μM	Function Assay	24 h	Induces autophagic cell death	25632225
CCL119		Cytotoxic Assay	72 h	IC50=0.062 μM	25878331
CCRF-CEM	10 μM	Growth Inhibition Assay	96 h	IC50=0.094 μM	20108338
CHLA-10	10 μM	Growth Inhibition Assay	96 h	IC50=0.060 μM	21448591
CHLA-119	10 μM	Growth Inhibition Assay	96 h	IC50=0.022 μM	21448591
CHLA-122	10 μM	Growth Inhibition Assay	96 h	IC50=0.019 μM	21448591
CHLA-136	10 μM	Growth Inhibition Assay	96 h	IC50=0.039 μM	21448591
CHLA-140	10 μM	Growth Inhibition Assay	96 h	IC50=0.026 μM	21448591
CHLA-25	10 μM	Growth Inhibition Assay	96 h	IC50=0.168 μM	21448591
CHLA-258	10 μM	Growth Inhibition Assay	96 h	IC50=0.132 μM	21448591
CHLA-266	10 μM	Growth Inhibition Assay	96 h	IC50=0.072 μM	20108338
CHLA-32	10 μM	Growth Inhibition Assay	96 h	IC50=0.136 μM	21448591
CHLA-56	10 μM	Growth Inhibition Assay	96 h	IC50=10 μM	21448591
CHLA-9	10 μM	Growth Inhibition Assay	96 h	IC50=0.018 μM	21448591
CHLA-90	10 μM	Growth Inhibition Assay	96 h	IC50=0.061 μM	21448591
COG-E-352	10 μM	Growth Inhibition Assay	96 h	IC50=0.043 μM	21448591
COG-LL-317	10 μM	Growth Inhibition Assay	96 h	IC50=0.047 μM	20108338
CRL-2396	100 μM	Growth Inhibition Assay		IC50=0.092 μM	23153524
CRL-2396	1 μM	Cytotoxic Assay	48 h	Induces apoptosis	23153524
DAOY	10 μM	Cytotoxic Assay	72 h	IC50=0.04 μM	22669335
DB	10 μM	Cytotoxic Assay	7 d	IC50=0.042 μM	21291867
DLD-1	0.5 μM	Growth Inhibition Assay	72 h	IC50<0.8 μM	26136684
DND41		Cytotoxic Assay	72 h	IC50=0.1 μM	25878331
DOX40	4 μM	Growth Inhibition Assay	72 h	IC50=5.48 μM	20382844
FLO-1	0.5 μM	Cytotoxic Assay	24 h	Decreases cell survival	22972611
GB169	1 μM	Growth Inhibition Assay	7 d	IC50=0.032 μM	25106428
GB30	1 μM	Growth Inhibition Assay	7 d	IC50=0.011 μM	25106428
GB9	1 μM	Growth Inhibition Assay	7 d	IC50=0.024 μM	25106428
Granta-4	10 μM	Cytotoxic Assay	7 d	IC50=0.040 μM	21291867
H9		Cytotoxic Assay	72 h	IC50=0.6 μM	25878331
HCT116	0.5 μM	Growth Inhibition Assay	72 h	IC50=0.04 μM	26136684
HCT15	0.5 μM	Growth Inhibition Assay	72 h	IC50<0.4 μM	26136684
HF2303	100 μM	Cytotoxic Assay	24 h	IC50=0.060 μM	22274399
HF2359	100 μM	Cytotoxic Assay	24 h	IC50=0.060 μM	22274399
HF2414	100 μM	Cytotoxic Assay	24 h	IC50=0.080 μM	22274399
HF66	100 μM	Cytotoxic Assay	24 h	IC50=0.225 μM	22274399
HH		Cytotoxic Assay	72 h	IC50=0.7 μM	25878331
HL-60	3 μM	Growth Inhibition Assay	72 h	Diminishes cell viability	22488249
HSC-3	1 μM	Growth Inhibition Assay	48 h	IC50=0.54 μM	25366143
IMR32	10 μM	Cytotoxic Assay	72 h	IC50=0.03 μM	22669335
INA6	4 μM	Growth Inhibition Assay	72 h	IC50=0.002 μM	20382844
J.Cam 1.6		Cytotoxic Assay	72 h	IC50=0.105 μM	25878331
Jeko-1		Cytotoxic Assay	72 h	IC50=0.029 μM	25878331
JVM-2		Cytotoxic Assay	72 h	IC50=0.01 μM	25878331
K562	10 μM	Growth Inhibition Assay	96 h	IC50=0.087 μM	21091633
Karpas-299	10 μM	Growth Inhibition Assay	96 h	IC50=0.038 μM	20108338
Kasumi-1	10 μM	Growth Inhibition Assay	96 h	IC50=0.103 μM	20108338
KG-1	3 μM	Growth Inhibition Assay	72 h	Diminishes cell viability	22488249
LAMA-84	10 μM	Growth Inhibition Assay	96 h	IC50=0.057 μM	21091633
LA-N-6	10 μM	Growth Inhibition Assay	96 h	IC50=0.054 μM	21448591
Leio285	75 nM	Cytotoxic Assay	96 h	Induces apoptosis	22821997
LN18	100 μM	Cytotoxic Assay	24 h	IC50=0.210 μM	22274399
LN443	100 μM	Cytotoxic Assay	24 h	IC50=0.220 μM	22274399
LR5	4 μM	Growth Inhibition Assay	72 h	IC50=2.53 μM	20382844
LS174T	0.5 μM	Growth Inhibition Assay	72 h	IC50=0.05 μM	26136684
LS180	0.5 μM	Growth Inhibition Assay	72 h	IC50=1 μM	26136684
MCF7	5 μM	Function Assay	24 h	Induces G2/M arrest	25834401
MCF7	5 μM	Function Assay	24 h	Decreases the expression level of CDK1/CDC2	25834401
MCF7	5 μM	Function Assay	24 h	Decreases the expression level of CDK2	25834401
MCF7	5 μM	Function Assay	24 h	Decreases the expression level of cyclin B1	25834401
MCF7	5 μM	Function Assay	24 h	Increases the expression level of p21 Waf1/Cip1	25834401
MCF7	5 μM	Function Assay	24 h	Increases the expression level of p27 Kip1	25834401
MCF7	5 μM	Apoptosis Assay	24 h	Induces apoptotic death	25834401
MCF7	1 μM	Function Assay	72 h	Induces autophagic death	25834401
MDA-MB-231	5 μM	Function Assay	24 h	Induces G3/M arrest	25834401
MDA-MB-231	5 μM	Function Assay	24 h	Decreases the expression level of CDK1/CDC2	25834401
MDA-MB-231	1 μM	Function Assay	24 h	Increases the expression level of CDK2	25834401
MDA-MB-231	5 μM	Function Assay	24 h	Decreases the expression level of cyclin B1	25834401
MDA-MB-231	5 μM	Function Assay	24 h	Increases the expression level of p21 Waf1/Cip1	25834401
MDA-MB-231	5 μM	Function Assay	24 h	Increases the expression level of p27 Kip1	25834401
MDA-MB-231	5 μM	Function Assay	24 h	Increases the expression level of p53	25834401
MDA-MB-231	5 μM	Apoptosis Assay	24 h	Induces apoptotic death	25834401
MDA-MB-231	1 μM	Function Assay	72 h	Induces autophagic death	25834401
Mes-Sa	75 nM	Cytotoxic Assay	96 h	Induces apoptosis	22821997
MG-63	50 μM	Growth Inhibition Assay	24 h	IC50=9.5 μM	25792811
MG-63	5 μM	Apoptosis Assay	24 h	Induces apoptotic cell death	25792811
MG-63	5 μM	Function Assay	24 h	Promotes autophagic cell death	25792811
MIP-101	0.5 μM	Growth Inhibition Assay	72 h	IC50=1 μM	26136684
MM15	4 μM	Growth Inhibition Assay	72 h	IC50=0.13 μM	20382844
MM1R	4 μM	Growth Inhibition Assay	72 h	IC50=1.68 μM	20382844
MOLM-13	3 μM	Growth Inhibition Assay	72 h	Diminishes cell viability	22488249
Molt-4	10 μM	Cytotoxic Assay	72 h	IC50=0.02 μM	22669335
MOLT-4	10 μM	Growth Inhibition Assay	96 h	IC50=0.026 μM	20108338
MV4-11	3 μM	Growth Inhibition Assay	72 h	Diminishes cell viability	22488249
NALM-6	10 μM	Growth Inhibition Assay	96 h	IC50=0.062 μM	20108338
NB-1643	10 μM	Growth Inhibition Assay	96 h	IC50=0.037 μM	21448591
NB-EBc1	10 μM	Growth Inhibition Assay	96 h	IC50=0.050 μM	21448591
NCI-N78	25 μM	Growth Inhibition Assay	24 h	IC50=26.33 μM	25609923
NCI-N78	5 μM	Apoptosis Assay	24 h	Induces apoptosis	25609923
NCI-N78	5 μM	Function Assay	24 h	Induces the autophagy	25609923
NOMO-1	3 μM	Growth Inhibition Assay	72 h	Diminishes cell viability	22488249
OCI-Ly10		Cytotoxic Assay	72 h	IC50=0.058 μM	25878331
OCI-LY7		Cytotoxic Assay	72 h	IC50=0.081 μM	25878331
OCL-AML2	3 μM	Growth Inhibition Assay	72 h	Diminishes cell viability	22488249
OE33	0.5 μM	Cytotoxic Assay	24 h	Decreases cell survival	22972611
OPM1	4 μM	Growth Inhibition Assay	72 h	IC50=0.03 μM	20382844
OPM2	4 μM	Growth Inhibition Assay	72 h	IC50=4.37 μM	20382844
OVCAR4	100 μM	Growth Inhibition Assay	24 h	IC50=22.13 μM	25624750
OVCAR4	5 μM	Function Assay	72 h	Induces G2/M arrest	25624750
OVCAR4	5 μM	Apoptosis Assay	24 h	Induces apoptosis	25624750
OVCAR-5	50 nM	Function Assay		Inhibits cell migration	23334327
PANC-1	50 μM	Growth Inhibition Assay	24 h	IC50=7.1 μM	25632225
PANC-1	5 μM	Function Assay	24 h	Induces cell cycle arrest in G2/M phase	25632225
PANC-1	5 μM	Function Assay	24 h	Induces autophagic cell death	25632225
PL-21	3 μM	Growth Inhibition Assay	72 h	Diminishes cell viability	22488249
Ramos-RA1	10 μM	Growth Inhibition Assay	96 h	IC50=0.127 μM	20108338
RD	10 μM	Growth Inhibition Assay	96 h	IC50=0.228 μM	20108338
Rec-1		Cytotoxic Assay	72 h	IC50=0.087 μM	25878331
Rh30	10 μM	Growth Inhibition Assay	96 h	IC50=0.230 μM	20108338
Rh41	10 μM	Growth Inhibition Assay	96 h	IC50=0.090 μM	20108338
RL	10 μM	Cytotoxic Assay	7 d	IC50=0.015 μM	21291867
RPM1	4 μM	Growth Inhibition Assay	72 h	IC50=10.32 μM	20382844
RS4-11	10 μM	Growth Inhibition Assay	96 h	IC50=0.018 μM	20108338
RT4	1 μM	Function Assay	48 h	Induces cell cycle arrest	23403633
RT4	3.16 μM	Apoptosis Assay	96 h	IC50=0.1198 μM	23403633
S462	100 μM	Growth Inhibition Assay	72 h	Attenuates cell growth	23328114
SH2	3 μM	Growth Inhibition Assay	72 h	Diminishes cell viability	22488249
SJ-GBM2	10 μM	Growth Inhibition Assay	96 h	IC50=0.050 μM	20108338
SKLMS	75 nM	Cytotoxic Assay	96 h	Induces apoptosis	22821997
SKM-1	3 μM	Growth Inhibition Assay	72 h	Diminishes cell viability	22488249
SK-N-BE-1	10 μM	Growth Inhibition Assay	96 h	IC50=0.028 μM	21448591
SK-N-BE-2	10 μM	Growth Inhibition Assay	96 h	IC50=0.036 μM	21448591
SK-N-MC	10 μM	Growth Inhibition Assay	96 h	IC50=0.072 μM	21448591
SKOV3	100 μM	Growth Inhibition Assay	24 h	IC50=20.48 μM	25624750
SKOV3	5 μM	Function Assay	72 h	Induces G2/M arrest	25624750
SKOV3	5 μM	Apoptosis Assay	24 h	Induces apoptosis	25624750
SKOV3ip2	50 nM	Function Assay		Inhibits cell migration	23334327
SMS-KAN	10 μM	Growth Inhibition Assay	96 h	IC50=0.034 μM	21448591
SMS-KANR	10 μM	Growth Inhibition Assay	96 h	IC50=0.026 μM	21448591
SMS-KCN	10 μM	Growth Inhibition Assay	96 h	IC50=0.019 μM	21448591
SMS-KCNR	10 μM	Growth Inhibition Assay	96 h	IC50=0.010 μM	21448591
SMS-LHN	10 μM	Growth Inhibition Assay	96 h	IC50=0.032 μM	21448591
SMS-MSN	10 μM	Growth Inhibition Assay	96 h	IC50=0.022 μM	21448591
SMS-SAN	10 μM	Growth Inhibition Assay	96 h	IC50=0.020 μM	21448591
SNU1544	0.5 μM	Growth Inhibition Assay	72 h	IC50=1 μM	26136684
SU-DHL2		Cytotoxic Assay	72 h	IC50=0.01 μM	25878331
SU-DHL6		Cytotoxic Assay	72 h	IC50=0.482 μM	25878331
Sup-T1		Cytotoxic Assay	72 h	IC50=2.142 μM	25878331
SW948	0.5 μM	Growth Inhibition Assay	72 h	IC50=1 μM	26136684
T24	1 μM	Function Assay	48 h	Induces cell cycle arrest	23403633
T24	3.16 μM	Apoptosis Assay	96 h	IC50=0.0306 μM	23403633
T84	0.5 μM	Growth Inhibition Assay	72 h	IC50=0.09 μM	26136684
T98	100 μM	Cytotoxic Assay	24 h	IC50=0.125 μM	22274399
TC-32	10 μM	Growth Inhibition Assay	96 h	IC50=0.039 μM	21448591
TC-71	10 μM	Growth Inhibition Assay	96 h	IC50=0.102 μM	21448591
TC-71	10 μM	Growth Inhibition Assay	96 h	IC50=0.102 μM	20108338
Tib 152		Cytotoxic Assay	72 h	IC50=0.8 μM	25878331
TIB-48	100 μM	Growth Inhibition Assay		IC50=0.088 μM	23153524
TIB-48	1 μM	Cytotoxic Assay	48 h	Induces apoptosis	23153524
U-2 OS	50 μM	Growth Inhibition Assay	24 h	IC50=16.6 μM	25792811
U-2 OS	5 μM	Apoptosis Assay	24 h	Induces apoptotic cell death	25792811
U-2 OS	5 μM	Function Assay	24 h	Promotes autophagic cell death	25792811
U251	100 μM	Cytotoxic Assay	24 h	IC50=0.100 μM	22274399
U266	4 μM	Growth Inhibition Assay	72 h	IC50=1.43 μM	20382844
U87	100 μM	Cytotoxic Assay	24 h	IC50=0.105 μM	22274399
UM-UC-3	1 μM	Function Assay	48 h	Induces cell cycle arrest	23403633
UM-UC-3	3.16 μM	Apoptosis Assay	96 h	IC50=0.0449 μM	23403633
Z-138		Cytotoxic Assay	72 h	IC50=0.013 μM	25878331

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02551055	Neoplasms, Advanced or Metasta... 展开 >>tic 收起 <<	Phase 1	Terminated(Business Decision; ... 展开 >>No Safety Or Efficacy Concerns.) 收起 <<	-	United States, New York ... 展开 >> Lake Success, New York, United States New York, New York, United States United States, Pennsylvania Philadelphia, Pennsylvania, United States United States, Texas Dallas, Texas, United States Houston, Texas, United States Spain Barcelona, Spain 收起 <<
NCT01540682	Head and Neck Cancer	Phase 1	Completed	-	United States, Pennsylvania ... 展开 >> Abramson Cancer Center of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 收起 <<
NCT01316692	Recurrent Melanoma ... 展开 >> Stage IIIc Melanoma Stage IV Melanoma 收起 <<	Phase 2	Terminated(low accrual)	-	United States, Tennessee ... 展开 >> Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37232-6838 收起 <<
NCT01316692	-		Terminated(low accrual)	-	-
NCT01677559	Adenocarcinoma ... 展开 >> Pancreatic Neoplasms 收起 <<	Phase 1	Completed	-	United States, Missouri ... 展开 >> Washington University School of Medicine Saint Louis, Missouri, United States, 63110 收起 <<
NCT02327169	Advanced Nonhematologic Malign... 展开 >>ancies 收起 <<	Phase 1	Completed	-	United States, Massachusetts ... 展开 >> Massachusetts General Hospital Cancer Center Boston, Massachusetts, United States, 2114 Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 2115 Dana Farber Cancer Institute Boston, Massachusetts, United States, 2115 United States, Pennsylvania Fox Chase Cancer Center Philadelphia, Pennsylvania, United States, 19111 United States, Texas The University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 France Institut Bergonie Bordeaux cedex, Gironde, France, 33076 Institut Claudius Regaud-Oncopole Toulouse cedex 09, Haute Garonne, France, 31059 Institut Gustave Roussy Villejuif cedex, Val De Marne, France, 94805 Spain Hospital Universitari Vall d'Hebron Barcelona, Spain, 8035 START Madrid. Fundacion Jimenez Diaz Madrid, Spain, 28040 Hospital Clinico Universitario Virgen de la Victoria Malaga, Spain, 29010 United Kingdom Sarah Cannon Research Institure UK London, Greater London, United Kingdom, W1G 6AD The Chrisie Manchester, Greater Manchester, United Kingdom, M20 4BX Churchill Hospital Oxford, Oxfordshire, United Kingdom, OX3 7LJ 收起 <<
NCT02780011	CD30-positive Lymphoma ... 展开 >> CD30-positive Solid Tumor 收起 <<	Phase 1	Withdrawn(lack of funding)	September 2018	United States, Texas ... 展开 >> Houston Methodist Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT01397825	Diffuse Large B-Cell Lymphoma ... 展开 >> Transformed Follicular Lymphoma Mantle Cell Lymphoma Burkitt's Lymphoma 收起 <<	Phase 1 Phase 2	Completed	-	-
NCT01601535	Neuroblastoma	Phase 1 Phase 2	Active, not recruiting	December 2018	United States, California ... 展开 >> Children's Hospital Los Angeles Los Angeles, California, United States, 90027-0700 Lucile Packard Children's Hospital at Stanford University Medical Center Palo Alto, California, United States, 94304 UCSF Helen Diller Family Comprehensive Cancer Center San Francisco, California, United States, 94115 United States, Colorado Children Hospital of Colorado Aurora, Colorado, United States, 80045 United States, Georgia Children's Healthcare of Atlanta Atlanta, Georgia, United States, 30322 United States, Illinois University of Chicago Comer Children's Hospital Chicago, Illinois, United States, 60637 United States, Massachusetts Childrens Hospital Boston, Dana-Farber Cancer Institute. Boston, Massachusetts, United States, 02115 United States, Michigan University of Michigan Comprehensive Cancer Center Ann Arbor, Michigan, United States, 48109 United States, Ohio Cincinnati Children's Hospital Medical Center Cincinnati, Ohio, United States, 45229-3039 United States, Pennsylvania Children's Hospital of Philadelphia Philadelphia, Pennsylvania, United States, 19104-4318 United States, Texas Cook Children's Medical Center - Fort Worth Fort Worth, Texas, United States, 76104 United States, Washington Children's Hospital and Regional Medical Center - Seattle Seattle, Washington, United States, 98105 Canada, Ontario Hospital for Sick Children Toronto, Ontario, Canada, M5G 1X8 收起 <<
NCT01034553	-		Completed	-	-
NCT01397825	-		Completed	-	-
NCT00500903	Advanced Malignancies	Phase 1	Completed	-	United States, Tennessee ... 展开 >> Sarah Cannon Research Institute (SCRI) Nashville, Tennessee, United States, 37203 收起 <<
NCT00962091	Advanced Solid Tumors	Phase 1	Completed	-	United States, California ... 展开 >> Premiere Oncology, A Medical Corporation Santa Monica, California, United States, 90404 收起 <<
NCT01034553	Refractory Multiple Myeloma	Phase 1 Phase 2	Completed	-	United States, Arizona ... 展开 >> Mayo Clinic in Arizona Scottsdale, Arizona, United States, 85259 United States, California University of California, San Francisco San Fransisco, California, United States, 94143 United States, Massachusetts Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Missouri Washington University School of Medicine Saint Louis, Missouri, United States, 63110 United States, Ohio Ohio State University Columbus, Ohio, United States, 43210 收起 <<
NCT01154816	Hepatoblastoma ... 展开 >> Previously Treated Childhood Rhabdomyosarcoma Recurrent Childhood Acute Lymphoblastic Leukemia Recurrent Childhood Acute Myeloid Leukemia Recurrent Childhood Kidney Neoplasm Recurrent Childhood Malignant Germ Cell Tumor Recurrent Childhood Rhabdomyosarcoma Recurrent Childhood Soft Tissue Sarcoma Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor Recurrent Neuroblastoma Recurrent Osteosarcoma 收起 <<	Phase 2	Completed	-	-
NCT01094288	Advanced Solid Tumors ... 展开 >> Adenocarcinoma of the Prostate 收起 <<	Phase 1	Completed	-	United States, Indiana ... 展开 >> Indianapolis, Indiana, United States United States, Oregon Portland, Oregon, United States United States, Texas San Antonio, Texas, United States United States, Washington Seattle, Washington, United States 收起 <<
NCT01482962	Relapsed Peripheral T-Cell Lym... 展开 >>phoma Refractory Peripheral T-Cell Lymphoma 收起 <<	Phase 3	Completed	-	-
NCT01154816	-		Completed	-	-
NCT00651664	Advanced Malignancies	Phase 1	Completed	-	Spain ... 展开 >> Ciutat Sanitaria Vall d'Hebron - Servicio de Oncologia Barcelona, Spain, 08035 H. Clínico Universitario de Valencia Valencia, Spain 收起 <<
NCT02560025	Acute Myeloid Leukemia	Phase 2	Active, not recruiting	October 2019	United States, Massachusetts ... 展开 >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Dana Farber Cancer Institute Boston, Massachusetts, United States, 02215 收起 <<
NCT02114229	Malignant Rhabdoid Tumor ... 展开 >> Atypical Teratoid Rhabdoid Tumor 收起 <<	Phase 2	Recruiting	May 2027	United States, California ... 展开 >> Children's Hospital of Los Angeles Withdrawn Los Angeles, California, United States, 90027 Lucille Packard Children's Hospital at Stanford University Medical Center Recruiting Palo Alto, California, United States, 94304 Contact: Sonia Partap, MD 650-723-0993 spartap@stanford.edu Principal Investigator: Sonia Partap, MD Rady Children's Hospital Recruiting San Diego, California, United States, 92123 Contact: John Crawford, MD, MS 858-576-1700 jcrawford@rchsd.org Principal Investigator: John Crawford, MD, MS United States, Colorado Children's Hospital Colorado Recruiting Aurora, Colorado, United States, 80045 Contact: Kathleen Dorris, MD 720-777-6672 kathleen.dorris@childrenscolorado.org Principal Investigator: Kathleen Dorris, MD United States, District of Columbia Children's National Medical Center Recruiting Washington, District of Columbia, United States, 20010 Contact: Lindsay B. Kilburn, MD 202-476-2800 lkilburn@childrensnational.org Principal Investigator: Lindsay B. Kilburn, MD United States, Florida UF Cancer Center at Orlando Health Recruiting Orlando, Florida, United States, 32806 Contact: Amy A. Smith, MD 321-841-7246 amy.smith@orlandohealth.com Principal Investigator: Amy A. Smith, MD United States, Georgia Children's Healthcare of Atlanta Recruiting Atlanta, Georgia, United States, 30322 Contact: Sindy Moon 404-785-1441 cindy.moon@choa.org Contact: Jaclyn Smith 404-785-0692 jaclyn.smith@choa.org Principal Investigator: Dolly Aguilera, MD United States, Minnesota Children's Hospital and Clinics of Minnesota Recruiting Minneapolis, Minnesota, United States, 55102 Contact: Anne Bendel, MD 651-220-6732 anne.bendel@childrensmn.org Principal Investigator: Anne Bendel, MD United States, Tennessee St. Jude Children's Research Hospital Recruiting Memphis, Tennessee, United States, 38105 Contact: Tabatha E. Doyle, RN 901-595-2544 tabatha.doyle@stjude.org Principal Investigator: Santhosh Upadhyaya, MD United States, Texas Texas Children's Hospital Recruiting Houston, Texas, United States, 77030 Contact: Patricia Baxter, MD 832-824-1000 pabaxter@txch.org Principal Investigator: Patricia Baxter, MD United States, Washington Seattle Children's Hospital Recruiting Seattle, Washington, United States, 98105 Contact: Sarah Leary, MD 866-987-2000 sarah.leary@seattlechildrens.org Principal Investigator: Sarah Leary, MD 收起 <<
NCT01897012	MYC Positive ... 展开 >>Recurrent B-Cell Non-Hodgkin Lymphoma Recurrent Burkitt Lymphoma Recurrent Diffuse Large B-Cell Lymphoma Recurrent Follicular Lymphoma Recurrent High Grade B-Cell Lymphoma With MYC and BCL2 or BCL6 Rearrangements Recurrent Hodgkin Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Mature T- and NK-Cell Non-Hodgkin Lymphoma Refractory B-Cell Non-Hodgkin Lymphoma Refractory Burkitt Lymphoma Refractory Diffuse Large B-Cell Lymphoma Refractory Follicular Lymphoma Refractory High Grade B-Cell Lymphoma With MYC and BCL2 or BCL6 Rearrangements Refractory Hodgkin Lymphoma Refractory Mantle Cell Lymphoma Refractory Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma 收起 <<	Phase 1	Active, not recruiting	-	United States, Texas ... 展开 >> M D Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT03005262	-		-	-	-
NCT02560025	-		Active, not recruiting	-	-
NCT02038647	Small Cell Lung Cancer (SCLC)	Phase 2	Active, not recruiting	August 7, 2017	-
NCT01471964	Non-small Cell Lung Cancer Met... 展开 >>astatic Non-small Cell Lung Cancer Recurrent 收起 <<	Phase 1 Phase 2	Terminated(Phase I portion com... 展开 >>pleted. Phase II will open pending amendment approval.) 收起 <<	-	United States, Pennsylvania ... 展开 >> Fox Chase Cancer Center Philadelphia, Pennsylvania, United States, 19111 收起 <<
NCT01482962	-		Completed	-	-
NCT01695941	Recurrent B-Cell Non-Hodgkin L... 展开 >>ymphoma Recurrent Mantle Cell Lymphoma Refractory B-Cell Non-Hodgkin Lymphoma Refractory Mantle Cell Lymphoma 收起 <<	Phase 1	Active, not recruiting	-	United States, New York ... 展开 >> Montefiore Medical Center-Einstein Campus Bronx, New York, United States, 10461 Montefiore Medical Center - Moses Campus Bronx, New York, United States, 10467 Laura and Isaac Perlmutter Cancer Center at NYU Langone New York, New York, United States, 10016 United States, Pennsylvania Fox Chase Cancer Center Philadelphia, Pennsylvania, United States, 19111 收起 <<
NCT02367352	Advanced Solid Tumors ... 展开 >> Ovarian Cancer Small Cell Lung Cancer 收起 <<	Phase 1	Completed	-	Japan ... 展开 >> Chiba, Japan Shizuoka, Japan Korea, Republic of Seoul, Korea, Republic of 收起 <<
NCT01923337	Mucinous Adenocarcinoma of the... 展开 >> Colon Mucinous Adenocarcinoma of the Rectum Recurrent Colon Cancer Recurrent Rectal Cancer Signet Ring Adenocarcinoma of the Colon Signet Ring Adenocarcinoma of the Rectum Stage IIIA Colon Cancer Unspecified Adult Solid Tumor, Protocol Specific 收起 <<	Phase 1	Active, not recruiting	December 2019	United States, California ... 展开 >> UC Davis Comprehensive Cancer Center Sacramento, California, United States, 95817 收起 <<
NCT02444884	Unspecified Childhood Solid Tu... 展开 >>mor, Excluding CNS Neuroblastoma 收起 <<	Phase 1	Completed	-	-
NCT01924260	Acinar Cell Adenocarcinoma of ... 展开 >>the Pancreas Duct Cell Adenocarcinoma of the Pancreas Recurrent Pancreatic Cancer Stage III Pancreatic Cancer Stage IV Pancreatic Cancer Unspecified Adult Solid Tumor, Protocol Specific 收起 <<	Phase 1	Active, not recruiting	December 2020	United States, California ... 展开 >> UC Davis Comprehensive Cancer Center Sacramento, California, United States, 95817 收起 <<
NCT01466881	Adult Nasal Type Extranodal NK... 展开 >>/T-Cell Lymphoma Anaplastic Large Cell Lymphoma Angioimmunoblastic T-Cell Lymphoma Hepatosplenic T-Cell Lymphoma Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma Recurrent Adult Non-Hodgkin Lymphoma Recurrent Adult T-Cell Leukemia/Lymphoma 收起 <<	Phase 2	Completed	-	-
NCT01045421	-		Completed	-	-
NCT01637961	Recurrent Uterine Corpus Sarco... 展开 >>ma Uterine Corpus Leiomyosarcoma 收起 <<	Phase 2	Completed	-	-
NCT01637961	-		Completed	-	-
NCT01466881	-		Completed	-	-
NCT01799278	Small Cell Prostate Cancer ... 展开 >> Neuroendocrine Prostate Cancer Prostate Adenocarcinoma Plus > 50% Immunohistochemical Staining for Neuroendocrine Markers 收起 <<	Phase 2	Completed	-	United States, Illinois ... 展开 >> University of Chicago Chicago, Illinois, United States, 60637 United States, Michigan Karmanos Cancer Institute Detroit, Michigan, United States, 48201 United States, New Jersey Rutgers Cancer Institute of New Jersey New Brunswick, New Jersey, United States, 08903 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 Weill Cornell Medical College New York, New York, United States, 10065 United States, North Carolina Duke University Health System Durham, North Carolina, United States, 27710 United States, Ohio University Hospitals Cleveland Medical Center Cleveland, Ohio, United States, 44106 United States, Washington University of Washington Medical Center Seattle, Washington, United States, 98195 收起 <<
NCT01653028	-		Completed	-	-
NCT00697346	B-cell Follicular Lymphoma ... 展开 >> B-cell Marginal Zone Lymphoma Diffuse Large B-cell Lymphoma B-cell Mantle Cell Lymphoma B-cell Small Lymphocytic Lymphoma (SLL) B-Cell Chronic Lymphocytic Leukemia (B-CLL) Multiple Myeloma Waldenstrom's Macroglobulinemia Noncutaneous Peripheral T-cell Lymphoma Not Otherwise Specified (PTCL-NOS) Angioimmunoblastic T-cell Lymphoma (AITL) Anaplastic Large Cell Lymphoma Enteropathy Associated T-cell Lymphoma (EATCL) NK Lymphoma (NKL) 收起 <<	Phase 1	Completed	-	United States, Arizona ... 展开 >> Scottsdale, Arizona, United States United States, Kentucky Lexington, Kentucky, United States United States, Maryland Baltimore, Maryland, United States United States, Nebraska Omaha, Nebraska, United States United States, New Jersey Hackensack, New Jersey, United States United States, New York Buffalo, New York, United States United States, North Carolina Chapel Hill, North Carolina, United States United States, Tennessee Nashville, Tennessee, United States United States, Texas Houston, Texas, United States San Antonio, Texas, United States 收起 <<
NCT01091428	Ovarian Carcinoma ... 展开 >> Fallopian Tube Cancer Peritoneal Cancer Breast Carcinoma 收起 <<	Phase 2	Completed	-	United States, New York ... 展开 >> Bronx, New York, United States United States, Pennsylvania Philadelphia, Pennsylvania, United States United States, Texas Houston, Texas, United States United States, Washington Seattle, Washington, United States 收起 <<
NCT02319018	Malignant Digestive System Neo... 展开 >>plasm 收起 <<	Phase 1	Completed	-	United States, Connecticut ... 展开 >> Smilow Cancer Center/Yale-New Haven Hospital New Haven, Connecticut, United States, 06510 Yale University New Haven, Connecticut, United States, 06520 United States, Maryland Johns Hopkins University/Sidney Kimmel Cancer Center Baltimore, Maryland, United States, 21287 United States, Michigan Wayne State University/Karmanos Cancer Institute Detroit, Michigan, United States, 48201 United States, Tennessee Vanderbilt University/Ingram Cancer Center Nashville, Tennessee, United States, 37232 收起 <<
NCT01045421	Advanced Nonhematological Mali... 展开 >>gnancies Non-Small Cell Lung Cancer Small Cell Lung Cancer Metastatic Breast Cancer Head and Neck Squamous Cell Carcinoma Gastroesophageal Adenocarcinoma 收起 <<	Phase 1 Phase 2	Completed	-	United States, Texas ... 展开 >> Houston, Texas, United States United States, Utah Salt Lake City, Utah, United States 收起 <<
NCT01639911	Malignant Neoplasm of Breast ... 展开 >> CNS Malignancy Malignant Neoplasm of Gastrointestinal Tract Genitourinary Neoplasms Malignancy and Gender Unspecified Head and Neck Neoplasms Melanoma Malignant Neoplasm of Thorax 收起 <<	Phase 1	Completed	-	United States, Illinois ... 展开 >> University of Illinois Cancer Center Chicago, Illinois, United States, 60612 收起 <<
NCT01653028	Myxofibrosarcoma ... 展开 >> Recurrent Adult Soft Tissue Sarcoma Recurrent Leiomyosarcoma Recurrent Liposarcoma Recurrent Malignant Peripheral Nerve Sheath Tumor Recurrent Undifferentiated Pleomorphic Sarcoma Stage III Soft Tissue Sarcoma AJCC v7 Stage IV Soft Tissue Sarcoma AJCC v7 收起 <<	Phase 2	Completed	-	-
NCT00853307	Ovarian Carcinoma	Phase 2	Completed	-	United States, New Jersey ... 展开 >> Summit Medical Group Berkeley Heights, New Jersey, United States, 07922 收起 <<
NCT00853307	-		Completed	-	-
NCT01567709	Adult B Acute Lymphoblastic Le... 展开 >>ukemia Adult T Acute Lymphoblastic Leukemia Anaplastic Large Cell Lymphoma Angioimmunoblastic T-Cell Lymphoma Chronic Lymphocytic Leukemia Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue Hepatosplenic T-Cell Lymphoma Intraocular Lymphoma Lymphomatous Involvement of Non-Cutaneous Extranodal Site Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma Nodal Marginal Zone Lymphoma Primary Cutaneous B-Cell Non-Hodgkin Lymphoma Recurrent Adult Acute Lymphoblastic Leukemia Recurrent Adult Burkitt Lymphoma Recurrent Adult Grade III Lymphomatoid Granulomatosis Recurrent Adult Hodgkin Lymphoma Recurrent Adult Immunoblastic Lymphoma Recurrent Adult Lymphoblastic Lymphoma Recurrent Adult T-Cell Leukemia/Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Marginal Zone Lymphoma Recurrent Mycosis Fungoides and Sezary Syndrome Recurrent Non-Hodgkin Lymphoma Recurrent Primary Cutaneous T-Cell Non-Hodgkin Lymphoma Recurrent Small Lymphocytic Lymphoma Refractory Chronic Lymphocytic Leukemia Refractory Hairy Cell Leukemia Small Intestinal Lymphoma Splenic Marginal Zone Lymphoma T-Cell Large Granular Lymphocyte Leukemia Testicular Lymphoma Waldenstrom Macroglobulinemia 收起 <<	Phase 1	Completed	-	United States, California ... 展开 >> City of Hope Comprehensive Cancer Center Duarte, California, United States, 91010 USC / Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 University of California Davis Comprehensive Cancer Center Sacramento, California, United States, 95817 United States, Pennsylvania Penn State Milton S Hershey Medical Center Hershey, Pennsylvania, United States, 17033-0850 University of Pittsburgh Cancer Institute (UPCI) Pittsburgh, Pennsylvania, United States, 15232 收起 <<
NCT01091428	-		Completed	-	-
NCT01799278	-		Completed	-	-
NCT00830518	-		Completed	-	-
NCT02187991	Breast Cancer ... 展开 >> Breast Carcinoma Breast Tumors Malignant Neoplasm of Breast 收起 <<	Phase 2	Active, not recruiting	September 2019	United States, Texas ... 展开 >> 22 Sites Including Dallas And Austin, Texas, United States 收起 <<
NCT01848067	Adenocarcinoma of the Prostate... 展开 >> Hormone-resistant Prostate Cancer Recurrent Prostate Cancer Stage IV Prostate Cancer 收起 <<	Phase 1 Phase 2	Completed	-	United States, Pennsylvania ... 展开 >> Thomas Jefferson University Philadelphia, Pennsylvania, United States, 19107 收起 <<
NCT01848067	-		Completed	-	-
NCT01779843	Acute Myelogenous Leukemia	Phase 1	Completed	-	United States, Massachusetts ... 展开 >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Brigham and Women's Hospital Boston, Massachusetts, United States, 02215 Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02215 收起 <<
NCT00830518	Acute Myelogenous Leukemia ... 展开 >> High-Grade Myelodysplastic Syndrome 收起 <<	Phase 2	Completed	-	United States, New Jersey ... 展开 >> Hematology and Oncology Associates of Northern New Jersey Morristown, New Jersey, United States, 07962 收起 <<
NCT02219789	Estrogen Receptor Positive ... 展开 >> Progesterone Receptor Positive Recurrent Breast Carcinoma Stage IIIB Breast Cancer Stage IIIC Breast Cancer Stage IV Breast Cancer 收起 <<	Phase 1	Completed	-	United States, Minnesota ... 展开 >> Mayo Clinic Rochester, Minnesota, United States, 55905 收起 <<
NCT01812005	-		Terminated(Slow patient enroll... 展开 >>ment and study discontinued after 14 patients enrolled) 收起 <<	-	-
NCT01812005	Extranodal Marginal Zone B-cel... 展开 >>l Lymphoma of Mucosa-associated Lymphoid Tissue Nodal Marginal Zone B-cell Lymphoma Recurrent Adult Burkitt Lymphoma Recurrent Adult Diffuse Large Cell Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Marginal Zone Lymphoma Splenic Marginal Zone Lymphoma Waldenström Macroglobulinemia 收起 <<	Phase 2	Terminated(Slow patient enroll... 展开 >>ment and study discontinued after 14 patients enrolled) 收起 <<	-	United States, Georgia ... 展开 >> Emory University Atlanta, Georgia, United States, 30322 United States, Ohio Arthur G. James Cancer Hospital and Solove Research Institute at Ohio State University Medical Center Columbus, Ohio, United States, 43210 收起 <<
NCT02860000	Estrogen Receptor Status ... 展开 >> HER2/Neu Negative Invasive Breast Carcinoma Postmenopausal Stage III Breast Cancer Stage IIIA Breast Cancer Stage IIIB Breast Cancer Stage IIIC Breast Cancer Stage IV Breast Cancer 收起 <<	Phase 2	Recruiting	December 15, 2021	United States, Minnesota ... 展开 >> Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Clinical Trials Referral Office 855-776-0015 Principal Investigator: Tufia C. Haddad 收起 <<
NCT00807495	Diffuse Large B-cell Lymphoma ... 展开 >> Mantle Cell Lymphoma Burkitt's Lymphoma T-cell Lymphoma, Excluding Primary Cutaneous T-cell Lymphoma Transformed Follicular Lymphoma With ≥ 50% Diffuse Large Cell Component 收起 <<	Phase 2	Completed	-	United States, New Jersey ... 展开 >> Hematology Oncology Associates, Virtua Memorial Hospital Burlington County Mount Holly, New Jersey, United States, 08060 收起 <<
NCT00807495	-		Completed	-	-
NCT02259010	Advanced Solid Tumors ... 展开 >> Relapsed/Refractory Lymphoma 收起 <<	Phase 1	Unknown	April 2016	United States, Missouri ... 展开 >> St. Louis, Missouri, United States United States, Oklahoma Oklahoma City, Oklahoma, United States United States, Tennessee Germantown, Tennessee, United States United States, Texas Dallas, Texas, United States 收起 <<
NCT01613261	Advanced Nonhematologic Malign... 展开 >>ancies 收起 <<	Phase 1	Withdrawn	November 2015	United States, Texas ... 展开 >> South Texas Accelerated Research Therapeutics (START) San Antonio, Texas, United States, 78229 收起 <<
NCT02109328	Bladder Cancer ... 展开 >> Transitional Cell Carcinoma 收起 <<	Phase 2	Unknown	March 2018	Italy ... 展开 >> Fondazione IRCCS Istituto Nazionale dei Tumori Not yet recruiting Milano, Mi, Italy, 20133 Contact: Andrea Necchi, MD +39022390 ext 2402 andrea.necchi@istitutotumori.mi.it Sub-Investigator: Patrizia Giannatempo, MD Principal Investigator: Andrea Necchi, MD 收起 <<
NCT02530619	Acute Megakaryoblastic Leukemi... 展开 >>a Myelofibrosis Primary Myelofibrosis 收起 <<	Not Applicable	Active, not recruiting	March 2020	United States, Florida ... 展开 >> University of Miami Miller School of Medicine-Sylvester Cancer Center Miami, Florida, United States, 33136 United States, Illinois Northwestern University Chicago, Illinois, United States, 60611 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 收起 <<
NCT01844583	Solid Tumors ... 展开 >>Lymphoma 收起 <<	Phase 1	Completed	-	United States, Florida ... 展开 >> Sarasota, Florida, United States United States, Missouri St. Louis, Missouri, United States United States, Oklahoma Oklahoma City, Oklahoma, United States United States, Tennessee Nashville, Tennessee, United States United States, Texas Dallas, Texas, United States San Antonio, Texas, United States 收起 <<
NCT02293005	Lung Cancer M... 展开 >>esothelioma 收起 <<	Phase 2	Active, not recruiting	May 2022	United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT01512758	Advanced Solid Tumors ... 展开 >> Lymphomas 收起 <<	Phase 1	Completed	-	Singapore ... 展开 >> National Cancer Centre Tiong Bahru, Singapore, 169610 收起 <<
NCT02700022	Diffuse Large B-cell Lymphoma ... 展开 >> Follicular Lymphoma Burkitt Lymphoma 收起 <<	Phase 1	Terminated(Lack of funding)	-	United States, California ... 展开 >> City of Hope Comprehensive Cancer Center Duarte, California, United States, 91010 United States, North Carolina University of North Carolina at Chapel Hill Lineberger Comprehensive Cancer Center Chapel Hills, North Carolina, United States, 27599 收起 <<
NCT01898078	Advanced Solid Tumors ... 展开 >> Lymphoma 收起 <<	Phase 1	Active, not recruiting	February 2017	United States, New York ... 展开 >> Bronx, New York, United States United States, Tennessee Nashville, Tennessee, United States United States, Texas San Antonio, Texas, United States 收起 <<
NCT02186509	Adult Anaplastic Astrocytoma ... 展开 >> Adult Anaplastic Ependymoma Adult Anaplastic Oligodendroglioma Adult Brain Stem Glioma Adult Diffuse Astrocytoma Adult Giant Cell Glioblastoma Adult Glioblastoma Adult Gliosarcoma Adult Mixed Glioma Adult Oligodendroglioma Adult Pilocytic Astrocytoma Adult Pineal Gland Astrocytoma Adult Subependymal Giant Cell Astrocytoma Recurrent Adult Brain Tumor 收起 <<	Phase 1	Active, not recruiting	January 2019	United States, Pennsylvania ... 展开 >> Sidney Kimmel Cancer Center at Thomas Jefferson University Philadelphia, Pennsylvania, United States, 19107 收起 <<
NCT02719691	Metastatic Breast Cancer ... 展开 >> Solid Tumors 收起 <<	Phase 1	Recruiting	November 2018	United States, Colorado ... 展开 >> University of Colorado Cancer Center Recruiting Aurora, Colorado, United States, 80045 Contact: Matthew Lee 303-848-0630 matthew.lee@ucdenver.edu Principal Investigator: Jennifer Diamond, MD 收起 <<
NCT02214147	Advanced Solid Tumors ... 展开 >> Relapsed/Refractory Lymphoma 收起 <<	Phase 1	Completed	-	United States, Florida ... 展开 >> Miami, Florida, United States United States, Illinois Chicago, Illinois, United States United States, Michigan Ann Arbor, Michigan, United States United States, Missouri Saint Louis, Missouri, United States United States, Texas Dallas, Texas, United States Houston, Texas, United States San Antonio, Texas, United States 收起 <<
NCT02214147	-		Completed	-	-
NCT02812056	Malignant Neoplasms of Digesti... 展开 >>ve Organs Malignant Neoplasms of Female Genital Organs Malignant Neoplasms of Lip Oral Cavity and Pharynx Malignant Neoplasms of Male Genital Organs 收起 <<	Phase 1	Withdrawn	-	-
NCT01714947	Advanced Solid Tumors ... 展开 >> Lymphoma 收起 <<	Phase 1	Completed	-	United States, Washington ... 展开 >> Comprehensive Clinical Development Tacoma, Washington, United States, 98418 收起 <<
NCT01714947	-		Completed	-	-

靶点	Aurora A Aurora A, IC50:1.2 nM
描述	The Aurora family of serine/threonine kinases, which consists of Aurora A, B and C, plays an important role in chromosome alignment, segregation, and cytokinesis during mitosis. Alisertib is a selective Aurora A kinase inhibitor with IC50 value of 1.2nM versus 396.5nM for Aurora B (measured by enzymatic assay). Consistent with inhibition by Aurora A on cell phenotype, treatment with 50nM Alisertib casued an increase in cells in the G2/M phase at 24 and 48 hours in HCT-116 cells, as well as caused mitotic spindle abnormalities and chromosome misalignment in cells. However, at a higher concentration of 0.25 or 1μM, Alisertib caused an increase in the number of cells with 8N DNA content and multinuclear in cells, as phenotypes consistent with Aurora B inhibition. Alisertib can inhibit cell proliferation, including HCT-116, SW480, DLD-1, H460, MDA-MB-231, PC3, SKOV3, HPAC, OCI-LY-3, OCI-LY-7, OCI-LY-10, OCI-LY-19 and WSU cell lines, with IC50 values ranging in 15-469nM, suggesting its widely anti-proliferative effect on colon, lung, breast, prostate, ovarian, pancreatic and lymphoma tumor. Alisertib possessed good pharmacodynamics as orally dosed at 3, 10, and 30mg/kg with Alisertib resulted in a time- and dose-dependent increase in the mitotic marker p-HisH3, suggesting Aurora A inhibition, in tumor tissue from HCT-116 xenografts. Misaligned chromosomes and reduced bipolar mitotic spindles can also be observed. Oral administration of Alisertib at 3, 10, and 30 mg/kg once daily for 21 consecutive days dose-dependently inhibit tumor growth in nude mice bearing subcutaneous HCT-116 tumors. The broad antitumor activity of Alisertib can also be observed in a diverse set of solid tumor xenograft models as well as regressions in in vivo models of lymphoma, including the cell lines mentioned above^[1].
作用机制	Alisertib binds Aurora-A at the ATP-binding pocket.^[2]

Dose	Mice: min = 3mg/kg, max =30 mg/kg^[1]
Administration	p.o.

CAS号	1028486-01-2
分子式	C₂₇H₂₀ClFN₄O₄
分子量	518.92
SMILES Code	O=C(O)C1=CC=C(NC2=NC=C3C(C4=CC=C(Cl)C=C4C(C5=C(OC)C=CC=C5F)=NC3)=N2)C=C1OC
MDL No.	MFCD16621243

别名	MLN 8237
运输	蓝冰
InChI Key	ZLHFILGSQDJULK-UHFFFAOYSA-N
Pubchem ID	24771867

Alisertib {[allProObj[0].p_purity_real_show]}

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Alisertib {[allProObj[0].p_purity_real_show]}

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