Dinaciclib | SCH 727965 | CDK2/5/9 Inhibitor | AmBeed-信号通路专用抑制剂

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产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 HCl	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											SGK,ERK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinA, IC50: 70 nM CDK2/CyclinE, IC50: 35 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinA, IC50: 4 nM CDK2/CyclinE, IC50: 3 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinA, IC50: 8 nM CDK2/CyclinE, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinA, IC50: 45 nM CDK2/CyclinE, IC50: 363 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinA, IC50: 0.68μM CDK2/CyclinE, IC50: 7.5μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinA, IC50: 38 nM CDK2/CyclinE, IC50: 48 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 HCl	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinA, IC50: 0.7 μM CDK2/CyclinE, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 2HCl									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				99%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinA, IC50: 224 nM CDK2/CyclinE, IC50: 2.54 μM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			98%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		99%+
(E/Z)-TG003												+++ mCLK4, IC50: 15 nM mCLK1, IC50: 200 nM		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。

靶点	CDK5 CDK5, IC50:1 nM CDK2 CDK2, IC50:1 nM CDK9 CDK9, IC50:4 nM CDK1 CDK1, IC50:3 nM
描述	CDK4/6, forming a complex with its partner Cyclin D1/2/3, can mediate the phosphorylation of Rb in G1 cell cycle, as well as stimulating the synthesis cyclin E and D-type cyclins controlled by extracellular mitogens^[2]. Dinaciclib can inhibit CDK2, CDK5, CDK1, and CDK9 activity with IC50 values of 1, 1, 3 and 4 nM (measured by Recombinant cyclin/CDK), respectively. Dinaciclib strongly suppressed phosphorylation of Rb on Ser 807/811 at concentrations >6.25 nM for 16h in A2780 cells. Along with that, apoptosis as indicated by the appearance of the p85 PARP cleavage can also be observed. Dinaciclib has broad antiproliferative activity against a wide range of tumor cells, including prostate, breast, colon, SCLC, SCLC, ovarian, pancreatic, melanoma, leukemia, bladder, liver, mantle and lymphoma cell lines, with IC50 ranging from 6-17 nM. Exposure to 250-500 nM of dinaciclib is sufficient to completely suppress DNA synthesis for 24 hours in A2780 cells and that was correlated with the accumulation of apoptosis (sub-G1), which means that short exposures to dinaciclib can induce long-lasting effects in target cells. Intraperitoneal administration of dinaciclib at 8, 16, 32 and 48 mg/kg daily for 10 days resulted in tumor inhibition by 70%, 70%, 89%, and 96%, respectively, in A2780 xenograft mice^[1]. Up to now, a lot of clinical trails of dinaciclib treatment for cancer, including ALL, AML, CLL, mantle cell lymphoma, multiple myeloma, melanoma, NSCLC, breast and pancreatic cancer, are undergoing.
作用机制	Dinaciclib can interact with both ATP-binding site and the acetyl-lysine recognition site of bromodomains of CDKs^[3].

Cell Line MCF7-Re cells THP-1 cells BCSphCs CLB-GA cells Kelly cells HB PDX cells HCC PDXOs THLE-2	Concentration	Treated Time	Description	References
MCF7-Re cells	0.5 μM	48 h	Dinaciclib significantly reduced BRCA1 phosphorylation and expression, induced more DNA damage and apoptosis, and significantly increased the sensitivity to cisplatin in MCF7-Re cells.	Nat Commun. 2018 Apr 23;9(1):1595.
THP-1 cells	10 nM	21 days	Screening for CDK9 inhibitor-resistant cells	Cell. 2021 Jun 10;184(12):3143-3162.e32.
BCSphCs	10 nM	6 days	To evaluate the effect of Dinaciclib on the cell viability of BCSphCs, results showed that Dinaciclib significantly reduced the cell viability of BCSphCs	Oncogene. 2022 Apr;41(15):2196-2209.
CLB-GA cells	10 nM	8 h	To investigate the effect of Dinaciclib on TERT mRNA expression and chromatin occupancy of epigenetic modulators at the TERT gene locus, results showed that Dinaciclib significantly inhibited TERT expression and reduced the binding of Brd4 and H3K27Ac at the TERT promoter or gene body.	Cancer Res. 2020 Mar 1;80(5):1024-1035.
Kelly cells	10 nM	8 h	To investigate the effect of Dinaciclib on TERT mRNA expression, results showed that Dinaciclib significantly inhibited TERT expression.	Cancer Res. 2020 Mar 1;80(5):1024-1035.
HB PDX cells	0.1 µM	24 h	Dinaciclib significantly inhibited the proliferation of PDX282 and PDX303 cells and induced apoptosis, while having less effect on PDX214 cells with low CDK9 expression.	Hepatology. 2024 Jul 1;80(1):55-68.
HCC PDXOs	0.01 μM	48 h	To evaluate the cytotoxic effects of Dinaciclib on HCC PDXOs, results showed that Dinaciclib significantly reduced cell viability.	J Exp Clin Cancer Res. 2022 Aug 15;41(1):249.
THLE-2	0.01 μM	48 h	To evaluate the toxicity of Dinaciclib on non-tumorigenic liver epithelial cells THLE-2, results showed that Dinaciclib had lower toxicity on THLE-2 cells.	J Exp Clin Cancer Res. 2022 Aug 15;41(1):249.

Species Mice Nude mice Mice Nude mice Mice	Animal Model BCSphCs xenograft model CLB-GA xenograft model KrasG12DSetd2–/– lung tumor model HB PDX model HCC PDX model	Administration	Dosage	Frequency	Description	References
Mice	BCSphCs xenograft model	Intraperitoneal injection	25 mg/kg	3 times per week for 3 weeks	To evaluate the effect of Dinaciclib on tumor growth in the BCSphCs xenograft model, results showed that Dinaciclib significantly reduced tumor volume	Oncogene. 2022 Apr;41(15):2196-2209.
Nude mice	CLB-GA xenograft model	Intraperitoneal injection	40 mg/kg	Daily, continuous treatment	To investigate the effect of Dinaciclib on the growth of CLB-GA xenograft tumors, results showed that Dinaciclib significantly inhibited tumor growth, and the effect was enhanced when combined with AZD5153.	Cancer Res. 2020 Mar 1;80(5):1024-1035.
Mice	KrasG12DSetd2–/– lung tumor model	Intraperitoneal injection	20 mg/kg	3 times weekly for 7 weeks	Dinaciclib markedly suppressed the growth of KrasG12DSetd2–/– lung tumors and significantly prolonged the survival of mice	JCI Insight. 2023 Feb 22;8(4):e154120
Nude mice	HB PDX model	Intraperitoneal injection	20 mg/kg	3 times per week for 11 days	Dinaciclib significantly reduced the volume of PDX282 tumors but also caused some side effects such as weight loss and unexpected death.	Hepatology. 2024 Jul 1;80(1):55-68.
Mice	HCC PDX model	Intraperitoneal injection	5 mg/kg	Three times a week until tumors reached endpoint volume	To evaluate the tumor suppressive effects of Dinaciclib in combination with Ixazomib on HCC PDX tumors, results showed that the combination treatment significantly inhibited tumor growth and outperformed Sorafenib alone.	J Exp Clin Cancer Res. 2022 Aug 15;41(1):249.

CAS号	779353-01-4
分子式	C₂₁H₂₈N₆O₂
分子量	396.49
SMILES Code	OCC[C@H]1N(CCCC1)C2=NC3=C(C=NN3C(NCC4=C[N+]([O-])=CC=C4)=C2)CC
MDL No.	MFCD16037702

别名	SCH 727965; PS-095760
运输	蓝冰

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CDK5	CDK5, IC50:1 nM
CDK2	CDK2, IC50:1 nM
CDK9	CDK9, IC50:4 nM
CDK1	CDK1, IC50:3 nM

1205Lu	10/30 nM	Growth Inhibition Assay	72 h	inhibits cell growth and survival	23527225
8226	2/5/10 nM	Function Assay	4 h	blocks induction of XBP-1s and downstream targets	24362465
BaF3/Bcr-abl	1.5/3/8 nM	Function Assay	6 h	blocks induction of XBP-1s and downstream targets	24362465
BT-12		Growth Inhibition Assay		IC50=8.5 nM	22315240
CA46	100 nM	Apoptosis Assay	24 h	induces cell cycle arrest	25289887
CCRF-CEM		Growth Inhibition Assay		IC50=5.6 nM	22315240
CHLA-10		Growth Inhibition Assay		IC50=6.3 nM	22315240
CHLA-136		Growth Inhibition Assay		IC50=9.8 nM	22315240
CHLA-258		Growth Inhibition Assay		IC50=9.9 nM	22315240
CHLA-266		Growth Inhibition Assay		IC50=7.3 nM	22315240
CHLA-9		Growth Inhibition Assay		IC50=8 nM	22315240
CHLA-90		Growth Inhibition Assay		IC50=7.5 nM	22315240
COG-LL-317		Growth Inhibition Assay		IC50=6.5 nM	22315240
GBM2		Growth Inhibition Assay		IC50=6.5 nM	22315240
H929	2/5/10 nM	Function Assay	4 h	blocks induction of XBP-1s and downstream targets	24362465
K562	1.5/3/8 nM	Function Assay	6 h	blocks induction of XBP-1s and downstream targets	24362465
Karpas-299		Growth Inhibition Assay		IC50=3.9 nM	22315240
Kasumi-1	100 nM	Apoptosis Assay	24 h	induces cell cycle arrest	25289887
Kasumi-1		Growth Inhibition Assay		IC50=4.5 nM	22315240
MIAPaCa-2		Growth Inhibition Assay	72 h	GI50=10 nM	21768779
ML-1	1-1000 nM	Apoptosis Assay	4 h	induces apoptosis slightly	21768777
MOLT-4		Growth Inhibition Assay		IC50=9.3 nM	22315240
NALM-6		Growth Inhibition Assay		IC50=4.6 nM	22315240
NB-1643		Growth Inhibition Assay		IC50=3.3 nM	22315240
NB-EBc1		Growth Inhibition Assay		IC50=7 nM	22315240
Pa20C		Growth Inhibition Assay	72 h	GI50=20 nM	21768779
Ramos-RA1		Growth Inhibition Assay		IC50=7.9 nM	22315240
RD		Growth Inhibition Assay		IC50=8.2 nM	22315240
Rh18		Growth Inhibition Assay		IC50=10.5 nM	22315240
Rh30		Growth Inhibition Assay		IC50=9 nM	22315240
Rh41		Growth Inhibition Assay		IC50=10.5 nM	22315240
RS4;11		Growth Inhibition Assay		IC50=5.1 nM	22315240
TC-71		Growth Inhibition Assay		IC50=3.9 nM	22315240
U937	2/5/10 nM	Function Assay	3 h	blocks induction of XBP-1s and downstream targets	24362465
U937	2/10 nM	Function Assay	3 h	blocks induction of XBP-1s and downstream targets	24362465
WM1366	10/30 nM	Growth Inhibition Assay	72 h	inhibits cell growth and survival	23527225

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