PI-103 | PI3K/mTOR Inhibitor | AmBeed-信号通路专用抑制剂

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]}	现货	1周咨询	- +

产品名称	C2β ↓ ↑	p110α ↓ ↑	p110β ↓ ↑	p110γ ↓ ↑	p110δ ↓ ↑	PI3K ↓ ↑	Vps34 ↓ ↑	其他靶点	纯度
A66	+ C2β, IC50: 462 nM	++ p110α, IC50: 32 nM							99%+
Taselisib	+ C2β, IC50: 292 nM	++++ PI3Kα, Ki: 0.29 nM	+++ PI3Kβ, Ki: 9.1 nM	++++ PI3Kγ, Ki: 0.97 nM	++++ PI3Kδ, Ki: 0.12 nM		+ hVps34, IC50: 374 nM		99%+
Gedatolisib		++++ PI3Kα, IC50: 0.4 nM		+++ PI3Kγ, IC50: 5.4 nM				mTOR	99%
HS-173		++++ PI3Kα , IC50: 0.8 nM							99%+
Serabelisib		+++ PI3Kα, IC50: 21 nM							99%+
GNE-477		++++ PI3Kα, IC50: 4 nM						mTOR	99%
YM-201636		+ p110α, IC50: 3.3 μM						PIKfyve	98%
AS-252424		+ PI3Kα, IC50: 935 nM		++ PI3Kγ, IC50: 33 nM					99%
Alpelisib		+++ PI3Kα, IC50: 5 nM							99%+
AS-604850		+ PI3Kα, IC50: 4.5 μM		+ PI3Kγ, IC50: 0.25 μM					99%
SF2523		++ PI3Kα, IC50: 34 nM		++ PI3Kγ, IC50: 158 nM				DNA-PK,mTOR	99%+
Inavolisib		++++ PI3K alpha, IC50: 0.038 nM							99%+
Bimiralisib		++++ PI3Kα, Kd: 1.5 nM	+++ PI3Kβ, Kd: 11 nM	++ PI3Kγ, Kd: 25 nM	++ PI3Kδ, Kd: 25 nM			mTOR	99%+
GSK1059615		++++ PI3Kα, IC50: 0.4 nM	++++ PI3Kβ, IC50: 0.6 nM	+++ PI3Kγ, IC50: 5 nM	++++ PI3Kδ, IC50: 2 nM			mTOR	98%
GSK2636771			✔						99%
Fimepinostat		+++ PI3Kα, IC50: 19 nM	++ PI3Kβ, IC50: 54 nM		++ PI3Kδ, IC50: 39 nM				99%+
VS-5584		++++ PI3Kα, IC50: 2.6 nM	+++ PI3Kβ, IC50: 21 nM	++++ PI3Kγ, IC50: 3.0 nM	++++ PI3Kδ, IC50: 2.7 nM			mTOR	98%
Dactolisib		++++ p110α1, IC50: 4 nM	++ p110β, IC50: 75 nM	+++ p110γ, IC50: 5 nM	+++ p110δ, IC50: 7 nM				98+%
PI-103		++++ p110α, IC50: 2 nM	++++ p110β, IC50: 3 nM	+++ p110γ, IC50: 15 nM	++++ p110δ, IC50: 3 nM			DNA-PK,mTOR	99%+
PI-3065			+ p110β, IC50: 1078 nM		+++ p110δ, IC50: 15 nM				99%+
Voxtalisib		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	99%+
AZD-8835		+++ PI3Kα, IC50: 6.2 nM	+ PI3Kβ, IC50: 431 nM	++ PI3Kγ, IC50: 90 nM	+++ PI3Kδ, IC50: 5.7 nM				99%
Pilaralisib analogue		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 36 nM	+++ PI3Kγ, IC50: 23 nM	++ PI3Kδ, IC50: 36 nM				99%+
ZSTK474		+++ PI3Kα, IC50: 16 nM	++ PI3Kβ, IC50: 44 nM	++ PI3Kγ, IC50: 49 nM	+++ PI3Kδ, IC50: 4.6 nM	++ PI3K, IC50: 37 nM			98%
AS-605240		++ PI3Kα, IC50: 60 nM	+ PI3Kβ, IC50: 270 nM	+++ PI3Kγ, IC50: 8 nM	+ PI3Kδ, IC50: 300 nM				98%
TGX-221			+++ p110β, IC50: 5 nM		++ p110δ, IC50: 0.1 μM				99%+
PF-04691502		++++ PI3Kα, Ki: 1.8 nM	++++ PI3Kβ, Ki: 2.1 nM	++++ PI3Kγ, Ki: 1.9 nM	++++ PI3Kδ, Ki: 1.6 nM			mTOR	98+%
GDC-0084		++++ PI3Kα, Ki app: 2 nM	++ PI3Kβ, Ki app: 46 nM	+++ PI3Kγ, Ki app: 10 nM	++++ PI3Kδ, Ki app: 3 nM			mTOR	99%+
Buparlisib		++ p110α, IC50: 52 nM	+ p110β, IC50: 166 nM	+ p110γ, IC50: 262 nM	++ p110δ, IC50: 116 nM		+ Vps34, IC50: 2.4 μM	mTOR	98%
LY294002		+ p110α, IC50: 0.5 μM	+ p110β, IC50: 0.97 μM		+ p110δ, IC50: 0.57 μM			DNA-PK	99%+
AZD 6482		+ PI3Kα, IC50: 870 nM	+++ PI3Kβ, IC50: 10 nM		++ PI3Kδ, IC50: 80 nM			DNA-PK	99%+
Pictilisib		++++ p110α, IC50: 3 nM	++ p110β, IC50: 33 nM	++ p110γ, IC50: 75 nM	++++ p110δ, IC50: 3 nM			mTOR	99%+
PKI-402		++++ PI3Kα, IC50: 2 nM	+++ PI3Kβ, IC50: 7 nM	+++ PI3Kγ, IC50: 16 nM	+++ PI3Kδ, IC50: 14 nM			mTOR	98%
Copanlisib		++++ PI3Kα, IC50: 0.5 nM	++++ PI3Kβ, IC50: 3.7 nM	+++ PI3Kγ, IC50: 6.4 nM	++++ PI3Kδ, IC50: 0.7 nM				99%+
Omipalisib		++++ p110α, Ki: 0.019 nM	++++ p110β, Ki: 0.13 nM	++++ p110γ, Ki: 0.06 nM	++++ p110δ, Ki: 0.024 nM				99%+
Izorlisib		+++ PI3Kα, IC50: 14 nM	++ PI3Kβ, IC50: 0.12 μM	++ PI3Kγ, IC50: 36 nM	+ PI3Kδ, IC50: 0.50 μM				99%+
AZD8186		++ PI3Kα, IC50: 35 nM	++++ PI3Kβ, IC50: 4 nM		+++ PI3Kδ, IC50: 12 nM				99%
KU-0060648		++++ PI3Kα, IC50: 4 nM	++++ PI3Kβ, IC50: 0.5 nM	+ PI3Kγ, IC50: 0.59 μM	++++ PI3Kδ, IC50: 0.1 nM			DNA-PK	98%
Apitolisib		+++ p110α, IC50: 5 nM	++ p110β, IC50: 27 nM	+++ p110γ, IC50: 14 nM	+++ p110δ, IC50: 7 nM			mTOR	98%+
CZC24832			+ PI3Kβ, IC50: 1.1 μM	++ PI3Kγ, IC50: 27 nM					98+%
BGT226 maleate		++++ PI3Kα, IC50: 4 nM	++ PI3Kβ, IC50: 63 nM	++ PI3Kγ, IC50: 38 nM				mTOR	99%+
TG 100713		++ PI3Kα, IC50: 165 nM	+ PI3Kβ, IC50: 215 nM	++ PI3Kγ, IC50: 50 nM	+++ PI3Kδ, IC50: 24 nM				98%+
PI3K-IN-1		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	98+%
TG100-115		+ PI3Kα, IC50: 1.3 μM	+ PI3Kβ, IC50: 1.2 μM	++ PI3Kγ, IC50: 83 nM	+ PI3Kδ, IC50: 235 nM				98%
PIK-90		+++ PI3Kα, IC50: 11 nM	+ PI3Kβ, IC50: 350 nM	+++ PI3Kγ, IC50: 18 nM	++ PI3Kδ, IC50: 58 nM				99%+
PIK-294			+ p110β, IC50: 490 nM	++ p110γ, IC50: 160 nM	+++ p110δ, IC50: 10 nM				99%+
Duvelisib			++++ PI3Kβ, Ki: 1564 pM	++ PI3Kγ, Ki: 243 pM	++++ PI3Kδ, Ki: 23 pM				99%+
GDC-0326		++++ PI3Kα, Ki: 0.2 nM	++ PI3Kβ, Ki: 26.6 nM	+++ PI3Kγ, Ki: 10.2 nM	++++ PI3Kδ, Ki: 4 nM				98%
Quercetin Dihydrate			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM				95%
Quercetin			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM			Sirtuin,PKC,Src	95%
Leniolisib		+ PI3Kα, IC50: 0.244 μM	+ PI3Kβ, IC50: 0.424 μM	+ PI3Kγ, IC50: 2.23 μM	+++ PI3Kδ, IC50: 0.011 μM			DNA-PK	99%+
PIK-108			✔						99%
Eganelisib				+++ PI3Kγ, IC50: 16 nM					99%+
CAY10505				✔					99%
IPI-3063					++++ p110δ, IC50: 2.5 nM				99%
Nemiralisib					++++ PI3Kδ, pKi: 9.9				99%+
PF-4989216		++++ p110α, IC50: 2 nM		++ p110γ, IC50: 65 nM	++++ p110δ, IC50: 1 nM				99%+
PIK-75 HCl		+++ p110α, IC50: 5.8 nM		++ p110γ, IC50: 76 nM	+ p110δ, IC50: 0.51 μM			DNA-PK	99%+
Tenalisib				++ PI3Kγ, IC50: 33.2 nM	++ PI3Kδ, IC50: 24.5 nM				98%
Acalisib					+++ p110δ, IC50: 14 nM				99%+
Umbralisib					+++ PI3Kδ, IC50: 22.2 nM				99%+
AMG319				+ PI3Kγ, IC50: 850 nM	+++ PI3Kδ, IC50: 18 nM				99%
IC-87114				+ PI3Kγ, IC50: 29 μM	+ PI3Kδ, IC50: 0.5 μM				99%+
Idelalisib				++ p110γ, IC50: 89 nM	++++ p110δ, IC50: 2.5 nM				98%
PIK-293				+ p110γ, IC50: 10 μM	+ p110δ, IC50: 0.24 μM				99%+
Vps34-PIK-III					+ PI3Kδ, IC50: 1.2μM		+++ Vps34, IC50: 0.018μM		99%+
GSK2292767					✔				98%
Seletalisib				+ PI3Kγ, IC50: 282 nM	+++ PI3Kδ, IC50: 12 nM				99%+
P110δ-IN-1					++++ P110δ, IC50: 0.6 nM				99%
PI3Kδ-IN-5					++++ PI3Kδ, IC50: 0.9 nM				99%
SRX3207		+ PI3K alpha, IC50: 244 nM		+ PI3K gamma, IC50: 9790 nM	+ PI3K delta, IC50: 388 nM			Syk	98%
Parsaclisib HCl					++++ PI3Kδ, IC50: 1 nM				98%
IHMT-PI3Kδ-372					+++ PI3Kδ, IC50: 14 nM				98%
Trigonelline						✔		Akt	99%+
Wortmannin						++++ PI3K, IC50: 3 nM		DNA-PK,MLCK	99%+
Samotolisib						✔		DNA-PK	99%+
GNE-317						✔			99%+
Oroxin B						✔		Akt,PTEN	99%+
NU 7026						+ PI3K, IC50: 13 μM		DNA-PK	98+%
Deguelin						✔		Akt	99%+
Ailanthone						✔		CDK,Akt,ATM/ATR	98%
Resibufogenin						✔		ROS	98%
KU-57788						+ PI3K, IC50: 5 μM		DNA-PK,mTOR	99%+
Cinobufagine						✔		Akt	99%
α-Linolenic acid						✔			97% (GC)
MTX-211						✔		EGFR	98%
PI3K/mTOR Inhibitor-2						++++ PI3K, IC50: 3.4 nM		mTOR	99%+
SPP-86						✔			99%+
(E)-Akt inhibitor-IV						✔			98%
Vps34-IN-1							++ Vps34, IC50: 25 nM		98%
SAR405							++++ Vps34, IC50: 1.2 nM		98+%
3-Methyladenine				+ PI3Kγ, IC50: 60 μM			+ Vps34, IC50: 25 μM	Autophagy	98%
Vps34-IN-4							+++ VPS34, IC50: 15 nM		98%+
Autophinib							+++ Vps34, IC50: 19 nM	Autophagy	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。

产品名称	Autophagy ↓ ↑	其他靶点	纯度
SBI-0206965	+++ ULK1, IC50: 108 nM ULK2, IC50: 711 nM		95%
Hydroxychloroquine sulfate	✔		99%
Valproic acid sodium	✔	HDAC	97%
PFK-015	++ PFKFB3, IC50: 207 nM		99%+
MRT68921 HCl	++++ ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM		99%+
ROC-325	✔		99%+
Autophinib	+++ Autophagy, IC50: 40 nM		99%
Lys05	✔		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。

产品名称	ATM ↓ ↑	ATR ↓ ↑	其他靶点	纯度
Wortmannin	++ ATM, IC50: 150 nM		DNA-PK,PI3K,MLCK	99%+
CP-466722	+ ATM, IC50: 410 nM			99%+
Torin 2	++ ATM, EC50: 28 nM	++ ATR, EC50: 35 nM	DNA-PK,mTOR	99%+
KU-55933	+++ ATM, IC50: 12.9 nM			96%
ETP-46464	+ ATM, IC50: 545 nM	+++ ATR, IC50: 14 nM	DNA-PK,mTOR	98%
CGK733	++ ATM, IC50: 200 nM	++ ATR, IC50: 200 nM		99%+
AZD0156	✔			99%+
Dactolisib		+++ ATR, IC50: 21 nM		98+%
Ceralasertib		++++ ATR, IC50: 1 nM		99%+
Berzosertib		+++ ATR, IC50: 19 nM		99%+
VE-821		+++ ATR, Ki: 13 nM		99%+
AZ20		++++ ATR, IC50: 5 nM	mTOR	99%+
Schizandrin B		+ ATR, IC50: 7.25 μM	P-gp	98%
m-PEG25-NHS ester		++++ ATR, IC50: 7 nM		95%
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。

产品名称	DNA-PK ↓ ↑	其他靶点	纯度
PI-103	++ DNA-PK, IC50: 23 nM		99%+
CC-115	+++ DNA-PK, IC50: 0.013 μM	mTOR	98+%
Samotolisib	✔		99%+
NU 7026	+ DNA-PK, IC50: 0.23 μM	PI3K	98+%
PIK-75 HCl	++++ DNA-PK, IC50: 2 nM		99%+
PP121	+ DNA-PK, IC50: 60 nM	VEGFR,PDGFR	99%+
KU-0060648	++++ DNA-PK, IC50: 5 nM		98%
KU-57788	+++ DNA-PK, IC50: 14 nM		99%+
LTURM34	++ DNA-PK, IC50: 0.034 μM		98%+
SF2523	+++ DNA-PK, IC50: 9 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。

Cell Line LNCaP cells PC3 cells 4T1 breast cancer cells MDA-MB-468 breast cancer cells 4306 ovarian cancer cells HCT116 BAX-ko cells HT29 cells 16HBE cells MDA-MB-231 MDA-MB-361 MDA-MB-453 HT29 cells HCT116 BAX-ko cells	Concentration	Treated Time	Description	References
LNCaP cells	3 μM		PI-103 significantly reduced CXCL13-mediated migration and invasion of LNCaP cells, indicating that LNCaP cell migration and invasion are dependent on PI3Kp110α.	Mol Cancer. 2010 Apr 22;9:85.
PC3 cells	3 μM		PI-103 significantly reduced CXCL13-mediated migration and invasion of PC3 cells, indicating that PC3 cell migration and invasion are dependent on PI3Kp110α.	Mol Cancer. 2010 Apr 22;9:85.
4T1 breast cancer cells	5 μM	48 h	Evaluate the effect of PI103 and PI103-SNP on the viability of 4T1 cells, results show that PI103-SNP sustained inhibition of Akt phosphorylation	Cancer Res. 2013 Dec 1;73(23):6987-97.
MDA-MB-468 breast cancer cells	5 μM	48 h	Evaluate the effect of PI103 and PI103-SNP on the viability of MDA-MB-468 cells, results show that PI103-SNP sustained inhibition of Akt phosphorylation	Cancer Res. 2013 Dec 1;73(23):6987-97.
4306 ovarian cancer cells	5 μM	48 h	Evaluate the effect of PI103 and PI103-SNP on the viability of 4306 cells, results show that PI103-SNP sustained inhibition of Akt phosphorylation	Cancer Res. 2013 Dec 1;73(23):6987-97.
HCT116 BAX-ko cells	20 μM	24 h	Induced autophagy, increased de novo ChoPL synthesis	Autophagy. 2020 Jun;16(6):1044-1060.
HT29 cells	100 μM	24 h	Induced autophagy, increased de novo ChoPL synthesis	Autophagy. 2020 Jun;16(6):1044-1060.
16HBE cells	10 ng/ml	24 h	To investigate the effect of PI-103 on IL-13-induced ER stress and mucus overproduction, results showed that PI-103 significantly reduced the fluorescence intensities of BIP and CHOP and decreased MUC5AC expression.	EBioMedicine. 2017 Feb;15:137-149.
MDA-MB-231	50 µM	72 h	To assess the toxicity effect of RIDR-PI-103 on breast cancer cells, results showed that MDA-MB-231 cells were sensitive to RIDR-PI-103.	Int J Mol Sci. 2021 Feb 19;22(4):2088.
MDA-MB-361	50 µM	72 h	To assess the toxicity effect of RIDR-PI-103 on breast cancer cells, results showed that MDA-MB-361 cells were sensitive to RIDR-PI-103.	Int J Mol Sci. 2021 Feb 19;22(4):2088.
MDA-MB-453	50 µM	72 h	To assess the toxicity effect of RIDR-PI-103 on breast cancer cells, results showed that MDA-MB-453 cells were sensitive to RIDR-PI-103.	Int J Mol Sci. 2021 Feb 19;22(4):2088.
HT29 cells	100 μM	24 h	To study changes in choline phospholipid metabolism during autophagy, results showed increased expression of autophagy marker LC3B-II	Autophagy. 2020 Jun;16(6):1044-1060.
HCT116 BAX-ko cells	20 μM	24 h	To study changes in choline phospholipid metabolism during autophagy, results showed increased expression of autophagy marker LC3B-II	Autophagy. 2020 Jun;16(6):1044-1060.

Species NSG mice Mice C57BL/6J mice	Animal Model PDX model 4T1 breast cancer model C57BL/6J mice	Administration	Dosage	Frequency	Description	References
NSG mice	PDX model	Intraperitoneal injection	10 mg/kg	Daily for 3 weeks	To investigate the inhibitory effect of PI-103 on tumor growth in the PDX model, it was found that PI-103 significantly reduced the tumor burden.	Hepatol Commun. 2020 Jul 27;4(9):1362-1381
Mice	4T1 breast cancer model	Tail vein injection	5 mg/kg	Every 48 hours for 3 doses	Evaluate the antitumor efficacy of PI103-SNP in the 4T1 breast cancer model, results show that PI103-SNP significantly inhibited tumor growth and prolonged survival	Cancer Res. 2013 Dec 1;73(23):6987-97.
C57BL/6J mice	C57BL/6J mice	Intraperitoneal injection	20 mg/kg	Single dose, duration of 96 hours	To evaluate the pharmacokinetic profile of RIDR-PI-103 in mice, results showed that the maximum plasma concentration of RIDR-PI-103 was 201.5 ng/mL with a half-life of 9.4 hours.	Int J Mol Sci. 2021 Feb 19;22(4):2088.

细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源

518A2	0.01–10 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	21048785
518A2	0.001–1 μM	Function Assay	24 h	suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets	21048785
A549	0.25/0.5/1 μM	Function Assay	24 h	inhibits Akt phosphorylation slightly	24351425
A549	0-3.3 μM	Function Assay	72 h	induces complete downregulation of pAKT	23259591
AGS HG		Growth Inhibition Assay		IC50=0.68 ± 0.031 μM	24597478
AGS LG		Growth Inhibition Assay		IC50=0.05 ± 0.001 μM	24597478
ALL-SIL	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
BT549	0-3 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25721419
CCRF-CEM	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
DETROIT562		Growth Inhibition Assay		IC50=0.13 μM	19584227
DND41	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
FaDu	0.25/0.5/1 μM	Function Assay	24 h	inhibits Akt phosphorylation significantly	24351425
G 35 DC	0.05-20 μM	Growth Inhibition Assay	24/72 h	inhibits cell viability dose and time dependently	26121251
G 35 SC	0.05-20 μM	Growth Inhibition Assay	24/72 h	inhibits cell viability dose and time dependently	26121251
G 38 DC	0.05-20 μM	Growth Inhibition Assay	24/72 h	inhibits cell viability dose and time dependently	26121251
G 38 SC	0.05-20 μM	Growth Inhibition Assay	24/72 h	inhibits cell viability dose and time dependently	26121251
G 40 DC	0.05-20 μM	Growth Inhibition Assay	24/72 h	inhibits cell viability dose and time dependently	26121251
G 40 SC	0.05-20 μM	Growth Inhibition Assay	24/72 h	inhibits cell viability dose and time dependently	26121251
H3122	0-3.3 μM	Function Assay	72 h	induces complete downregulation of pAKT	23259591
H460	0.25/0.5/1 μM	Function Assay	24 h	inhibits Akt phosphorylation slightly	24351425
H661	0.25/0.5/1 μM	Function Assay	24 h	inhibits Akt phosphorylation significantly	24351425
HCC1937	1 μM	Function Assay	24 h	reduces the phosphorylation of AKT	22488590
HCC827	0-3.3 μM	Function Assay	72 h	induces complete downregulation of pAKT	23259591
HCC827	0-3 μM	Growth Inhibition Assay	72 h	IC50=0.3 μM	21220474
HGC27 HG		Growth Inhibition Assay		IC50=0.38 ± 0.022 μM	24597478
HGC27 LG		Growth Inhibition Assay		IC50=0.02 ± 0.004 μM	24597478
HPB-ALL	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
HS578T	0-3 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25721419
HS578T	0.01-10 μM	Function Assay	24 h	downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins	25721419
HT1080	3 µM	Apoptosis Assay	12 h	sensitizes RD cells to DOX-induced apoptosis	23300809
HUVEC		Growth Inhibition Assay		IC50=0.08 μM	19584227
IGROV-1		Growth Inhibition Assay		IC50=0.06 μM	19584227
Jurkat	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
Karpas-45	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
KE37	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
KMS12-BM	0-2 μM	Growth Inhibition Assay	24 h	IC50＞2 μM	22829234
LN229	1 μM	Function Assay	48 h	induces autophagosome formation	21062993
LOUCY	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
MDA-MB-231	0-3 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25721419
MDA-MB-231	0.01-10 μM	Function Assay	24 h	downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins	25721419
MDA-MB-231	0.3 μM	Cell Viability Assay	72 h	enhances cytotoxic effects of PI3K/AKT pathway inhibitors	23601074
MDA-MB-436	0-3 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25721419
MDA-MB-436	1 μM	Function Assay	24 h	reduces the phosphorylation of AKT	22488590
MDA-MB-468	0-3 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25721419
MDA-MB-468	0.01-10 μM	Function Assay	24 h	downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins	25721419
MDA-MB-468	0.3 μM	Cell Viability Assay	72 h	enhances cytotoxic effects of PI3K/AKT pathway inhibitors	23601074
Mel-Juso	0.01–10 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	21048785
Mel-Juso	0.001–1 μM	Function Assay	24 h	suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets	21048785
MKN45 HG		Growth Inhibition Assay		IC50=1.01 ± 0.051 μM	24597478
MKN45 LG		Growth Inhibition Assay		IC50=0.87 ± 0.030 μM	24597478
MM1S	0-2 μM	Growth Inhibition Assay	24 h	IC50=0.5 μM	22829234
MOLT-16	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
MOLT-4	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
NCI-H929	0-2 μM	Growth Inhibition Assay	24 h	IC50=0.25 μM	22829234
NUGC4 HG		Growth Inhibition Assay		IC50=14.0 ± 3.913 μM	24597478
NUGC4 LG		Growth Inhibition Assay		IC50=14.0 ± 5.321 μM	24597478
PC3		Growth Inhibition Assay	24h	GI50 = 100 nM	20551061
PC3		Growth Inhibition Assay		IC50=0.10 μM	19584227
PC-9	0-3 μM	Growth Inhibition Assay	72 h	IC50=0.8 μM	21220474
PEER	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
PF-382	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
RD	1/1.5/2 μM	Apoptosis Assay	72 h	induces apoptosis combined with GANT61	25749378
RD	1/1.5/2 μM	Apoptosis Assay	72 h	induces caspase-dependent apoptosis combined with UO126	23684925
RD	3 µM	Apoptosis Assay	12 h	sensitizes RD cells to DOX-induced apoptosis	23300809
RH30	1/1.5/2 μM	Apoptosis Assay	72 h	induces apoptosis combined with GANT61	25749378
RH30	1/1.5/2 μM	Apoptosis Assay	72 h	induces caspase-dependent apoptosis combined with UO126	23684925
RMS13	1/1.5/2 μM	Apoptosis Assay	72 h	induces apoptosis combined with GANT61	25749378
RMS13	1/1.5/2 μM	Apoptosis Assay	72 h	induces caspase-dependent apoptosis combined with UO126	23684925
RPMI-8402	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
SAS	0.25/0.5/1 μM	Function Assay	24 h	inhibits Akt phosphorylation significantly	24351425
SF767	1 μM	Function Assay	48 h	induces autophagosome formation	21062993
SH-SY5Y	0-8 μM	Growth Inhibition Assay	24/48/72 h	induces time- and concentration-dependent inhibition on NB cell growth	26224681
SH-SY5Y	1 μM	Apoptosis Assay	0.5-24 h	sensitizes neuroblastoma cells to doxorubicin-induced apoptosis	26224681
SK-N-BE	0-8 μM	Growth Inhibition Assay	24/48/72 h	induces time- and concentration-dependent inhibition on NB cell growth	26224681
SKNBE(2c)	1.5/2.5/5 μM	Function Assay	24 h	induces G1 cell-cycle arrest and apoptosis	23378341
SKOV-3		Growth Inhibition Assay		IC50=0.12 μM	19584227
SUM1315MO2	1 μM	Function Assay	24 h	reduces the phosphorylation of AKT	22488590
SUM149PT	0-3 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25721419
SUM149PT	0.3 μM	Cell Viability Assay	72 h	enhances cytotoxic effects of PI3K/AKT pathway inhibitors	23601074
SUM149PT	1 μM	Function Assay	24 h	reduces the phosphorylation of AKT	22488590
SUP-T1	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
SW872	0.01-0.5 μM	Function Assay	24 h	reduces AKT phosphorylation (pAKT) and 4EBP1 phosphorylation (p4EBP1) in a dose-dependent manner	24695632
SW872	0.01-0.5 μM	Apoptosis Assay	48 h	induces apoptosis dose dependently	24695632
SW982	0.01-0.5 μM	Function Assay	24 h	reduces AKT phosphorylation (pAKT) and 4EBP1 phosphorylation (p4EBP1) in a dose-dependent manner	24695632
SW982	0.01-0.5 μM	Apoptosis Assay	48 h	induces apoptosis dose dependently	24695632
SY5Y	1.5/2.5/5 μM	Function Assay	24 h	induces G1 cell-cycle arrest and apoptosis	23378341
TALL-1	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
TE381.T	1/1.5/2 μM	Apoptosis Assay	72 h	induces apoptosis combined with GANT61	25749378
TE671	1/1.5/2 μM	Apoptosis Assay	72 h	induces caspase-dependent apoptosis combined with UO126	23684925
TP5014	3 µM	Apoptosis Assay	12 h	sensitizes RD cells to DOX-induced apoptosis	23300809
U118MG	0.1-1 μM	Function Assay	24 h	inhibits PI3K-mediated signaling	19633683
U138MG	0.1-1 μM	Function Assay	24 h	inhibits PI3K-mediated signaling	19633683
U373	1 μM	Function Assay	48 h	induces autophagosome formation	21062993
U87	1 μM	Function Assay	48 h	induces autophagosome formation	21062993
U87MG	0.1-1 μM	Function Assay	24 h	inhibits PI3K-mediated signaling	19633683
U87MG		Growth Inhibition Assay		IC50=0.14 μM	19584227
UCH-1	0-5 μM	Function Assay		inhibits the phosphorylation of both AKT and mTOR in a dose-dependent manner	19528441
UCH-1	0.01-10 μM	Growth Inhibition Assay	6 d	inhibits proliferation dose dependently	19528441
UCH-1	0.1-10 μM	Apoptosis Assay	24 h	induces apoptosis	19528441
UT5	0.25/0.5/1 μM	Function Assay	24 h	inhibits Akt phosphorylation significantly	24351425
VJ	1/1.5/2 μM	Apoptosis Assay	72 h	induces apoptosis combined with GANT61	25749378

靶点	p110γ p110γ, IC50:15 nM p110β p110β, IC50:3 nM p110α p110α, IC50:2 nM p110δ p110δ, IC50:3 nM
描述	PI3K/AKT/mTOR pathway directly relates to cellular quiescence, proliferation, cancer, and longevity. There are eight PI3 kinases have been identified as classes IA, 1B, II, and III based on the sequence homology and substrate preference. Among them, class IA PI3K is composed of a heterodimer consisting of a 110 kDa catalytic subunit (p110α, p110β and p110δ) and an 85 kDa regulatory subunit ^[2]. PI-103 is a dual inhibitor of Class IA PI3Ks (p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM determined using a scintillation proximity assay, respectively) and mTOR (IC50=30 nM), with less potent to DNA-PK (IC50=23 nM) ^[1]. PI-103 is usually used in ACUTE LYMPHOBLASTIC LEUKEMIA study. It can inhibit PI3K/Akt and mTORC1 activity in MOLM14, OCI-AML3 and MV4-11 leukemic cell lines, which have constitutive activation of PI3K/Akt (p-Akt Ser 473 and p-FOXO3a Thr32), mTORC1 (p-P70S6K Thr389) signaling pathways, with no inhibition on ERK/MAPK (p-p42/44 ERK/MAPK Thr202/Tyr204). In AML blast cells, PI-103 inhibits both constitutive and growth factor-induced PI3K/Akt and mTORC1 activation, reverses the positive feedback of mTORC1 inhibition on PI3K/Akt and induces significant apoptosis ^[3]. In glioma, PI‑103 induces autophagy and promotes cell survival by inhibiting mTOR activity. Conversely, PI‑103 can lead to apoptosis by combining with autophagy inhibitors like 3-ma or bafilomycin A1 ^[4].
作用机制	PI-103 acts as an ATP-competitive inhibitor of PI3K (Class IA). ^[5]

Dose	Mice: min = 5 mg/kg^[5] Nude Mice: min = 30 mg/kg, max = 100 mg/kg^[6]
Administration	i.p.

CAS号	371935-74-9
分子式	C₁₉H₁₆N₄O₃
分子量	348.36
SMILES Code	OC1=CC=CC(C2=NC(N3CCOCC3)=C(OC4=NC=CC=C45)C5=N2)=C1
MDL No.	MFCD11983145

PI-103 {[allProObj[0].p_purity_real_show]}

PI-103 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

PI-103 质控信息

PI-103 生物活性

PI-103 细胞实验

PI-103 动物实验

PI-103 动物研究

PI-103 参考文献

PI-103 实验方案

PI-103 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

p110γ	p110γ, IC50:15 nM
p110β	p110β, IC50:3 nM
p110α	p110α, IC50:2 nM
p110δ	p110δ, IC50:3 nM
mTOR	mTOR, IC50:30 nM
DNA-PK	DNA-PK, IC50:23 nM

别名
运输	蓝冰

PI-103 {[allProObj[0].p_purity_real_show]}

PI-103 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

PI-103 质控信息

PI-103 生物活性

PI-103 细胞实验

PI-103 动物实验

PI-103 动物研究

PI-103 参考文献

PI-103 实验方案

PI-103 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

PI-103 纯度/质量文件产品仅供科研