GDC-0941,[PI 3-K Inhibitor XXI];≥99% (HPLC)

别名;GDC0941;Pictrelisib;2-(1H-吲唑-4-基)-6-(4-甲磺酰哌嗪-1-基甲基)-4-吗啉-4-基-噻吩并[3,2-d]嘧啶;2-(1H-Indazol-4-yl)-6-(4-methylsulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2- d]pyrimidine;4-(2-(1H-Indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine;2-(1H-吲唑-4-基)-6-(4-甲烷磺酰基哌嗪-1-基甲基)-4-吗啉-4-基-噻吩并[3,2-d]嘧

Empirical Formula (Hill Notation): C23H27N7O3S2 CAS号: 957054-30-7 分子量: 513.64
货号(SKU): 5.09226
CAS号: 957054-30-7
MDL号: MFCD11616196
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¥926.00

说明

一般描述

A cell-permeable thienopyrimidine compound that acts as a potent, ATP-competitive inhibitor against class IA (IC50 = 3 nM/p110α, 33 nM/p110β, 3 nM/p110δ) & IB (IC50 = 75 nM/p110γ) PI 3-K kinases, including the two known p110α hot spot mutants E454K & H1047R (IC50 = 3 nM), while exhibiting much reduced or little potency against more than 200 other kinases, including TrkA, class II C2β, class IV mTOR & DNA-PK (IC50 = 2.85, 0.67, 0.58, and 1.23 µM, respectively) and class III Vps34 (IC50 >10 µM). Effectively inhibits cellular Akt S473 phosphorylation (IC50 = 28 to 46 nM) as well as proliferation in cancer cultures in vitro (GI50 = 280 to 950 nM) and completely prevents the expansion of U87MG glioblastoma xenograft in mice in vivo (by 83%; 75 mg/kg/d p.o. for 21 days). Oral bioavailability is reported in human, dog, mouse, and rat.
A cell-permeable thienopyrimidine compound that acts as a potent, ATP-competitive inhibitor against class IA (IC50 = 3 nM/p110α, 33 nM/p110β, 3 nM/p110δ) & IB (IC50 = 75 nM/p110γ) PI 3-K kinases, including the two known p110α hot spot mutants E454K & H1047R (IC50 = 3 nM), while exhibiting much reduced or little potency against more than 200 other kinases, including TrkA, class II C2β, class IV mTOR & DNA-PK (IC50 = 2.85, 0.67, 0.58, and 1.23 µM, respectively) and class III Vps34 (IC50 >10 µM). Effectively inhibits cellular Akt S473 phosphorylation (IC50 = 46 nM/U87MG, 37 nM/PC3, and 28 nM/MDA-MB-361) as well as proliferation in cancer cultures in vitro (GI50 = 950/U87MG, 280/PC3, and 720 nM/MDA-MB-361) and greatly prevents the expansion of U87MG glioblastoma xenograft in mice in vivo (by 83%; 75 mg/kg/d p.o. for 21 days). Oral bioavailability is reported in human, dog, mouse, and rat.
 

生化/生理作用

Cell permeable: yes
Primary Target
PI 3-K
Reversible: yes
 

警告

Toxicity: Standard Handling (A)
 

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Use only fresh DMSO for reconstitution.
 

其他说明

Tabe, Y., et al. 2014. Acta Haematol.131, 59.
Ware, J.A., et al. 2013. Mol. Pharm.10, 4047.
Junttila,.T., et al. 2009. Cancer Cell15, 429.
Raynaud, F.I., et al. 2009. Mol Cancer Ther.8, 1725.
Folkes, A. J., et al. 2008. J. Med. Chem.51, 5522.
 

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
 
 

属性

检测方案

≥99% (HPLC)

质量水平

形式

solid

manufacturer/tradename

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

white

溶解性

DMSO: 50 mg/mL

储存温度

2-8°C

InChI

1S/C23H27N7O3S2/c1-35(31,32)30-7-5-28(6-8-30)15-16-13-20-21(34-16)23(29-9-11-33-12-10-29)26-22(25-20)17-3-2-4-19-18(17)14-24-27-19/h2-4,13-14H,5-12,15H2,1H3,(H,24,27)

InChI key

LHNIIDJUOCFXAP-UHFFFAOYSA-N

 

安全信息

储存分类代码

11 - Combustible Solids

WGK

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.2-8°C冷藏
全球实时库存 Availability √美国St. Louis ≥ 20 | 欧洲Eur. ≥ 16 | 東京Tokyo ≥ 5 | 香港与北京 ≥ 20