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

别名;GDC0941;Pictrelisib;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

CAS号 957054-30-7 经验分子式(希尔表示法) C23H27N7O3S2 分子量 513.64
货号(SKU): 509226
CAS号: 957054-30-7
MDL号: MFCD11616196
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$185.93

产品描述

一种有效的PI3Kα/δ抑制剂,IC50:3 nM。

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PI 3-K

Reversible: yes

包装

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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.

Other Notes

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

性质

Quality Level  100
assay  ≥99% (HPLC)
form  solid
mfr. no.  Calbiochem®
storage condition  OK to freeze
 protect from light
storage conditions  +2C to +8C
color  white
solubility  DMSO: 50 mg/mL


安全信息

风险声明 (欧洲) 23/24/25
安全声明 (欧洲) 26-36
WGK德国 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 ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16