MRTX849 (Adagrasib, MRTX-849)

Chemical Structure : MRTX849

CAS No.: 2326521-71-3

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货号: PC-72227Not For Human Use, Lab Use Only.

MRTX849 (Adagrasib, MRTX-849) is a potent, selective, and covalent KRAS G12C inhibitor, inhibits KRAS-dependent signaling.

规格	价格	库存
5 mg	￥580	In stock
10 mg	￥880	In stock
25 mg	￥1380	In stock
50 mg	￥2280	In stock
100 mg	￥3780	In stock
250 mg		Get quote

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生物&药学活性

MRTX849 (Adagrasib, MRTX-849) is a potent, selective, and covalent KRAS G12C inhibitor, inhibits KRAS-dependent signaling.
MRTX849 (Adagrasib) binds to, stabilizes and selectively modifies mutant cysteine 12 in GDP-bound KRAS G12C, and inhibits KRAS-dependent signaling.
MRTX849 (Adagrasib) inhibited KRAS-dependent signaling targets including ERK1/2 phosphorylation (Thr202/Tyr204 ERK1; pERK), S6 phosphorylation (RSK-dependent Ser235/236; pS6) and expression of the ERK-regulated DUSP6, each with IC50 values in the single-digit nanomolar range in KRASG12C-mutant H358 lung and MIA PaCa-2 pancreatic cancer cell lines.
MRTX849 (Adagrasib) potently inhibited cell growth in the vast majority of KRASG12C-mutant cell lines with IC50 of 10-973 nM.
MRTX849 (Adagrasib) inhibited KRAS signaling and tumor growth in vivo, demonstrated potent anti-tumor activity in KRASG12C-mutant and non KRASG12C-mutant human tumor xenografts models.

物理化学性质&存储条件

分子量	604.13
分子式	C32H35ClFN7O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	20 mM in DMSO (12.1 mg/mL)
Chemical Name/SMILES	2-((S)-4-(7-(8-Chloronaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile

参考文献

1. Hallin J, et al. Cancer Discov. 2020 Jan;10(1):54-71.