MRTX1257 | KRAS G12C inhibitor | Probechem Biochemicals

Chemical Structure : MRTX1257

CAS No.: 2206736-04-9

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MRTX1257 (MRTX-1257, MRTX 1257)

货号: PC-35952Not For Human Use, Lab Use Only.

MRTX1257 (MRTX-1257, MRTX 1257) is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 0.9 nM.

规格	价格	库存
5 mg	￥1280	In stock
10 mg	￥1980	In stock
25 mg	￥3480	In stock
50 mg	￥5480	In stock
100 mg		Get quote

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生物&药学活性

MRTX1257 (MRTX-1257, MRTX 1257) is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 0.9 nM.
MRTX1257 demonstrates high selectivity toward the Cys12 of KRAS G12C in NCI-H358 cells, without effect on other free cysteine residues.
MRTX1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose in MIA PaCa-2 xenografts, shows rapid growth inhibition and durable efficacy even after dosing was stopped, and MRTX1257 is orally acitve.

物理化学性质&存储条件

分子量	565.722
分子式	C33H39N7O2
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	10 mM in DMSO
Chemical Name/SMILES	2-((S)-1-acryloyl-4-(7-(8-methylnaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)piperazin-2-yl)acetonitrile

参考文献

1. U.S. Pat. Appl. Publ. (2018), US 20180072723 A1 20180315.
2. Khan HY, et al. Cancer Res Commun. 2022 May;2(5):342-352.

MRTX1257 (MRTX-1257, MRTX 1257)

生物&药学活性

物理化学性质&存储条件

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MRTX1257 (MRTX-1257, MRTX 1257)

生物&药学活性

物理化学性质&存储条件

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