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MRTX-1257

本半岛bd体育手机客户端不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2206736-04-9

包装与价格：

半岛bd体育手机客户端介绍

MRTX-1257 是选择性的、不可逆的、共价的并具有口服活性的 KRAS G12C 抑制剂，其在 H358 细胞中测得 KRAS 依赖 ERK 磷酸化的 IC50 值为 900 pM。

Cas No.	2206736-04-9
分子式	C33H39N7O2
分子量	565.71
溶解度	DMSO : 55 mg/mL (97.22 mM; Need ultrasonic)
储存条件	Store at -20°C, stored under nitrogen
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端描述	MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells[1]. MRTX-1257 (1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg, orally, daily for 30 days) shows rapid tumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in mice[1].MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups[1].MRTX-1257 dosed of 100 mg/kg daily leads to complete responses that are maintained >70 days after cessation of treatment[1]. [1]. Matthew et al. Structure-Based Drug Discovery of MRTX1257, a Selective, Covalent KRAS G12C Inhibitor with Oral Activity in Animal Models of Cancer.