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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-MRTX0902
MRTX0902

Chemical Structure : MRTX0902

CAS No.: 2654743-22-1

MRTX0902 (MRTX-0902, MRTX 0902)

货号: PC-73313Not For Human Use, Lab Use Only.

MRTX0902 is a highly potent, selective SOS1 inhibitor with binding IC50 of 2 nM, cellular IC50 of 33 nM (pERK).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MRTX0902 is a highly potent, selective SOS1 inhibitor with binding IC50 of 2 nM, cellular IC50 of 33 nM (pERK).
MRTX0902 displays weak to no affinity for SOS2 with IC50 of >10 uM.
MRTX0902 exhibits promising potency, selectivity, and exposure in preclinical species.
MRTX0902 in combined with MRTX849 demonstrates durable regression in KRasG12C NSCLC and CRC PDX models.
MRTX0902 demonstrates improved efficacy with osimertinib (EGFRi), VS-6766 (RAF/MEKc) in MAPK tumor models.

物理化学性质&存储条件

分子量 388.475
分子式 C22H24N6O
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

(R)-2-methyl-3-(1-((4-methyl-7-morpholinopyrido[3,4-d]pyridazin-1-yl)amino)ethyl)benzonitrile

参考文献

1. Ketcham JM, et al. J Med Chem. 2022 Jul 28;65(14):9678-9690.

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