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MRTX0902
本产品不向个人销售,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。
MRTX0902图片
CAS NO:2654743-22-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍

MRTX0902 (MRTX-0902) is a novel, potent, selective, brain-penetrant, and orally bioavailable SOS1 binder that disrupts the SOS1:KRASG12C PPI (protein-protein interaction) with a binding Ki of 1.9 nM and IC50 of 29 nM in MKN1 cells. Oral administration of MRTX0902 in combination with MRTX849 results in a significant increase in antitumor activity relative to that of either single agent, including tumor regressions in a subset of animals in the MIA PaCa-2 tumor mouse xenograft model. SOS1 is one of the major guanine nucleotide exchange factors that regulates the ability of KRAS to cycle through its 'on' and 'off' states. Disrupting the SOS1:KRASG12C protein–protein interaction (PPI) can increase the proportion of GDP-loaded KRASG12C, providing a strong mechanistic rationale for combining inhibitors of the SOS1:KRAS complex with inhibitors like MRTX849 that target GDP-loaded KRASG12C.

纯度:≥98%

CAS:2654743-22-1