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K-Ras(G12C)inhibitor 12
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。
K-Ras(G12C)inhibitor 12图片
CAS NO:1469337-95-8
规格:98%
分子量:449.67
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
allosteric inhibitor of K-Ras(G12C)
CAS:1469337-95-8
分子式:C15H17ClIN3O3
分子量:449.67
纯度:98%
存储:Store at -20°C

Background:

K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of K-Ras(G12C) [1].


K-Ras is a GTPase and plays an important role in many signal transduction pathways. The mutation of K-Ras occurs in many cancers.


K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of K-Ras(G12C). K-Ras(G12C) exhibited a slight preference for GTP. However, K-Ras(G12C) inhibitor 12 significantly reduced the affinity for GTP and led to the modification of K-Ras(G12C). Also, K-Ras(G12C) inhibitor 12 inhibited SOS-catalysed nucleotide exchange. In H1792 and H358 K-Ras(G12C)-mutant lung cancer cell lines, K-Ras(G12C) inhibitor 12 reduced the association of C-Raf and B-Raf with Ras. In H1792, H358, H23 and Calu-1 cell lines containing G12C mutations, K-Ras(G12C) inhibitor 12 decreased viability and induced apoptosis. K-Ras(G12C) inhibitor 12 exhibited EC50 value of 0.32 μM in H1792 cells. Also, the H1792 cells exhibited low levels of K-Ras GTP, which was consistent with the preference of K-Ras(G12C) inhibitor 12 to K-Ras GDP [1].


Reference:
[1].  Ostrem JM1, Peters U, Sos ML, et al. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature, 2013, 503(7477): 548-551.