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K-Ras(G12C)inhibitor 6
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 6图片
CAS NO:2060530-16-5
规格:98%
分子量:405.34
包装与价格:
包装价格(元)
10mg电议
25mg电议

产品介绍
K-Ras (G12C) inhibitor
CAS:2060530-16-5
分子式:C17H22Cl2N2O3S
分子量:405.34
纯度:98%
存储:Store at -20°C

Background:

K-Ras (G12C) inhibitor 6 is an allosterical inhibitor of oncogenic mutation K-Ras G12C [1].


K-Ras (G12C) inhibitor 6 is a cysteine-reactive small molecule. It irreversibly binds to the G12C mutantion of GTPase K-Ras but not the wild-type K-Ras with the relative potency value of 4.2. The binding pocket of K-Ras for K-Ras (G12C) inhibitor 6 is a new allosteric pocket, S-IIP. Binding of this pocket results in a change of the relative nucleotide affinity of Ras to favour GDP over GTP, leading to an accumulation of inactive Ras. Since the mutation of K-Ras is quite common in human cancers, the inhibitor of K-Ras G12C should exert suppression activities in tumor cells. It has been reported that, some of the K-Ras G12C inhibitors are indeed effective to decrease cell viability and increase apoptosis in lung cancer cell lines [1].


参考文献:
[1] Ostrem J M, Peters U, Sos M L, et al. K-Ras (G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature, 2013, 503(7477): 548-551.