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K-Ras(G12C) inhibitor 6

现货
Catalog No.
B3694
K-Ras (G12C)抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,300.00
现货
10mg
¥ 2,000.00
现货
25mg
¥ 4,200.00
现货

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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].

References:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt405.34
Cas No.2060530-16-5
FormulaC17H22Cl2N2O3S
Solubility≥20.25mg/mL in DMSO
SDFDownload SDF
Canonical SMILESC1CN(CCC1NC(=O)CCCS)C(=O)COC2=C(C=C(C=C2)Cl)Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

描述 K-Ras(G12C) inhibitor 6是一种选择性的致癌基因K-Ras(G12C)变构抑制剂。
靶点 K-Ras(G12C)          
IC50            

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