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G12Si-5 formic
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。
G12Si-5 formic图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
G12Si-5 formic 是K-RasG12S突变体的共价抑制剂 (Ki: 26 μM)。G12Si-5 formic 与 S-IIP 结构域结合并抑制致癌信号。G12Si-5 formic 可降低 KRAS G12S 突变细胞中的 ERK 磷酸化水平。
生物活性

G12Si-5 formic is a covalent inhibitor of theG12Smutant ofK-Ras(Ki: 26 μM). G12Si-5 formic binds with the S-IIP domain and suppresses oncogenic signaling. G12Si-5 formic reduces phospho-ERK level in KRAS G12S mutated cells[1].

IC50& Target[1]

KRas G12S

26 μM (Ki)

体外研究
(In Vitro)

G12Si-5 (10 μM, 2 h) formic leads to nearly complete loss of RasoGTP and concomitant inhibition of phospho-ERK in A549 cells[1].
G12Si-5 (10 μM, 2 h) formic leads to a reduction in the phospho-ERK level and gel-mobility shift of the K-Ras protein in cell lines with confirmed KRAS p.G12S mutations (A549, KMS20)[1].
G12Si-5 (100 μM, 72 h) formic inhibits the growth of the K-Ras(G12S)-transduced Ba/F3 cells with an IC50of 2.4 μM[1].

Western Blot Analysis[1]

Cell Line:A549 cells
Concentration:0, 0.37, 1.1, 3.3, 10, 30 μM
Incubation Time:2 h
Result:Dose-dependently decreased Ras (G12S) and p-ERK expression.
分子量

620.07

Formula

C32H31ClFN5O5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.