G12Si-5

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G12Si-5

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

生物活性

G12Si-5 is a covalent inhibitor of theG12Smutant ofK-Ras(K_i: 26 μM). G12Si-5 binds with the S-IIP domain and suppresses oncogenic signaling. G12Si-5 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) leads to nearly complete loss of RasoGTP and concomitant inhibition of phospho-ERK in A549 cells^[1].
G12Si-5 (10 μM, 2 h) 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) 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

574.05

Formula

C₃₁H₂₉ClFN₅O₃

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.