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K-Ras(G12C) inhibitor 12 Sale

目录号 : GC12247

An allosteric inhibitor of oncogenic K-Ras(G12C)

K-Ras(G12C) inhibitor 12 Chemical Structure

Cas No.:1469337-95-8

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10mM (in 1mL DMSO)
¥1,428.00
现货
5mg
¥1,050.00
现货
25mg
¥2,489.00
现货

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Sample solution is provided at 25 µL, 10mM.

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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.

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1 mg 5 mg 10 mg
1 mM 2.2239 mL 11.1193 mL 22.2385 mL
5 mM 0.4448 mL 2.2239 mL 4.4477 mL
10 mM 0.2224 mL 1.1119 mL 2.2239 mL
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