1469337-95-8K-Ras(G12C) inhibitor 12

产品属性：

Cas No.1469337-95-8

别名

化学名 1-[4-[2-(4-chloro-2-hydroxy-5-iodoanilino)acetyl]piperazin-1-yl]prop-2-en-1-one

分子式 C15H17ClIN3O3

分子量 449.67

溶解度 ≥ 8.98mg/mL in DMSO with gentle warming

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
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].