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K-Ras(G12C) inhibitor 12

现货
Catalog No.
B4876
K-Ras(G12C)别构抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,440.00
Ship with 10-15 days
5mg
¥ 1,440.00
Ship with 10-15 days
25mg
¥ 4,200.00
Ship with 10-15 days

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Background

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.

文献引用

1. Chen Z, Yang D, et al. "Final-2 targeted glycolysis mediated apoptosis and autophagy in human lung adenocarcinoma cells but failed to inhibit xenograft in nude mice." Food Chem Toxicol. 2019 Aug;130:1-11. PMID:31054290

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt449.67
Cas No.1469337-95-8
FormulaC15H17ClIN3O3
Solubility≥8.98mg/mL in DMSO with gentle warming
Chemical Name1-[4-[2-(4-chloro-2-hydroxy-5-iodoanilino)acetyl]piperazin-1-yl]prop-2-en-1-one
SDFDownload SDF
Canonical SMILESC=CC(=O)N1CCN(CC1)C(=O)CNC2=CC(=C(C=C2O)Cl)I
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。

试验操作

细胞实验[1]:

细胞系

肺癌细胞系H23, H358 和 H1792

溶解方法

在DMSO中的溶解度有限。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

72 h,10 μM

应用

K-Ras(G12C) inhibitor 12是一种高效的Ras抑制剂,在H1792细胞中的EC50是0.32 μM。它选择性地不可逆结合到K-Ras的G12C致癌突变体上,却不影响野生型Ras的活性。和没有突变的细胞比起来,用K-Ras(G12C) inhibitor 12处理后的K-Ras(G12C)突变细胞活力下降,凋亡增加。

References:

[1]. Ostrem J M, Peters U, Sos M L, et al. K-Ras (G12C) inhibitors allosterically control GTP affinity and effector interactions[J]. Nature, 2013, 503(7477): 548-551.

质量控制

质量控制和MSDS

批次:

化学结构

K-Ras(G12C) inhibitor 12

相关生物数据

K-Ras(G12C) inhibitor 12