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K-Ras(G12C) inhibitor 9

现货
Catalog No.
B6002
致癌K-ras(G12C)的变构抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,400.00
Ship with 10-15 days
25mg
¥ 3,500.00
Ship with 10-15 days

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Background

Target: K-Ras(G12C)

IC50: N/A

K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C) [1]. Ras proteins belong to the large family of GTPase enzymes which are essential to transduce extracellular signals into diverse cellular responses including proliferation, differentiation, and apoptosis. About 30% of all human cancers contain activating Ras mutations, making them one of the most common known genetic molecular drivers of cancer [2]. Therefore, K-Ras signaling have potential therapeutic advantages in cancer. K-Ras(G12C) is present in roughly 10–20% of Ras-driven cancers and in an estimated 50% of Ras-mutated lung adenocarcinomas [3].

In vitro: K-Ras(G12C) inhibitor 9 belongs to a series of small molecules, which irreversibly compete with GTP and GDP for binding to a common oncogenic K-Ras(G12C) mutant and blocked the association of B-Raf and C-Raf with K-Ras(G12C). K-Ras(G12C) inhibitor 9 (10 μM) decreased viability and increased apoptosis of G12C mutations-containing lung cancer cell lines (H1792, Calu-1, H358, and H23) [1].

In vivo: N/A

References:
1.  Ostrem JM, Peters U, Sos ML, Wells JA, Shokat KM. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature. 2013;503(7477):548-51.
2.  Hunter JC, Gurbani D, Ficarro SB, Carrasco MA, Lim SM, Choi HG, et al. In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C. Proc Natl Acad Sci U S A. 2014;111(24):8895-900.
3.  Lim SM, Westover KD, Ficarro SB, Harrison RA, Choi HG, Pacold ME, et al. Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor. Angew Chem Int Ed Engl. 2014;53(1):199-204.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt513.78
Cas No.1469337-91-4
FormulaC16H21ClIN3O4S
SolubilitySoluble in DMSO
Chemical NameN-(1-(2-((4-chloro-5-iodo-2-methoxyphenyl)amino)acetyl)piperidin-4-yl)ethenesulfonamide
SDFDownload SDF
Canonical SMILESC=CS(NC1CCN(C(CNC2=C(OC)C=C(Cl)C(I)=C2)=O)CC1)(=O)=O
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。

质量控制

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批次:

化学结构

K-Ras(G12C) inhibitor 9