K-Ras inhibitor 12

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K-Ras inhibitor 12

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。

CAS NO:	1469337-95-8
规格:	≥98%

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议

产品介绍

K-Ras(G12C) inhibitor 12 is a co-valent and allosteric inhibitor of K-Ras G12C with potential antitumor activity. KRAS G12C is the mutated form of K-ras and is oncogenic. K-Ras(G12C) inhibitor 12 acts by binding to K-Ras(G12C) and forming a covalent bond with the 12C cysteine of KRAS.

理化性质和储存条件

Molecular Weight (MW)	449.67
Formula	C15H17ClIN3O3
CAS No.	1469337-95-8
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 27 mg/mL (60.0 mM)
	Water: <1 mg/mL
	Ethanol: <1 mg/mL
Other info	Chemical Name: 1-(4-(2-((4-Chloro-2-hydroxy-5-iodophenyl)amino)acetyl)piperazin-1-yl)prop-2-en-1-one InChi Key: JFIFBWVNHLXJFY-UHFFFAOYSA-N InChi Code: InChI=1S/C15H17ClIN3O3/c1-2-14(22)19-3-5-20(6-4-19)15(23)9-18-12-8-11(17)10(16)7-13(12)21/h2,7-8,18,21H,1,3-6,9H2 SMILES Code: C=CC(N1CCN(C(CNC2=CC(I)=C(Cl)C=C2O)=O)CC1)=O
Synonyms	K-Ras(G12C) inhibitor 12; K-Ras(G12C) inhibitor

实验参考方法

In Vitro	In vitro activity: K-Ras(G12C) inhibitor 12 belongs to a series of small molecules, which irreversibly bind to a common oncogenic mutant K-Ras(G12C) and blocks K-Ras(G12C) interactions. Some of them decrease viability and increase apoptosis of G12C-containing cancer cell lines. Cell Assay: K-Ras(G12C) inhibitor 12 is a highly effective Ras inhibitor and its EC50 value in H1792 cells is 0.32 μM.It selectively binds to an oncogenic mutant K-Ras(G12C) in a irreversible manner without affecting the activity of wild-type Ras. After treatment with K-Ras(G12C) inhibitor 12, K-Ras(G12C)-mutant cells exhibit decreased viability and increased apoptosis comparing to cells lacking this mutation.
In Vivo
Animal model
Formulation & Dosage
References	Nature. 2013 Nov 28;503(7477):548-51.