K-Ras inhibitor 6

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K-Ras inhibitor 6

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CAS NO:	2060530-16-5
规格:	≥98%

包装与价格：

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

K-Ras (G12C) inhibitor 6 is a novel, potent, allosteric, irreversible,/covalent cysteine-reactive small molecule KRAS G12C inhibitor with anticancer activity. KRAS G12C is oncogenicand can cause 100% modification of the protein when used at 10 μM for 24 hours in vitro. It binds to the G12C mutantion of GTPase K-Ras irreversibly but does not bind the wild-type K-Ras with the relative potency value of 4.2. The binding pocket of K-Ras for K-Ras (G12C) inhibitor 6 is a new allosteric pocket, S-IIP. Binding of this pocket results in a change of the relative nucleotide affinity of Ras to favour GDP over GTP, leading to an accumulation of inactive Ras.

理化性质和储存条件

Molecular Weight (MW)	405.34
Formula	C17H22Cl2N2O3S
CAS No.	2060530-16-5
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 81 mg/mL (199.8 mM)
	Water: <1 mg/mL
	Ethanol: 30 mg/mL (74.0 mM)
Other info	Chemical Name: N-(1-(2-(2,4-dichlorophenoxy)acetyl)piperidin-4-yl)-4-mercaptobutanamide InChi Key: ZPXCEHMKUTXHRZ-UHFFFAOYSA-N InChi Code: InChI=1S/C17H22Cl2N2O3S/c18-12-3-4-15(14(19)10-12)24-11-17(23)21-7-5-13(6-8-21)20-16(22)2-1-9-25/h3-4,10,13,25H,1-2,5-9,11H2,(H,20,22) SMILES Code: ClC1=CC=C(OCC(N2CCC(NC(CCCS)=O)CC2)=O)C(Cl)=C1
Synonyms	K-Ras(G12C) Inhibitor-6

实验参考方法

In Vitro	In vitro activity: K-Ras(G12C) inhibitor 6 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: Since the mutation of K-Ras is quite common in human cancers, the inhibitor of K-Ras G12C should exert suppression activities in tumor cells. It has been reported that, some of the K-Ras G12C inhibitors are indeed effective to decrease cell viability and increase apoptosis in lung cancer cell lines.
In Vivo
Animal model
Formulation & Dosage
References	Nature. 2013 Nov 28;503(7477):548-51.