product name K-Ras(G12C) inhibitor 6
Description: K-Ras(G12C) inhibitor 6 is an allosteric, cysteine-reactive small molecule and selective inhibitor of oncogenic K-Ras(G12C). 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.
References: Nature. 2013 Nov 28;503(7477):548-51.
405.34
Formula
C17H22Cl2N2O3S
CAS No.
587841-73-4
Storage
-20℃ for 3 years in powder form
-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)
Solubility (In vivo)
Synonyms
other peoduct :
| 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. Kinase Assay: 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. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Nature. 2013 Nov 28;503(7477):548-51. |
