K RAS INHIBITOR-12

Cas No.:	1469337-95-8
Chemical Name:	1-[4-[2-[(4-chloro-2-hydroxy-5-iodophenyl)amino]acetyl]-1-piperazinyl]-2-propen-1-one
Synonyms:	K RAS INHIBITOR 12, G12C INHIBITOR12
SMILES:	IC1=C(Cl)C=C(O)C(NCC(N2CCN(C(C=C)=O)CC2)=O)=C1
Formula:	C15H17CliN3O3
M.Wt:	449.67
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Ostrem JM, et al. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature. 2013 Nov 28;503(7477):548-551.

Description:

K-Ras(G12C) inhibitor 12 is a K-Ras(G12C) inhibitor, the half-maximum effective concentration (EC50) for K-Ras(G12C) inhibitor 12 in H1792 cells is 0.32 μM.Binding of K-Ras(G12C) inhibitor 12 to K-Ras(G12C) disrupts both switch-I and switch-II, subverting the native nucleotide preference to favour GDP over GTP and impairing binding to Raf. In the absence of K-Ras(G12C) inhibitor 12, K-Ras(G12C) shows a slight preference for GTP (relative affinity 0.6).