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RMC-4550 (RMC4550)
RMC-4550 is a potent, selective and orally available small molecule allosteric inhibitor of SHP2, acting by stabilizing the SHP2 protein in an inactive conformation that is unable to transmit cell growth signals. It inhibits purified, activated full length human SHP2 with an IC50 of 1.6 nM, and has cellular IC50 of 39 nM in PC9 cells with a pERK readout. RMC-4550 has no detectable inhibitory activity up to 10 µM against the catalytic domain of SHP2, a panel of 14 additional protein phosphatases, and a panel of 468 protein kinases. RMC-4450 as a single agent was found to attenuate signal transduction through the RAS-MAP kinase cascade, reduce tumor growth and cause tumor cell death in preclinical xenograft studies of human tumors carrying select mutations in the RAS-MAP kinase pathway.
Catalog NO: CT-RMC4550
Synonym: RMC4550
CAS NO: 2172651-73-7
Mol. Formula: C21H26Cl2N4O2
MW: 437.4
** in vivo grade material. >99.5% Pure by achiral and chiral HPLCs, a stereomerically pure single isomer (out of possible four), free base (salt-free), validated by a spot-on microanalysis, made for in vivo studies. Bulk stock (Grams), prompt.