Cas No.: | 2172651-73-7 |
Synonyms: | RMC-4550,RMC 4550,RMC4550 |
SMILES: | ClC1=C(Cl)C(C2=NC(CO)=C(N3CCC4(CO[C@@H](C)[C@H]4N)CC3)N=C2C)=CC=C1 |
Formula: | C21H26Cl2N4O2 |
M.Wt: | 437.365 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | RMC-4550 is a potent, selective and allosteric inhibitor of SHP2, with an IC50 of 0.583 nM. |
Target: | IC50:0.583 nM (SHP2)[1]. |
In Vitro: | RMC-4550 is an allosteric inhibitor of SHP2 and stabilizes the auto-inhibited conformation of wild-type SHP2 enzyme, with a mode of inhibition similar to SHP099. Consistent with an allosteric mode of inhibition, RMC-4550 inhibits the activity of full-length wild-type SHP2 enzyme activated by a di-phosphotyrosine peptide, but lacks activity against the free catalytic domain of SHP2[1]. |
References: | [1]. Nichols RJ, et al. RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers. Nat Cell Biol. 2018 Sep;20(9):1064-1073. |