For research use only. Not for therapeutic Use.
RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction[1].
RMC-0331 has an IC50 of 71 nM measuring by the rate of GDP/GTP exchange in vitro[1].
RMC-0331 (100-250 mg/kg; p.o.; qd; immunocompetent mice) shows single agent anti-tumor activity in SHP2-mutant models[1].
| Catalog Number | I044531 |
| CAS Number | 2488788-52-7 |
| Synonyms | [4-[[(1R)-1-[3-amino-5-(trifluoromethyl)phenyl]ethyl]amino]-2-chloro-5,7-dihydropyrrolo[3,4-d]pyrimidin-6-yl]-(4-methoxyoxan-4-yl)methanone |
| Molecular Formula | C22H25ClF3N5O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H25ClF3N5O3/c1-12(13-7-14(22(24,25)26)9-15(27)8-13)28-18-16-10-31(11-17(16)29-20(23)30-18)19(32)21(33-2)3-5-34-6-4-21/h7-9,12H,3-6,10-11,27H2,1-2H3,(H,28,29,30)/t12-/m1/s1 |
| InChIKey | HOBOGRTXXDLZIB-GFCCVEGCSA-N |
| SMILES | CC(C1=CC(=CC(=C1)N)C(F)(F)F)NC2=NC(=NC3=C2CN(C3)C(=O)C4(CCOCC4)OC)Cl |
| Reference | [1]. Andreas Buckl, et al. Discovery of a Potent, Selective and Orally Bioavailable SOS1 Inhibitor, RMC-0331 (RM-023), an in vivo Tool Compound that Blocks RAS Activation via Disruption of the RAS-SOS1 Interaction. |
