MRTX-0902

MRTX-0902 is an inhibitor of the protein-protein interaction between son of sevenless homolog 1 (SOS1) and K-Ras containing a glycine-to-cysteine mutation at position 12 (K-RasG12C, Ki = 1.9 nM). It is selective for the SOS1-K-RasG12C protein-protein interaction over the SOS1 and wild-type K-Ras protein-protein interaction (IC50 = >10,000 nM). MRTX-0902 decreases phosphorylated ERK levels in MKN1 gastric adenosquamous carcinoma cells (IC50 = 29 nM). In vivo, MRTX-0902 (25 or 50 mg/kg twice per day), in combination with the covalent inhibitor of K-RasG12C MTX-849 (Cay-31440), reduces tumor volume and phosphorylated ERK levels in a PaCa-2 pancreatic cancer mouse xenograft model.Formal Name: 2-methyl-3-[(1R)-1-[[4-methyl-7-(4-morpholinyl)pyrido[3,4-d]pyridazin-1-yl]amino]ethyl]-benzonitrile. CAS Number: 2654743-22-1. Molecular Formula: C22H24N6O. Formula Weight: 388.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble. SMILES: C[C@H](C1=CC=CC(C#N)=C1C)NC2=NN=C(C)C3=C2C=C(N4CCOCC4)N=C3. InChi Code: InChI=1S/C22H24N6O/c1-14-17(12-23)5-4-6-18(14)15(2)25-22-19-11-21(28-7-9-29-10-8-28)24-13-20(19)16(3)26-27-22/h4-6,11,13,15H,7-10H2,1-3H3,(H,25,27)/t15-/m1/s1. InChi Key: ILPWEAHQRAWJIU-OAHLLOKOSA-N.