MRTX-1133

MRTX-1133 is an inhibitor of K-RasG12D, a mutant form of K-Ras that accumulates in cancer cells. It selectively reduces ERK phosphorylation in AsPC-1 cells expressing mutant K-RasG12D (IC50 = 10.8 nM) over MiaPaCa-2 and SW620 cells expressing mutant K-RasG12C or K-RasG12V (IC50s = 456 and 4,400 nM, respectively) and MCF-7 cells expressing wild-type K-Ras in which ERK phosphorylation was not reduced.Formal Name: 4-[4-(3,8-diazabicyclo[3.2.1]oct-3-yl)-8-fluoro-2-[[(2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl]methoxy]pyrido[4,3-d]pyrimidin-7-yl]-5-ethynyl-6-fluoro-2-naphthalenol. CAS Number: 2621928-55-8. Molecular Formula: C33H31F3N6O2. Formula Weight: 600.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 50 mg/ml. lambdamax: 230 nm. SMILES: FC1=C(C2=CC(O)=CC3=C2C(C#C)=C(F)C=C3)N=CC4=C1N=C(N=C4N5CC6NC(CC6)C5)OC[C@]78N(CCC8)C[C@H](C7)F. InChi Code: InChI=1S/C33H31F3N6O2/c1-2-23-26(35)7-4-18-10-22(43)11-24(27(18)23)29-28(36)30-25(13-37-29)31(41-15-20-5-6-21(16-41)38-20)40-32(39-30)44-17-33-8-3-9-42(33)14-19(34)12-33/h1,4,7,10-11,13,19-21,38,43H,3,5-6,8-9,12,14-17H2/t19-,20?,21?,33+/m0/s1. InChi Key: SCLLZBIBSFTLIN-CKTHFEKDSA-N.