AMG 510

AMG 510 is a covalent inhibitor of K-RasG12C. It inhibits EGF-induced phosphorylation of ERK1/2 in MIA PaCa-2 cells (IC50 = 68 nM). AMG 510 reduces the viability of MIA PaCa-2 cells that express K-RasG12C but not K-RasG12S-expressing A549 cells (IC50s = 5 and 36,500 nM, respectively). In vivo, AMG 510 (10, 30, and 100 mg/kg) reduces intratumor ERK1/2 phosphorylation and tumor volume in a MIA PaCa-2 mouse xenograft model.Formal Name: (1R)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-pyrido[2,3-d]pyrimidin-2(1H)-one. CAS Number: 2296729-00-3. Molecular Formula: C30H30F2N6O3. Formula Weight: 560.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 25 mg/ml, DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml, DMSO: 20 mg/ml, Ethanol: 1 mg/ml. lambdamax: 214 nm. SMILES: O=C1N=C(N2CCN(C(C=C)=O)CC2C)C3=CC(F)=C(C4=C(O)C=CC=C4F)N=C3N1C5=C(C(C)C)N=CC=C5C. InChi Code: InChI=1S/C30H30F2N6O3/c1-6-23(40)36-12-13-37(18(5)15-36)28-19-14-21(32)26(24-20(31)8-7-9-22(24)39)34-29(19)38(30(41)35-28)27-17(4)10-11-33-25(27)16(2)3/h6-11,14,16,18,39H,1,12-13,15H2,2-5H3. InChi Key: NXQKSXLFSAEQCZ-UHFFFAOYSA-N.