AZM475271

AZM475271 is an inhibitor of c-Src kinase (IC50 = 0.01 µM). It inhibits phosphorylation of c-Src kinase, Lck, c-Yes, and VEGFR2 (IC50s = 0.01, 0.03, 0.08, and 0.7 µM, respectively). AZM475271 inhibits proliferation of NIH3T3 fibroblasts, as well as PC3 and DU145 prostate and A549 lung cancer cells (IC50s = 0.5, 32, 16, and 17 µM, respectively). It reduces tumor cell proliferation and microvessel density and increases apoptosis in an L3.6pl pancreatic cancer mouse xenograft model when administered at a dose of 50 mg/kg per day. AZM475271 inhibits tumor growth and metastasis in the same mouse xenograft model when administered in combination with gemcitabine (Cay-11690, Cay-9003096).Formal Name: N-(2-chloro-5-methoxyphenyl)-6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-4-quinazolinamine. CAS Number: 476159-98-5. Synonyms: M475271. Molecular Formula: C23H27ClN4O3. Formula Weight: 442.9. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: Slightly soluble, DMSO: Slightly soluble, Ethanol: Slightly soluble. SMILES: ClC1=CC=C(C=C1NC2=C3C=C(OC)C(OCC4CCN(CC4)C)=CC3=NC=N2)OC. InChi Code: InChI=1S/C23H27ClN4O3/c1-28-8-6-15(7-9-28)13-31-22-12-19-17(11-21(22)30-3)23(26-14-25-19)27-20-10-16(29-2)4-5-18(20)24/h4-5,10-12,14-15H,6-9,13H2,1-3H3,(H,25,26,27). InChi Key: WPOXAFXHRJYEIC-UHFFFAOYSA-N.