R428

R428 is a small molecule inhibitor of Axl kinase, both in an in vitro biochemical assay and in a cell-based assay using phosphorylation of Ser473 on Akt as the readout (EC50s = 14 nM for both). It is orally bioavailable, blocks angiogenesis in corneal micropocket and tumor models, and reduces metastatic burden while extending survival in mouse models of breast cancer metastasis. R428 synergizes with cisplatin (Cay-13119) to enhance suppression of liver micrometastasis. R428 is used to study the role of Axl kinase signaling in cancer, cellular senescence, and Zika virus infection.Formal Name: 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5Hbenzocyclohepten-2-yl]-1H-1,2,4-triazole-3,5-diamine. CAS Number: 1037624-75-1. Synonyms: Bemcentinib, BGB 324. Molecular Formula: C30H34N8. Formula Weight: 506.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: >5 mg/ml. lambdamax: 258, 317 nm. SMILES: NC1=NC(NC2=CC=C3C(CC[C@@H](N4CCCC4)CC3)=C2)=NN1C5=NN=C(C(C=CC=C6)=C6CCC7)C7=C5. InChi Code: InChI=1S/C30H34N8/c31-29-33-30(32-24-13-10-20-11-14-25(15-12-22(20)18-24)37-16-3-4-17-37)36-38(29)27-19-23-8-5-7-21-6-1-2-9-26(21)28(23)35-34-27/h1-2,6,9-10,13,18-19,25H,3-5,7-8,11-12,14-17H2,(H3,31,32,33,36)/t25-/m0/s1. InChi Key: KXMZDGSRSGHMMK-VWLOTQADSA-N.