ALW-II-41-27

ALW-II-41-27 is a multi-kinase inhibitor that inhibits EphB2, EphA3, Kit, FMS, VEGFR2/KDR, FLT1, FGR, Src, Lyn, BMX, and Bcr-Abl in tyrosine kinase-transformed Ba/F3 cells (EC50s = 50s = 51 and 14 nM, respectively) as well as wild-type and mutant RET kinases (IC50s = 24.7, 94.2, and 15.8 nM for wild-type, RETV804L, and RETV804M, respectively). It reduces growth of NCI-H2286 and HCC-366 cancer cells (GI50s = 0.51 and 0.65 µM, respectively) and RAT1 cells transformed by RETC634R or RETM918T (IC50s = 44 and 56 nM, respectively). ALW-II-41-27 also inhibits growth of MDA-MB-231 breast cancer cells in a concentration-dependent manner and inhibits tumor growth in vivo in a mouse patient-derived xenograft (PDX) model of EphA2-overexpressing triple-negative breast cancer (TNBC).Formal Name: N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-3-[[[5-(2-thienyl)-3-pyridinyl]carbonyl]amino]-benzamide. CAS Number: 1186206-79-0. Molecular Formula: C32H32F3N5O2S. Formula Weight: 607.7. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 277 nm. SMILES: CCN1CCN(CC2=CC=C(NC(C3=CC=C(C)C(NC(C4=CC(C5=CC=CS5)=CN=C4)=O)=C3)=O)C=C2C(F)(F)F)CC1. InChi Code: InChI=1S/C32H32F3N5O2S/c1-3-39-10-12-40(13-11-39)20-23-8-9-26(17-27(23)32(33,34)35)37-30(41)22-7-6-21(2)28(16-22)38-31(42)25-15-24(18-36-19-25)29-5-4-14-43-29/h4-9,14-19H,3,10-13,20H2,1-2H3,(H,37,41)(H,38,42). InChi Key: HYWXBDQAYLPMIX-UHFFFAOYSA-N.