SB-743921 (hydrochloride)

SB-743921 is a potent inhibitor of the kinesin spindle protein Eg5 (Ki = 0.5 nM for microtubule-stimulated ATPase activity). It inhibits the growth of HCT116 colon, LNCaP and PC3 prostate, K562 leukemia, BxPC-3 pancreas, and NCI-H1299 lung cancer cell lines in vitro (GI50s = 25, 22, 48, 50, 80, and 82 nM, respectively). In vivo, SB-743921 induces complete tumor regression in a COLO 205 mouse xenograft model and partial regression in MCF-7, SK-MES, H69, and OVCAR-3 mouse xenograft models. SB-743921 (2.5-10 mg/kg) also reduces tumor volume in a dose-dependent manner in a diffuse large B cell lymphoma (DLBCL) mouse xenograft model.Formal Name: N-(3-aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-4H-1-benzopyran-2-yl]-2-methylpropyl]-4-methyl-benzamide, monohydrochloride. CAS Number: 940929-33-9. Molecular Formula: C31H33ClN2O3 . HCl. Formula Weight: 553.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMSO: 50 mg/ml, Ethanol: 20 mg/ml, PBS (pH 7.2): 0.2 mg/ml. lambdamax: 203, 309 nm. SMILES: ClC1=CC=C(C(C(CC2=CC=CC=C2)=C([C@H](N(C(C3=CC=C(C)C=C3)=O)CCCN)C(C)C)O4)=O)C4=C1.Cl. InChi Code: InChI=1S/C31H33ClN2O3.ClH/c1-20(2)28(34(17-7-16-33)31(36)23-12-10-21(3)11-13-23)30-26(18-22-8-5-4-6-9-22)29(35)25-15-14-24(32)19-27(25)37-30,/h4-6,8-15,19-20,28H,7,16-18,33H2,1-3H3,1H/t28-,/m1./s1. InChi Key: MLMZVWABFOLFGV-LNLSOMNWSA-N.