HTI 286

HTI 286 is an inhibitor of microtubule polymerization. It binds to (Kd = 260 nM) and inhibits the polymerization of tubulin in a cell-free assay when used at concentrations of 0.1 and 1 µM. HTI 286 (30 nM) induces cell cycle arrest at the G2/M phase and apoptosis in KB-3-1 epidermoid carcinoma cells. It inhibits cell growth in a panel of 18 tumor cell lines, including HCT-15 and DLD-1 colon cancer cells, which overexpress P-glycoprotein (mean IC50 = 2.5 nM). HTI 286 (1.6 mg/kg) reduces tumor volume in LOX, KB-3-1, KB-8-5, MX-1, DLD-1, and HCT-15 mouse xenograft models.Formal Name: N,beta,beta-trimethyl-L-phenylalanyl-N-[(1S,2E)-3-carboxy-1-(1-methylethyl)-2-buten-1-yl]-N,3-dimethyl-L-valinamide. CAS Number: 228266-40-8. Synonyms: Taltobulin, SPA 110. Molecular Formula: C27H43N3O4. Formula Weight: 473.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 40 mg/ml. SMILES: CC(C)(C1=CC=CC=C1)[C@H](NC)C(N[C@@H](C(C)(C)C)C(N(C)[C@@H](C(C)C)/C=C(C)/C(O)=O)=O)=O. InChi Code: InChI=1S/C27H43N3O4/c1-17(2)20(16-18(3)25(33)34)30(10)24(32)22(26(4,5)6)29-23(31)21(28-9)27(7,8)19-14-12-11-13-15-19/h11-17,20-22,28H,1-10H3,(H,29,31)(H,33,34)/b18-16+/t20-,21-,22-/m1/s1. InChi Key: CNTMOLDWXSVYKD-PSRNMDMQSA-N.