BO-264

BO-264 is a transforming acidic coiled-coil containing protein 3 (TACC3) inhibitor. It binds to TACC3 in thermal shift and drug affinity responsive target stability (DARTS) assays and inhibits the growth of JIMT-1, HCC1954, MDA-MB-231, MDA-MB-436, and CAL-51 cancer cells (IC50s = 0.19, 0.16, 0.12, 0.13, and 0.36 µM, respectively). BO-264 is cytotoxic to RT4 cells that endogenously express TACC3-FGFR3 fusion proteins (IC50 = 3.66 µM). It induces mitotic arrest, apoptosis, and aberrant spindle formation and reduces centrosomal localization of TACC3 in JIMT-1 cells. BO-264 (25 mg/kg) reduces tumor volume and increases median survival in an EMT6 mouse xenograft model.Formal Name: N-[3-(4-methoxyphenyl)-5-isoxazolyl]-2-(4-morpholinyl)-4-pyrimidinamine. CAS Number: 2408648-20-2. Molecular Formula: C18H19N5O3. Formula Weight: 353.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 1 mg/ml, Ethanol: insol, PBS (pH 7.2): insol. lambdamax: 252, 312 nm. SMILES: COC(C=C1)=CC=C1C2=NOC(NC3=NC(N4CCOCC4)=NC=C3)=C2. InChi Code: InChI=1S/C18H19N5O3/c1-24-14-4-2-13(3-5-14)15-12-17(26-22-15)20-16-6-7-19-18(21-16)23-8-10-25-11-9-23/h2-7,12H,8-11H2,1H3,(H,19,20,21). InChi Key: WRCGBYNVBFVRTN-UHFFFAOYSA-N.