TAS 103 (hydrochloride)

TAS 103 is an inhibitor of DNA topoisomerase I and II (IC50s = 2 and 6.5 µM, respectively). It stabilizes topoisomerase I-DNA and topoisomerase II-DNA cleavable complexes in KB cells when used at a concentration of 3 µM. It is cytotoxic to P388 and KB cells (IC50s = 1.1 and 9.6 nM, respectively). TAS 103 (15, 26, and 45 mg/kg per day) reduces pulmonary metastasis in murine B16-BL6 melanoma and UV-2237M fibrosarcoma models of lung metastasis. It also reduces tumor growth in a variety of human cancer mouse xenograft models.Formal Name: 6-[[2-(dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one, dihydrochloride. CAS Number: 174634-09-4. Molecular Formula: C20H19N3O2 . 2HCl. Formula Weight: 406.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: PBS (pH 7.2): 1 mg/ml. lambdamax: 229, 244, 262, 292 nm. SMILES: O=C1C(C(NCCN(C)C)=NC2=C3C=CC(O)=C2)=C3C4=C1C=CC=C4.Cl.Cl. InChi Code: InChI=1S/C20H19N3O2.2ClH/c1-23(2)10-9-21-20-18-17(13-5-3-4-6-14(13)19(18)25)15-8-7-12(24)11-16(15)22-20,,/h3-8,11,24H,9-10H2,1-2H3,(H,21,22),2*1H. InChi Key: HAYAYGFVSIWSGQ-UHFFFAOYSA-N.