COTI-2

COTI-2 is an orally available thiosemicarbazone that activates mutant forms of p53. It induces apoptosis in a wide variety of human tumor cells in culture, inhibits the proliferation of colorectal cancer cell lines more effectively than cetuximab and erlotinib (Cay-10483), and is active against human glioblastoma cell lines at nanomolar concentrations. COTI-2 functions well in vivo, inhibiting the growth of HT-29 colorectal, SHP-77 small cell lung cancer, and OVCAR-3 ovarian carcinoma xenograft cells in mice with minimal toxicity.Formal Name: 4-(2-pyridinyl)-2-(6,7-dihydro-8(5H)-quinolinylidene)hydrazide-1-piperazinecarbothioic acid. CAS Number: 1039455-84-9. Molecular Formula: C19H22N6S. Formula Weight: 366.5. Purity: >95% (E/Z mixture). Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2.5 mg/mL, DMF:PBS (pH 7.2) (1:4): 0.2 mg/mL, DMSO: 1 mg/mL. SMILES: S=C(N/N=C1C(N=CC=C2)=C2CCC\1)N(CC3)CCN3C4=NC=CC=C4. InChi Code: InChI=1S/C19H22N6S/c26-19(23-22-16-7-3-5-15-6-4-10-21-18(15)16)25-13-11-24(12-14-25)17-8-1-2-9-20-17/h1-2,4,6,8-10H,3,5,7,11-14H2,(H,23,26)/b22-16-. InChi Key: UTDAKQMBNSHJJB-JWGURIENSA-N.