COTI-2

Information COTI-2 COTI-2 is an orally available third generation thiosemicarbazone and activator of mutant forms of the p53 protein, with potential antineoplastic activity. Targets p53 mutants In vitro The thiosemicarbazone COTI-2 is reported to promote refolding of mutant p53 and restore wild-type-p53 function. It is active against human tumour cell lines of various origins at nanomolar concentrations, induces cell death by apoptosis. COTI-2 is highly efficacious against multiple cancer cell lines from a broad range of human cancers both in vitro and in vivo. COTI-2 does not significantly inhibit over 200 kinases from major kinase pathways involved in cancer that were evaluated in both kinase assays and does not inhibit the ATPase activity of Hsp90, a ubiquitous molecular chaperone that plays an essential role in cell survival and cell cycle control. In vivo COTI-2 significantly inhibited tumor growth in the HT-29 human colorectal tumor xenografts at a dose of 10 mg/kg. COTI-2 also significantly inhibited tumor growth in the SHP-77 SCLC xenograft model at a dose as low as 3 mg/kg. Its treatment delays U87-MG, MDA-MB-231 and OVCAR-3 xenograft growth. COTI-2 treatment demonstrates a safe toxicity profile in vivo. COTI-2 selectively targets a wide variety of human cancer cell lines, as demonstrated by the in vitro data, while having little deleterious effects on normal cells. Cell Research(from reference) Cell lines：SHP-77 cells Concentrations：100, 250, 1000 nM Incubation Time：48 h

No numbering system information yet

No physical and chemical property information yet

No safety information yet

No production method and use information yet

No upstream information yet

No downstream information yet

No related product information yet