COTI-2

• CAT Number: I006193
• CAS Number: 1039455-84-9
• Molecular Formula: C19H22N6S
• Molecular Weight: 366.5
• Purity: ≥95%
• Synonyms: COTI-2; COTI2; COTI 2;(E)-N/’-(6,7-dihydroquinolin-8(5H)-ylidene)-4-(pyridin-2-yl)piperazine-1-carbothiohydrazide
• Target: p53
• Solubility: Soluble in DMSO
• Storage: Store at -20°C
• IUPAC Name: N-(6,7-dihydro-5H-quinolin-8-ylideneamino)-4-pyridin-2-ylpiperazine-1-carbothioamide
• InChI: 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+
• InChIKey: UTDAKQMBNSHJJB-JWGURIENSA-N
• SMILES: S=C(N/N=C1C(N=CC=C2)=C2CCC1)N(CC3)CCN3C4=NC=CC=C4

COTI-2 (Cat.No:I006193) is an investigational anticancer drug with promising potential. It targets mutant p53, a common genetic alteration in various cancers, to restore normal function and inhibit tumor growth. Preclinical studies have shown encouraging results, highlighting COTI-2 as a potential therapeutic option for patients with p53-mutated cancers. Clinical trials are underway to evaluate its efficacy and safety in humans.

Reference

1:Oncotarget. 2016 Jul 5;7(27):41363-41379. doi: 10.18632/oncotarget.9133. COTI-2, a novel small molecule that is active against multiple human cancer cell lines in vitro and in vivo.Salim KY,Maleki Vareki S,Danter WR,Koropatnick J, PMID: 27150056 PMCID: PMC5173065 DOI: 10.18632/oncotarget.9133 Abstract: Identification of novel anti-cancer compounds with high efficacy and low toxicity is critical in drug development. High-throughput screening and other such strategies are generally resource-intensive. Therefore, in silico computer-aided drug design has gained rapid acceptance and popularity. We employed our proprietary computational platform (CHEMSAS®), which uses a unique combination of traditional and modern pharmacology principles, statistical modeling, medicinal chemistry, and machine-learning technologies to discover and optimize novel compounds that could target various cancers. COTI-2 is a small molecule candidate anti-cancer drug identified using CHEMSAS. This study describes the in vitro and in vivo evaluation of COTI-2. Our data demonstrate that COTI-2 is effective against a diverse group of human cancer cell lines regardless of their tissue of origin or genetic makeup. Most treated cancer cell lines were sensitive to COTI-2 at nanomolar concentrations. When compared to traditional chemotherapy or targeted-therapy agents, COTI-2 showed superior activity against tumor cells, in vitro and in vivo. Despite its potent anti-tumor efficacy, COTI-2 was safe and well-tolerated in vivo. Although the mechanism of action of COTI-2 is still under investigation, preliminary results indicate that it is not a traditional kinase or an Hsp90 inhibitor.