COTI-2

1039455-84-9

C19H22N6S

H2O : < 0.1 mg/mL (insoluble); DMSO : 6.67 mg/mL (18.20 mM; Need ultrasonic)

Apoptosis

COTI-2 is a small molecule candidate anti-cancer drug which can convert mutant p53 to wild-type conformation. IC50 & Target: p53^[1] In Vitro: COTI-2 efficiently inhibits the proliferation rate of all the tested cell lines following 72 h of treatment. COTI-2 is significantly effective at inhibiting tumor cell proliferation in all three cell lines (COLO-205, HCT-15, and SW620). Relatively low concentrations of COTI-2 are active against all human glioblastoma cell lines tested (U87-MG, SNB-19, SF-268, and SF-295). COTI-2 treatment of SHP-77 cells with approximate IC₅₀ concentrations results in the induction of early apoptosis among 40 to 47% of total cells^[2]. In Vivo: COTI-2 significantly inhibits tumor growth in the HT-29 human colorectal tumor xenografts at a dose of 10 mg/kg. In addition to reducing tumor volumes at specific times post-treatment, COTI-2 also delays the time required for tumors to reach specified volumes. COTI-2 also significantly inhibits tumor growth in the SHP-77 SCLC xenograft model at a dose as low as 3 mg/kg. COTI-2 treatment both reduces U87-MG tumor volumes at specific times post-treatment and lengthens the time required for U87-MG xenografts to grow in nude mice. Control tumors in mice treated with vehicle alone take only 5 days to reach an average volume of 828 mm³ while tumors in animals treated with COTI-2 take double that time (10 days) to reach a similar mean volume (857 mm³). COTI-2 treatment effectively inhibits OVCAR-3 xenograft growth regardless of the route of administration^[2].