CAS NO: | 1039455-84-9 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | COTI-2, an anti-cancer drug with low toxicity, is an orally available third generation activator ofp53 mutantforms. COTI-2 acts both by reactivating mutant p53 and inhibiting thePI3K/AKT/mTORpathway. COTI-2 inducesapoptosisin multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation[1][2][3]. | ||||||||||||||||
IC50& Target | p53[1] | ||||||||||||||||
体外研究 (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 IC50concentrations results in the induction of early apoptosis among 40 to 47% of total cells[2]. | ||||||||||||||||
体内研究 (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 mm3while 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]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 366.48 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C19H22N6S | ||||||||||||||||
CAS 号 | 1039455-84-9 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 5 mg/mL(13.64 mM;Need ultrasonic) 配制储备液
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