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编 号:F752529
分子式:C15H15ClN2O2
分子量:290.74
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生物活性:
Tubulin polymerization-IN-14 (Compound 20a) is a tubulin polymerization inhibitor with an IC50 of 3.15 μM. Tubulin polymerization-IN-14 shows potent anti-vascular and anticancer activities, induces cancer cell apoptosis.

体内研究:
Tubulin polymerization-IN-14 (Compound 20a) (15 and 30 mg/kg; i.v.; daily for 21 days) displays obvious and dose-dependent antitumor effect with no significant toxicity in the liver tumor allograft mouse model.Animal Model:Five-week-old male ICR mice, liver tumor allograft model
Dosage:15 and 30 mg/kg
Administration:Intravenous injection, daily for 21 days
Result:The decrease in tumor weight reached 68.7% at doses of 30 mg/kg per day at 21 daysafter initiation of treatment as compared to vehicle without obvious loss of body weight.

体外研究:
Tubulin polymerization-IN-14 (Compound 20a) binds to the colchicine binding site on tubulin.Tubulin polymerization-IN-14 (0-1 μM; 72 h) inhibits cancer cell growth.Tubulin polymerization-IN-14 (5-20 nM; 48 h) arrests K562 cell cycle at G2/M phase, significantly induces cell apoptosis in K562 cells in a concentration-dependent manner, and induces mitochondrial membrane potential (MMP) collapse and mitochondrial dysfunction in K562 cells.Tubulin polymerization-IN-14 (5-20 nM; 24 h) significantly decreases wound closure and capillary-like tubules formation in a concentration-dependent manner in HUVECs.
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