产品
编 号：F752254
分子式：C26H22O8
分子量：462.45
分子式：C26H22O8
分子量：462.45
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CAS No: 2411697-71-5
产品详情
生物活性：
Tubulin inhibitor 25 is a potent tubulin inhibitor with an IC50 value of 0.98 μM. Tubulin inhibitor 25 exhibits remarkable activity against cancer cell line HT29. Tubulin inhibitor 25 displays the potent inhibition on cell migration and tube formation that contributes to the anti-angiogenesis.
体内研究：
Tubulin inhibitor 25 (1.5 mg/kg; IV; single) exhibits good metabolic stability.Pharmacokinetic Parameters of Tubulin inhibitor 25 in male Sprague-Dawley rats.IV (1.5 mg/kg)
T1/2 (h)3.81 ± 2.14
MRT0-∞ (h)5.12 ± 2.86
AUC0-∞ (ng/mL·h)2156.12 ± 851.88
VZ (L/kg)3.348 ± 0.734
Animal Model:SD rats
Dosage:1.5 mg/kg
Administration:IV; single (Pharmacokinetic Analysis)
Result:Exhibited good metabolic stability.
体外研究：
Tubulin inhibitor 25 (compound 6c) (0-100 μM; 48 hours) exhibits high antiproliferative activity against tested cancer cell lines.Tubulin inhibitor 25 (0-200 μM; 48 hours) exhibits low cytotoxicity in normal cell lines.Tubulin inhibitor 25 (0.05, 0.1 and 0.2 μM; 24 hours) inhibits the colony formation of HT29 cells in a dose-dependent manner.Tubulin inhibitor 25 (2 and 4 μM) can inhibit the tubulin polymerization and compete with colchicine binding site.Tubulin inhibitor 25 (0.25-1 μM; 12-48 hours) arrests the cell cycle at G2/M phase and induces HT29 cells apoptosis in a dose- and time-dependent manner, besides induces HT29 cell depolarized mitochondria in the process of apoptosis.Tubulin inhibitor 25 (0.25-1 μM; 24 hours) increases the expression of P21 and Cyclin B1 and decreases the expression of Cdc2, p-CDC2 and p-Cdc25c; as well as induces the microtubule collapse in HT29 cells in a dose-dependent manner.Tubulin inhibitor 25 (0.01, 0.02 and 0.04 μM; 6 hours) effectively inhibits the HUVEC tube formation in a dose-dependent manner.Tubulin inhibitor 25 (0.1, 0.2 and 0.4 μM; 24 hours) inhibits migration of A549 cells in a dose-dependent manner.
Tubulin inhibitor 25 is a potent tubulin inhibitor with an IC50 value of 0.98 μM. Tubulin inhibitor 25 exhibits remarkable activity against cancer cell line HT29. Tubulin inhibitor 25 displays the potent inhibition on cell migration and tube formation that contributes to the anti-angiogenesis.
体内研究：
Tubulin inhibitor 25 (1.5 mg/kg; IV; single) exhibits good metabolic stability.Pharmacokinetic Parameters of Tubulin inhibitor 25 in male Sprague-Dawley rats.IV (1.5 mg/kg)
T1/2 (h)3.81 ± 2.14
MRT0-∞ (h)5.12 ± 2.86
AUC0-∞ (ng/mL·h)2156.12 ± 851.88
VZ (L/kg)3.348 ± 0.734
Animal Model:SD rats
Dosage:1.5 mg/kg
Administration:IV; single (Pharmacokinetic Analysis)
Result:Exhibited good metabolic stability.
体外研究：
Tubulin inhibitor 25 (compound 6c) (0-100 μM; 48 hours) exhibits high antiproliferative activity against tested cancer cell lines.Tubulin inhibitor 25 (0-200 μM; 48 hours) exhibits low cytotoxicity in normal cell lines.Tubulin inhibitor 25 (0.05, 0.1 and 0.2 μM; 24 hours) inhibits the colony formation of HT29 cells in a dose-dependent manner.Tubulin inhibitor 25 (2 and 4 μM) can inhibit the tubulin polymerization and compete with colchicine binding site.Tubulin inhibitor 25 (0.25-1 μM; 12-48 hours) arrests the cell cycle at G2/M phase and induces HT29 cells apoptosis in a dose- and time-dependent manner, besides induces HT29 cell depolarized mitochondria in the process of apoptosis.Tubulin inhibitor 25 (0.25-1 μM; 24 hours) increases the expression of P21 and Cyclin B1 and decreases the expression of Cdc2, p-CDC2 and p-Cdc25c; as well as induces the microtubule collapse in HT29 cells in a dose-dependent manner.Tubulin inhibitor 25 (0.01, 0.02 and 0.04 μM; 6 hours) effectively inhibits the HUVEC tube formation in a dose-dependent manner.Tubulin inhibitor 25 (0.1, 0.2 and 0.4 μM; 24 hours) inhibits migration of A549 cells in a dose-dependent manner.
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