产品
编 号：F756268
分子式：C21H21ClN2O4
分子量：400.86
分子式：C21H21ClN2O4
分子量：400.86
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CAS No: 2835559-00-5
产品详情
生物活性：
Tubulin polymerization-IN-4 is a potent tubulin polymerization inhibitor with IC50 value of 4.6 μM. Tubulin polymerization-IN-4 can disrupt tubulin polymerization and vasculature, arrest the cell cycle at the G2/M phase, induce apoptosis, and suppress clonogenesis and migration in HeLa cells. Tubulin polymerization-IN-4 can be used for researching cervical cancer.
体内研究：
Tubulin polymerization-IN-4 (100-1000 mg/kg; IP, single) exhibits extremely low toxicity with LD50 over 1000 mg/kg.Tubulin polymerization-IN-4 (30 and 60 mg/kg; IP; daily for 21 days) inhibits the tumor growth, with TGI of 35% and 58% at dosing 30 and 60 mg/kg.Tubulin polymerization-IN-4 (30 mg/kg; IP; single) presents the modest pharmacokinetic properties.Pharmacokinetic Parameters of Tubulin polymerization-IN-4 in ICR mice.IP (30 mg/kg)
T1/2 (h)1.56 ± 0.28
Tmax (h)0.25
Cmax (μg/L)6215 ± 308
AUC0-t (μg/L·h)5609 ± 347
AUC0-∞ (μg/L·h)5940 ± 347
VZ/F (L/kg)11.35 ± 1.29
CLZ/F (L/h/kg)5.05 ± 0.91
MRT (h)1.77 ± 0.43
体外研究：
Tubulin polymerization-IN-4 (compound 9j) (0-1 μM; 48 hours) exhibits sub-micromolar inhibitory activities against HeLa, SiHa and MS751.Tubulin polymerization-IN-4 (3, 6 and 12.5 μM; 0-20 min) inhibits tubulin polymerization in a concentration-dependent manner with the inhibition percentages of 39%, 54%, and 77% at 3, 6 and 12.5 μM.Tubulin polymerization-IN-4 (1-100 μM; 2 hours) inhibits the formation of EBI-β-tubulin adduct in a concentration-dependent manner.Tubulin polymerization-IN-4 (0.2 μM; 1 and 2 hours) disrupts the HUVEC-formed vascular tube.Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) increases cell distribution to the G2/M phase in a concentration-dependent manner.Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) induces apoptosis of HeLa cells.Tubulin polymerization-IN-4 (20, 50, 100 nM; 14 days) reduces new colony formation and suppresses HeLa cell growth for 14 days in a dose-dependent manner.Tubulin polymerization-IN-4 (0.1, 0.2 and 0.4 μM; 24 hours) effectively inhibits the migration of HeLa cells in a concentration-dependent manner.Tubulin polymerization-IN-4 (0-200 μM; 24 hours) exhibits good renal safety profile, with IC50 of 188 ± 16 μM in HK-2 cells.
Tubulin polymerization-IN-4 is a potent tubulin polymerization inhibitor with IC50 value of 4.6 μM. Tubulin polymerization-IN-4 can disrupt tubulin polymerization and vasculature, arrest the cell cycle at the G2/M phase, induce apoptosis, and suppress clonogenesis and migration in HeLa cells. Tubulin polymerization-IN-4 can be used for researching cervical cancer.
体内研究：
Tubulin polymerization-IN-4 (100-1000 mg/kg; IP, single) exhibits extremely low toxicity with LD50 over 1000 mg/kg.Tubulin polymerization-IN-4 (30 and 60 mg/kg; IP; daily for 21 days) inhibits the tumor growth, with TGI of 35% and 58% at dosing 30 and 60 mg/kg.Tubulin polymerization-IN-4 (30 mg/kg; IP; single) presents the modest pharmacokinetic properties.Pharmacokinetic Parameters of Tubulin polymerization-IN-4 in ICR mice.IP (30 mg/kg)
T1/2 (h)1.56 ± 0.28
Tmax (h)0.25
Cmax (μg/L)6215 ± 308
AUC0-t (μg/L·h)5609 ± 347
AUC0-∞ (μg/L·h)5940 ± 347
VZ/F (L/kg)11.35 ± 1.29
CLZ/F (L/h/kg)5.05 ± 0.91
MRT (h)1.77 ± 0.43
体外研究：
Tubulin polymerization-IN-4 (compound 9j) (0-1 μM; 48 hours) exhibits sub-micromolar inhibitory activities against HeLa, SiHa and MS751.Tubulin polymerization-IN-4 (3, 6 and 12.5 μM; 0-20 min) inhibits tubulin polymerization in a concentration-dependent manner with the inhibition percentages of 39%, 54%, and 77% at 3, 6 and 12.5 μM.Tubulin polymerization-IN-4 (1-100 μM; 2 hours) inhibits the formation of EBI-β-tubulin adduct in a concentration-dependent manner.Tubulin polymerization-IN-4 (0.2 μM; 1 and 2 hours) disrupts the HUVEC-formed vascular tube.Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) increases cell distribution to the G2/M phase in a concentration-dependent manner.Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) induces apoptosis of HeLa cells.Tubulin polymerization-IN-4 (20, 50, 100 nM; 14 days) reduces new colony formation and suppresses HeLa cell growth for 14 days in a dose-dependent manner.Tubulin polymerization-IN-4 (0.1, 0.2 and 0.4 μM; 24 hours) effectively inhibits the migration of HeLa cells in a concentration-dependent manner.Tubulin polymerization-IN-4 (0-200 μM; 24 hours) exhibits good renal safety profile, with IC50 of 188 ± 16 μM in HK-2 cells.
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