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编 号：F763008
分子式：C20H23NO7
分子量：389.4
分子式：C20H23NO7
分子量：389.4
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CAS No: 3031328-45-4
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生物活性：
Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity.
体内研究：
Microtubule inhibitor 2 (10 mg/kg; p.o.)displays excellent oral bioavailability (F% = 69.45) .Microtubule inhibitor 2 (10 mg/kg; i.p.; every other day for 22 days) shows antitumor activity and the level of tumor growth inhibition was 78.63%.Pharmacokinetic Parameters of Microtubule inhibitor 2 in Male Institute of Cancer Research (ICR) mice (18?23 g).p.o. i.v.
dose (mg/kg)101
T1/2 (h)2.120.62
Tmax (h)0.250.08
Tmax (ng/mL)776.31871.40
AUC(0-t) (h ng-1 mL)2432.04350.19
AUC(0-∞) (h ng-1 mL)2463.76353.02
MRT (h)2.570.68
CL (mL h-1 kg-1)-2855.67
F %69.45-
Animal Model:Male Institute of Cancer Research (ICR) mice (18?23 g)
Dosage:10 mg/kg
Administration:
Result:Displayed excellent oral bioavailability (F% = 69.45).
Animal Model: Male BALB/c nude mice (5 weeks old, 18?20 g) (A549 xenograft models)
Dosage:10 mg/kg
Administration:i.p.; every other day, 22 days
Result:Showed antitumor activity and the level of tumor growth inhibition was 78.63%.
体外研究：
Microtubule inhibitor 2 (compound 33) (48 h) shows antiproliferative activity with IC50 values of 0.01, 0.02, 0.02, 0.04, 0.05 μM for A549, Hela, A2780, HCT-8, MCF-7 cells, respectively.Microtubule inhibitor 2 shows selective toward normal human cells and cancer cells (IC50s of 0.01, 0.04, 1.45, 1.32,0.54 μM for A549, quiescent HUVECs, LO2, HLF, MCF-10A cells, respectively).Microtubule inhibitor 2 (48 h) shows antiproliferative activity toward drug-resistant cancer cells (IC50s of 0.02, 0.07, 0.04 for A549/ADM, HCT-8/VCR, A2780/TAX cells, respectively).Microtubule inhibitor 2 (5, 10, 20 nM; 24 h) dramatically disrupts the dynamic balance of the tubulin?microtubule system, induces the multipolarization of the mitotic spindle, and interfered with the mitosis of A549 cells.Microtubule inhibitor 2 (5, 10, 20 nM, 24 h, 48 h) arrests cell cycle progression at the G2/M phase in a dose and time-dependent manner.Microtubule inhibitor 2 triggers cell death through ferroptosis rather than apoptosis.
Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity.
体内研究：
Microtubule inhibitor 2 (10 mg/kg; p.o.)displays excellent oral bioavailability (F% = 69.45) .Microtubule inhibitor 2 (10 mg/kg; i.p.; every other day for 22 days) shows antitumor activity and the level of tumor growth inhibition was 78.63%.Pharmacokinetic Parameters of Microtubule inhibitor 2 in Male Institute of Cancer Research (ICR) mice (18?23 g).p.o. i.v.
dose (mg/kg)101
T1/2 (h)2.120.62
Tmax (h)0.250.08
Tmax (ng/mL)776.31871.40
AUC(0-t) (h ng-1 mL)2432.04350.19
AUC(0-∞) (h ng-1 mL)2463.76353.02
MRT (h)2.570.68
CL (mL h-1 kg-1)-2855.67
F %69.45-
Animal Model:Male Institute of Cancer Research (ICR) mice (18?23 g)
Dosage:10 mg/kg
Administration:
Result:Displayed excellent oral bioavailability (F% = 69.45).
Animal Model: Male BALB/c nude mice (5 weeks old, 18?20 g) (A549 xenograft models)
Dosage:10 mg/kg
Administration:i.p.; every other day, 22 days
Result:Showed antitumor activity and the level of tumor growth inhibition was 78.63%.
体外研究：
Microtubule inhibitor 2 (compound 33) (48 h) shows antiproliferative activity with IC50 values of 0.01, 0.02, 0.02, 0.04, 0.05 μM for A549, Hela, A2780, HCT-8, MCF-7 cells, respectively.Microtubule inhibitor 2 shows selective toward normal human cells and cancer cells (IC50s of 0.01, 0.04, 1.45, 1.32,0.54 μM for A549, quiescent HUVECs, LO2, HLF, MCF-10A cells, respectively).Microtubule inhibitor 2 (48 h) shows antiproliferative activity toward drug-resistant cancer cells (IC50s of 0.02, 0.07, 0.04 for A549/ADM, HCT-8/VCR, A2780/TAX cells, respectively).Microtubule inhibitor 2 (5, 10, 20 nM; 24 h) dramatically disrupts the dynamic balance of the tubulin?microtubule system, induces the multipolarization of the mitotic spindle, and interfered with the mitosis of A549 cells.Microtubule inhibitor 2 (5, 10, 20 nM, 24 h, 48 h) arrests cell cycle progression at the G2/M phase in a dose and time-dependent manner.Microtubule inhibitor 2 triggers cell death through ferroptosis rather than apoptosis.
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