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Microtubule inhibitor 2
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Microtubule inhibitor 2
MCE 站:Microtubule inhibitor 2
产品活性:Microtubule inhibitor 2 是一种有效的、选择性的、具有口服活性的 microtubule 抑制剂。Microtubule inhibitor 2 通过铁死亡 ferroptosis 触发细胞死亡。 Microtubule inhibitor 2 显示出抗肿瘤活性
研究领域:Cytoskeleton | Cell Cycle/DNA Damage | Apoptosis
作用靶点:Microtubule/Tubulin | Ferroptosis
In Vitro: Microtubule inhibitor 2 (compound 33) (48 h) shows antiproliferative activity with IC50 values of 0.01, 0.02, 0.02, 0.04, 0.05 M 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 M 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 tubulinmicrotubule 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.
In Vivo: 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 (1823 g).
p.o. | i.v. | |
dose (mg/kg) | 10 | 1 |
T1/2 (h) | 2.12 | 0.62 |
Tmax (h) | 0.25 | 0.08 |
Tmax (ng/mL) | 776.31 | 871.40 |
AUC(0-t) (h ng-1 mL) | 2432.04 | 350.19 |
AUC(0-∞) (h ng-1 mL) | 2463.76 | 353.02 |
MRT (h) | 2.57 | 0.68 |
CL (mL h-1 kg-1) | - | 2855.67 |
F % | 69.45 | - |
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