Microtubule inhibitor 2

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Microtubule inhibitor 2 

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

Microtubule inhibitor 2

Microtubule inhibitor 2 Chemical Structure

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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[1].

体外研究
(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 µM for A549, Hela, A2780, HCT-8, MCF-7 cells, respectively[1].
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)[1].
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)[1].
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[1].
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[1].
Microtubule inhibitor 2 triggers cell death through ferroptosis rather than apoptosis[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: A549, Hela, A2780, HCT-8, MCF-7 cells
Concentration:
Incubation Time: 48 h
Result: Showed antiproliferative activities 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.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 5, 10, 20 nM
Incubation Time: 24 h, 48 h
Result: Arrested cell cycle progression at the G2/M phase in a dose and time-dependent manner.

体内研究
(In Vivo)

Microtubule inhibitor 2 (10 mg/kg; p.o.)displays excellent oral bioavailability (F% = 69.45) [1].
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%[1].
Pharmacokinetic Parameters of Microtubule inhibitor 2 in Male Institute of Cancer Research (ICR) mice (18−23 g)[1].

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 –

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Institute of Cancer Research (ICR) mice (18−23 g) [1]
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) [1]
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%.

分子量

389.40

Formula

C20H23NO7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Zhou J, et al. Discovery of a Novel Stilbene Derivative as a Microtubule Targeting Agent Capable of Inducing Cell Ferroptosis. J Med Chem. 2022; 65(6):4687-4708.

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