Microtubule inhibitor 2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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].

Shanghai Jinpan Biotech Co Ltd 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 –

Shanghai Jinpan Biotech Co Ltd 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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务