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Microtubule inhibitor 2
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Microtubule inhibitor 2图片
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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
生物活性

Microtubule inhibitor 2 is a potent and selective, orally activemicrotubuleinhibitor. Microtubule inhibitor 2 triggers cell death throughferroptosis. Microtubule inhibitor 2 shows antitumor activity[1].

体外研究
(In Vitro)

Microtubule inhibitor 2 (compound 33) (48 h) shows antiproliferative activity with IC50values 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].

Cell Proliferation Assay[1]

Cell Line:A549, Hela, A2780, HCT-8, MCF-7 cells
Concentration:
Incubation Time:48 h
Result:Showed antiproliferative activities with IC50values 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)101
T1/2(h)2.120.62
Tmax(h)0.250.08
Tmax(ng/mL)776.31871.40
AUC(0-t)(h ng-1mL)2432.04350.19
AUC(0-∞)(h ng-1mL)2463.76353.02
MRT (h)2.570.68
CL (mL h-1kg-1)-2855.67
F %69.45-

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.