1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. Microtubule/Tubulin Apoptosis
  3. Tubulin polymerization-IN-41

Tubulin polymerization-IN-41 是一种有效的微管蛋白聚合 (tubulin polymerization) 抑制剂,IC50 为 2.61 μM。Tubulin polymerization-IN-41 靶向微管蛋白的秋水仙碱结合位点。Tubulin polymerization-IN-41 具有抗癌作用。

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Tubulin polymerization-IN-41 Chemical Structure

Tubulin polymerization-IN-41 Chemical Structure

CAS No. : 2804026-81-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tubulin polymerization-IN-41 is a potent tubulin polymerization inhibitor with the IC50 of 2.61 μM. Tubulin polymerization-IN-41 targets the Colchicine-binding site of tubulin. Tubulin polymerization-IN-41 has anticancer effects[1].

体外研究
(In Vitro)

Tubulin polymerization-IN-41 (compound C3) 表现出显着的抗增殖活性,对 K562、MCF-7、HT29 和 HCT116 细胞的 IC50 值分别为 6.3 nM、9.2 nM、8.3 nM 和 8.7 nM。此外,Tubulin polymerization-IN-41 对紫杉醇耐药的 MCF-7 细胞和 A549 细胞显示出显着的活性[1]
Tubulin polymerization-IN-41(compound C3;5-20 nM)以浓度依赖方式下调乙酰-α-微管蛋白(Ac-α-微管蛋白)的表达并上调脱酪氨酸-α-微管蛋白(DeY-α-微管蛋白)的表达[1]
Tubulin polymerization-IN-41 (compound C3; 5-20 nM; 24 h) 可将癌细胞阻滞在 G2/M ,并呈浓度依赖性诱导 MCF-7 细胞凋亡[1]
Tubulin polymerization-IN-41(compound C3;5-20 nM;24 小时)减少 Ser216 磷酸化,导致 cdc2 Tyr15 去磷酸化和 Thr161 磷酸化,最终导致后续 cdc2/cyclin B1 复合物的激活[1]
MCF-7 cells 5 nM, 10 nM, 20 nM 24 h MCF-7 cells 5 nM, 10 nM, 20 nM 24 h

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 5 nM, 10 nM, 20 nM
Incubation Time: 24 h
Result: Could arrest cancer cells in the G2/M phase.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 5 nM, 10 nM, 20 nM
Incubation Time: 24 h
Result: Induced MCF-7 cells apoptosis.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 5 nM, 10 nM, 20 nM
Incubation Time: 24 h
Result: Induced cdc25c activation.
体内研究
(In Vivo)

Tubulin polymerization-IN-41(compound C3;5-20 mg/kg;i.p;每两天一次;连续 21 天)在药物处理期间表现出显着的剂量依赖性肿瘤生长抑制效力,且体重没有减轻< sup>[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Five-week-old female athymic nude mice injected with MCF-7 cells[1]
Dosage: 5, 10, and 20 mg/kg
Administration: Intraperitoneal injection; every two days; for 21 consecutive days
Result: Exhibited the significant potency of tumor growth inhibition in a dose dependence without weight loss in the drug-treated period.
分子量

435.26

Formula

C20H16Cl2N2O5

CAS 号
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.

纯度 & 产品资料
参考文献

Tubulin polymerization-IN-41 相关分类

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