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编 号：F756080
分子式：C20H16Cl2N2O5
分子量：435.26
分子式：C20H16Cl2N2O5
分子量：435.26
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CAS No: 2804026-81-9
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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.
体内研究：
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。Animal Model:Five-week-old female athymic nude mice injected with MCF-7 cells
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.
体外研究：
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。Tubulin polymerization-IN-41（compoundC3；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。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。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。MCF-7 cells5 nM, 10 nM, 20 nM24 hMCF-7 cells5 nM, 10 nM, 20 nM24 h
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.
体内研究：
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。Animal Model:Five-week-old female athymic nude mice injected with MCF-7 cells
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.
体外研究：
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。Tubulin polymerization-IN-41（compoundC3；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。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。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。MCF-7 cells5 nM, 10 nM, 20 nM24 hMCF-7 cells5 nM, 10 nM, 20 nM24 h
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