Tubulin inhibitor 11

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tubulin inhibitor 11 是一种有效的具有口服活性的微管蛋白 (tubulin) 抑制剂。Tubulin inhibitor 11 靶向微管蛋白上的秋水仙碱结合位点，抑制微管蛋白聚合，促进有丝分裂阻断和细胞凋亡 (apoptosis)。

Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis.

Tubulin inhibitor 11 (Compound 48; 0.03-0.1 μM; 12 hours) causes cell cycle arrest at G2/M phase. Tubulin inhibitor 11 reduces cdc2 phosphorylation and increases cyclin B1 and phosphorylation of histone H3 at Ser10 in cells.Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM; 48 hours) causes cancer cell apoptosis.Tubulin inhibitor 11 (Compound 48) demonstrates favorable antiproliferative activities in DU145 cells with an IC50 of 8 nM.Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM) significantly reduces the expression levels of acetyl-α-tubulin and α-tubulin in a dose-dependent manner.Cell Cycle Analysis Cell Line:DU145 cells Concentration:0.01 μM, 0.03 μM, and 0.1 μM Incubation Time:12 hours Result:Caused cell cycle arrest at G2/M phase.Apoptosis Analysis Cell Line:DU145 cells Concentration:0.03 μM, 0.1 μM, and 0.3 μM Incubation Time:48 hours Result: Induced cancer cell apoptosis.Western Blot Analysis Cell Line:DU145 cells Concentration:0.01 μM, 0.03 μM, and 0.1 μM Incubation Time:12 hours Result:Reduced cdc2 phosphorylation and increased cyclin B1 and phosphorylation of histone H3 at Ser10 in cells.

Tubulin inhibitor 11 (Compound 48; 5-10 mg/kg; p.o; once daily) shows robust in vivo antitumor efficacies.Animal Model:Male athymic BALB/c nude mice (18-20 g) injected with DU145, NCI-H1299 or A549R cells Dosage:5 mg/kg, 10 mg/kg Administration:p.o; once dailyResult:Effectively suppressed tumor growth.

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Others

Other Targets

Microtubule Associated | Apoptosis

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2366260-33-3

409.5

C22H23N3O3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (244.20 mM; 超声助溶 )

N(S(=O)(=O)C1=CC=C(C)C=C1)C2=CC(C(NCC=3C=CC(C)=NC3)=O)=CC=C2C

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(-20℃)

With Ice Pack

≥ 2 years