Antitumor agent-138

产品编号 T85704Cas号 2975168-22-8

别名

Antitumor agent-138 (compound 5b) 作为一种微管蛋白聚合抑制剂，主要针对tubulin的colchicine结合位点，其IC50值达到1.87 μM。该化合物能够在G2/M期阻止细胞周期的进展，并促使MCF-7细胞发生自噬 (apoptosis)。此外，Antitumor agent-138还能有效抑制细胞的迁移及血管形成。

Antitumor agent-138

产品编号 T85704Cas号 2975168-22-8

规格	价格	库存	数量
10 mg	询价	10-14周
50 mg	询价	10-14周

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产品介绍

生物活性

产品描述	Antitumor agent-138 (compound 5b), with an IC 50 of 1.87 μM, inhibits tubulin polymerization at the tubulin colchicine-binding sites. It arrests the cell cycle at the G2/M phase and induces apoptosis in MCF-7 cells. Additionally, this compound suppresses cell migration and angiogenesis [1].
体外活性	Antitumor agent-138在细胞MCF-7, A549, MDA-MB-231, HT-29, HeLa和L02中表现出抗增殖活性，IC50值分别是0.04, 0.39, 0.04, 0.06, 0.11和2.73 μM [1]。Antitumor agent-138 (5-20 nM)抑制人乳腺癌细胞MCF-7集落的形成[1]。Antitumor agent-138 (25-200 nM)诱导MCF-7中微管蛋白崩溃[1]。Antitumor agent-138 (6.25-50 nM)剂量依赖地抑制HUVEC细胞成管，抑制血管形成[1]。Cell Migration Assay [1] Cell Line: A549 Concentration: 6.25-50 nM Incubation Time: 24 h Result: Inhibited the cell migration in a dose-dependent manner. Cell Proliferation Assay [1] Cell Line: MCF-7, A549, MDA-MB-231, HT-29, HeLa and L02 Concentration: 0-5 μM Incubation Time: 48 h Result: Exhibited anti-proliferative properties in cancer cells MCF-7, A549, MDA-MB-231, HT-29, HeLa with low concentrations in nanomole. Western Blot Analysis [1] Cell Line: MCF-7 Concentration: 6.25-25 nM Incubation Time: 24 h Result: Increased P21, Cyclin B1, Cdc25c and cdk7 in a dose- and time-dependent manner. Increased Bax, Cleaved-PARP, Bim and Cleaved Caspase-9, decreasesd Bcl-2 in a dose- and time-dependent manner. Immunofluorescence [1] Cell Line: MCF-7 Concentration: 25-200 nM Incubation Time: 8 h Result: Disrupted the microtubule network into punctate.
体内活性	抗肿瘤剂-138 (20 mg/kg，腹腔注射，21天) 在MCF-7异种移植BALB/c裸鼠模型中表现出68.95%的肿瘤生长抑制率 [1]。