MPT0B014

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

MPT0B014 是一种微管蛋白聚合 (tubulin polymerization) 抑制剂。MPT0B014 诱导癌细胞凋亡 (apoptosis)。MPT0B014 可用于癌症研究。

MPT0B014 is a tubulin polymerization inhibitor. MPT0B014 induces cancer cell apoptosis. MPT0B014 can be used for the research of cancer.

Cell Viability Assay Cell Line:A549, H1299, H226 and HUVEC cells Concentration:0, 0.025, 0.05, 0.075 and 1 μM Incubation Time:48 h Result:Inhibited cell viability with IC50s of 0.109±0.01, 0.055±0.004, 0.077±0.005 and 0.536±0.166 μM against A549, H1299, H226 and HUVEC cells, respectively.Cell Cycle Analysis Cell Line:A549, H1299 and H226 Concentration:0.05, 0.1 and 0.3 μM Incubation Time:24 and 48 h Result:Treatment for 24 h led to notable accumulation of cells in the G2/M phase. At 48 h, sub-G1 apoptotic cell populations were increased in a concentration-dependent manner. Cells in the G2/M phase began to rise at 12 h post-treatment and peaked at 24 h. Following this, there was an emergence of cells in the sub-G1 population phase until 48 h.Western Blot Analysis Cell Line:A549, H1299 and H226 Concentration:0.05, 0.1 and 0.3 μM Incubation Time:24 h Result:Resulted in a marked increase in expression of the mitosis marker MPM2 and the proteins cyclin B1, Cdc2, Thr161, Aurora A and Aurora B in a concentration-dependent manner. Decreased the expression of Cdc (Tyr15) and Cdc25C, whereas total protein levels of Cdc2 did not change.Apoptosis Analysis Cell Line:A549 Concentration:0.05, 0.075, 0.1 and 0.3 μM Incubation Time:48 h Result:Induced apoptosis in a concentration-dependent manner.Western Blot Analysis Cell Line:A549 Concentration:0.05, 0.1 and 0.3 μM Incubation Time:24, 36 and 48 h Result:Induced activation of caspases-3, -7, -8 and -9, and cleavage of PARP in a time- and concentration-dependent manner. Significantly induced Bcl-2 phosphorylation. Down-regulated Mcl-1 expression in a concentration-dependent manner.

Animal Model:Nude athymic mice, A549 xenograftsDosage:100 mg/kg alone or in combination with 25 mg/kg Erlotinib (HY-50896) Administration:i.v./i.p., daily for 25 days Result:The combined treatment resulted in more significant tumor growth delay (28%) compared with treatment alone (7%). The combination produced significantly higher anti-tumor activity. The growth of A549 cancer cell xenografts was suppressed by 11, 21 and 49% (tumor growth inhibition) after treatment with MPT0B014, Erlotinib and MPT0B014 plus Erlotinib, respectively.

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Others

Other Targets

Microtubule Associated

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1215208-59-5

323.34

C19H17NO4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (154.64 mM; 超声助溶 )

COc1cc(cc(OC)c1OC)C(=O)c1ccc2ncccc2c1

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(-20℃)

With Ice Pack

≥ 2 years