MPT0B014

MPT0B014 is a tubulin polymerization inhibitor. MPT0B014 induces cancer cell apoptosis. MPT0B014 can be used for the research of cancer[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

Tubulin polymerization[1]

MPT0B014 (0-1 μM; 48 h) 以剂量依赖的方式抑制 A549、H1299 和 H226 细胞的生长[1]。 MPT0B014 (0.05-0.3 μM; 24 and 48 h) 在 A549 细胞中使细胞周期阻滞于 G2/M 期和 sub-G1 期，诱导细胞凋亡[1]。 Cell Viability Assay[1] 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[1] 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[1] 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[1] 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[1] 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.

MPT0B014 (100 mg/kg; i.v./i.p.; daily for 25 days) 和 25 mg/kg Erlotinib (HY-50896) 联用显著改善小鼠 A549 肿瘤抑制[1]。 Animal Model: Nude athymic mice, A549 xenografts[1] Dosage: 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.

[1]. Tsai AC, et al. In vitro and in vivo anti-tumour effects of MPT0B014, a novel derivative aroylquinoline, and in combination with erlotinib in human non-small-cell lung cancer cells. Br J Pharmacol. 2014 Jan;171(1):122-33.