MPT0B014 6-(3′,4′,5′-Trimethoxybenzoylquinoline)|cas:1215208-59-5|西域试剂

MPT0B014 6-(3′,4′,5′-Trimethoxybenzoylquinoline),99.67%

产品编号：Bellancom-120786| CAS NO：1215208-59-5| 分子式：C₁₉H₁₇NO₄| 分子量：323.34

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货号	价格	库存与货期
Bellancom-120786	￥650.00	杭州北京（现货）
Bellancom-120786	￥1100.00	杭州北京（现货）
Bellancom-120786	￥2300.00	杭州北京（现货）
Bellancom-120786	￥3900.00	杭州北京（现货）
Bellancom-120786	￥6500.00	杭州北京（现货）

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产品介绍

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。

生物活性

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

体外研究

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。
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。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

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。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude athymic mice, A549 xenografts
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.

体内研究

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。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude athymic mice, A549 xenografts
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.

体内研究

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。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude athymic mice, A549 xenografts
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.