产品
编 号：F755089
分子式：C40H48NO11P
分子量：749.78
分子式：C40H48NO11P
分子量：749.78
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CAS No: 2734877-51-9
产品详情
生物活性：
Tubulin/MMP-IN-2 is dual inhibitor of tubulin and matrix metalloproteinases. Tubulin/MMP-IN-2 can strongly inhibit tubulin polymerization and induces cell apoptosis. Tubulin/MMP-IN-2 has inhibitory activities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively. Tubulin/MMP-IN-2 can be used for the research of cancer.
体内研究：
Tubulin/MMP-IN-2 (15, 30 mg/kg; every two days for three weeks) displays significant in vivo antitumor efficacy in A549 xenograft models without inducing apparent systemic toxicity.Animal Model:BALB/c nude mice
Dosage:15, 30 mg/kg
Administration:Every two days for three weeks
Result:Exhibited a dose-dependent inhibitory effect on tumor growth.Exhibited no obvious histopathological changes for the main organ tissues (e.g. heart, liver, spleen, lung and kidney).
体外研究：
Tubulin/MMP-IN-2 (Compound 9e) (0.01-20 μM; 24 h) has activity for HepG-2, HT29, A549, MGC-803 and LO2 cells with IC50 values of 0.36 μM, 0.31 μM, 0.19 μM, 0.42 μM and 10.45 μM, respectively.Tubulin/MMP-IN-2 has anti-proliferative activities for SK-OV-3, SK-OV-3/CDDP, MCF-7 and MCF-7/DOX cells with IC50 values of 0.32 μM, 0.39 μM, 0.27 μM and 0.25 μM, respectively.Tubulin/MMP-IN-2 has inhibitory activities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively.Tubulin/MMP-IN-2 (2.5, 5 Μm; 24 h) strongly inhibits tubulin polymerization, and induced cell apoptosis and cell cycle arrest in G2/M stage, remarkably displayed inhibition of cell migration against A549 cells in vitro.Tubulin/MMP-IN-2 (2.5, 5 Μm; 24 h) can induce apoptosis via mitochondria-dependent apoptosis pathway.Tubulin/MMP-IN-2 (2.5, 5 Μm; 24 h) can also cause ER stress demonstrating as up-regulation express of proteins (CHOP, p-elF2a, and p-PERK).
Tubulin/MMP-IN-2 is dual inhibitor of tubulin and matrix metalloproteinases. Tubulin/MMP-IN-2 can strongly inhibit tubulin polymerization and induces cell apoptosis. Tubulin/MMP-IN-2 has inhibitory activities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively. Tubulin/MMP-IN-2 can be used for the research of cancer.
体内研究：
Tubulin/MMP-IN-2 (15, 30 mg/kg; every two days for three weeks) displays significant in vivo antitumor efficacy in A549 xenograft models without inducing apparent systemic toxicity.Animal Model:BALB/c nude mice
Dosage:15, 30 mg/kg
Administration:Every two days for three weeks
Result:Exhibited a dose-dependent inhibitory effect on tumor growth.Exhibited no obvious histopathological changes for the main organ tissues (e.g. heart, liver, spleen, lung and kidney).
体外研究：
Tubulin/MMP-IN-2 (Compound 9e) (0.01-20 μM; 24 h) has activity for HepG-2, HT29, A549, MGC-803 and LO2 cells with IC50 values of 0.36 μM, 0.31 μM, 0.19 μM, 0.42 μM and 10.45 μM, respectively.Tubulin/MMP-IN-2 has anti-proliferative activities for SK-OV-3, SK-OV-3/CDDP, MCF-7 and MCF-7/DOX cells with IC50 values of 0.32 μM, 0.39 μM, 0.27 μM and 0.25 μM, respectively.Tubulin/MMP-IN-2 has inhibitory activities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively.Tubulin/MMP-IN-2 (2.5, 5 Μm; 24 h) strongly inhibits tubulin polymerization, and induced cell apoptosis and cell cycle arrest in G2/M stage, remarkably displayed inhibition of cell migration against A549 cells in vitro.Tubulin/MMP-IN-2 (2.5, 5 Μm; 24 h) can induce apoptosis via mitochondria-dependent apoptosis pathway.Tubulin/MMP-IN-2 (2.5, 5 Μm; 24 h) can also cause ER stress demonstrating as up-regulation express of proteins (CHOP, p-elF2a, and p-PERK).
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