产品
编 号：F752350
分子式：C21H18N4O3
分子量：374.39
分子式：C21H18N4O3
分子量：374.39
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CAS No: 2413587-26-3
产品详情
生物活性：
Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond interaction with HDAC8. Tubulin/HDAC-IN-1 inhibits tubulin polymerization and selectively inhibits HDAC8 (IC50: 150 nM). Tubulin/HDAC-IN-1 has cytotoxicity against various human cancer cells, also arrests cell cycle in the G2/M phase and induces cell apoptosis. Tubulin/HDAC-IN-1 can be used in the research of hematologic and solid tumors such as neuroblastoma, leukemia.
体内研究：
Tubulin/HDAC-IN-1 (Compound 12a, intratumoral injection, 0.25 mg/kg, three times a week for two weeks) decreases MCA205 tumor growth and extends the overall survival of treated mice in allogeneic sarcoma mice model.Animal Model:Allogeneic sarcoma model in C57BL/6 mice
Dosage:0.1, 0.25, 0.50 mg/kg, three times a week for two weeks.
Administration:Intratumoral injection
Result:Decreased tumor growth and extended the overall survival of treated mice with no obvious side effects.
体外研究：
Tubulin/HDAC-IN-1 (Compound 12a, 72 h) shows cytotoxicity against various human cancer cell lines with an averaged IC50 value of 0.6 nM.Tubulin/HDAC-IN-1 (2 nM, 24 h) induces HT29 cell cycle arrest in the G2/M phase and produces caspase-induced apoptosis of HT29 cells through mitochondrial dysfunction.Tubulin/HDAC-IN-1 selectively inhibits HDAC8 (IC50: 150 nM), inhibits HDAC6 and HDAC11 with IC 50 values of 1 μM and 1.9 μM respectively.Tubulin/HDAC-IN-1 (0.5-100 nM, 24 h/30 min) dose-dependently increases γH2AX level and acetylated SMC3 in HT-29 cells.Tubulin/HDAC-IN-1 (5-15 μΜ, 0-40 min) inhibits tubulin polymerization in a dose-dependent manner, with a maximal effect achieved at 10 μM.Tubulin/HDAC-IN-1 (250 nM, 30 min) depolymerizes the cell microtubule network, and the effect is not specific.Tubulin/HDAC-IN-1 shows good in vitro metabolic stability expressed by the intrinsic clearance CLint (given in μL/min/mg protein) using rat liver microsomes (RLM) and human liver microsomes (HLM).CompoundRLM RLM HLM HLM
t1/2 (h) CLint t1/2 CLint
Tubulin/HDAC-IN-16.61.75320.36
Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond interaction with HDAC8. Tubulin/HDAC-IN-1 inhibits tubulin polymerization and selectively inhibits HDAC8 (IC50: 150 nM). Tubulin/HDAC-IN-1 has cytotoxicity against various human cancer cells, also arrests cell cycle in the G2/M phase and induces cell apoptosis. Tubulin/HDAC-IN-1 can be used in the research of hematologic and solid tumors such as neuroblastoma, leukemia.
体内研究：
Tubulin/HDAC-IN-1 (Compound 12a, intratumoral injection, 0.25 mg/kg, three times a week for two weeks) decreases MCA205 tumor growth and extends the overall survival of treated mice in allogeneic sarcoma mice model.Animal Model:Allogeneic sarcoma model in C57BL/6 mice
Dosage:0.1, 0.25, 0.50 mg/kg, three times a week for two weeks.
Administration:Intratumoral injection
Result:Decreased tumor growth and extended the overall survival of treated mice with no obvious side effects.
体外研究：
Tubulin/HDAC-IN-1 (Compound 12a, 72 h) shows cytotoxicity against various human cancer cell lines with an averaged IC50 value of 0.6 nM.Tubulin/HDAC-IN-1 (2 nM, 24 h) induces HT29 cell cycle arrest in the G2/M phase and produces caspase-induced apoptosis of HT29 cells through mitochondrial dysfunction.Tubulin/HDAC-IN-1 selectively inhibits HDAC8 (IC50: 150 nM), inhibits HDAC6 and HDAC11 with IC 50 values of 1 μM and 1.9 μM respectively.Tubulin/HDAC-IN-1 (0.5-100 nM, 24 h/30 min) dose-dependently increases γH2AX level and acetylated SMC3 in HT-29 cells.Tubulin/HDAC-IN-1 (5-15 μΜ, 0-40 min) inhibits tubulin polymerization in a dose-dependent manner, with a maximal effect achieved at 10 μM.Tubulin/HDAC-IN-1 (250 nM, 30 min) depolymerizes the cell microtubule network, and the effect is not specific.Tubulin/HDAC-IN-1 shows good in vitro metabolic stability expressed by the intrinsic clearance CLint (given in μL/min/mg protein) using rat liver microsomes (RLM) and human liver microsomes (HLM).CompoundRLM RLM HLM HLM
t1/2 (h) CLint t1/2 CLint
Tubulin/HDAC-IN-16.61.75320.36
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