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编 号：F754828
分子式：C30H38N2O5
分子量：506.63
分子式：C30H38N2O5
分子量：506.63
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CAS No: 2709103-20-6
产品详情
生物活性：
HDAC6-IN-4 (C10) is a potent, orally active and highly selective HDAC6 inhibitor with an IC50 value of 23 nM. HDAC6-IN-4 induces cancer cells apoptosis and shows significant antitumor efficacy, without obvious toxicity.
体内研究：
HDAC6-IN-4 (C10) (0-100 mg/kg; i.g.; once daily for 21 days) shows excellent antitumor activity and significantly promoted T cell response in a dose-dependent manner, with no obvious toxicity.Animal Model:Five-week-old C57BL/6 mice (immune-related CT26 xenograft model).
Dosage:50 and 100 mg/kg
Administration:Oral gavage, once daily for 21 days
Result:Resulted in a substantial tumor growth and tumor tissue size inhibition in a dose-dependent way. Showed significantly high antitumor activity (TGI = 75%) at 100 mg/kg. Raised the plasma IFN-g level and the numbers of CD+ and CD3+CD+ (activated cytotoxic T) cells. Decreased CD4+CD25+CD127low/- T regulatory cells. Showed no obvious toxicity.
体外研究：
HDAC6-IN-4 (C10) (0-50 μM, 72 h) shows strong antiproliferative activity against different cancer cells with low cytotoxicity.HDAC6-IN-4 (0-6 μM, 24 h) exhibits significant selectivity for HDAC6 over HDAC1.HDAC6-IN-4 inhibits migration activity in a time-dependent and dose-dependent way in B16 and CT26 cells.HDAC6-IN-4 (0-8 μM, 24 h) induces B16 cell apoptosis in a dose-dependent manner.HDAC6-IN-4 exhibits significant plasma stability in humans (97% retention after 6 h), and exhibits significant metabolic stability in human (half-life of 101.91 min) and mouse liver (half-life of 67.94 min) microsomes.
HDAC6-IN-4 (C10) is a potent, orally active and highly selective HDAC6 inhibitor with an IC50 value of 23 nM. HDAC6-IN-4 induces cancer cells apoptosis and shows significant antitumor efficacy, without obvious toxicity.
体内研究：
HDAC6-IN-4 (C10) (0-100 mg/kg; i.g.; once daily for 21 days) shows excellent antitumor activity and significantly promoted T cell response in a dose-dependent manner, with no obvious toxicity.Animal Model:Five-week-old C57BL/6 mice (immune-related CT26 xenograft model).
Dosage:50 and 100 mg/kg
Administration:Oral gavage, once daily for 21 days
Result:Resulted in a substantial tumor growth and tumor tissue size inhibition in a dose-dependent way. Showed significantly high antitumor activity (TGI = 75%) at 100 mg/kg. Raised the plasma IFN-g level and the numbers of CD+ and CD3+CD+ (activated cytotoxic T) cells. Decreased CD4+CD25+CD127low/- T regulatory cells. Showed no obvious toxicity.
体外研究：
HDAC6-IN-4 (C10) (0-50 μM, 72 h) shows strong antiproliferative activity against different cancer cells with low cytotoxicity.HDAC6-IN-4 (0-6 μM, 24 h) exhibits significant selectivity for HDAC6 over HDAC1.HDAC6-IN-4 inhibits migration activity in a time-dependent and dose-dependent way in B16 and CT26 cells.HDAC6-IN-4 (0-8 μM, 24 h) induces B16 cell apoptosis in a dose-dependent manner.HDAC6-IN-4 exhibits significant plasma stability in humans (97% retention after 6 h), and exhibits significant metabolic stability in human (half-life of 101.91 min) and mouse liver (half-life of 67.94 min) microsomes.
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