产品
编 号：F753373
分子式：C15H9F5N2O3
分子量：360.24
分子式：C15H9F5N2O3
分子量：360.24
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CAS No: 2494082-34-5
产品详情
生物活性：
PTG-0861 is a selective histone deacetylase 6 (HDAC6) inhibitor with the IC50 value of 5.92 nM. PTG-0861 induces apoptosis and can be used in the study of acute myeloid leukemia, multiple myeloma and other hematological cancers.
体内研究：
PTG-0861 (compound 54) (oral administration, 20 mg/kg, everyday, 5 days) has no effect on weight and no obvious toxicity in CD1 mice.Animal Model:CD1 mice
Dosage:20 mg/kg
Administration:Oral administration; everyday; 5 days
Result:No weight loss in mice and no obvious toxicity.
Animal Model:Male CD1 mice
Dosage:20 mg/kg
Administration:Intraperitoneal injection; once
Result:The pharmacokinetic parameters of PTG-0861 in vivo ParameterPTG-0861
half-life0.25 h
Cmax526 ng/mL
AUClast190 h?ng/mL
AUCinf219 h?ng/mL
AUC Extr(%)0.324
MRT(h)0.350
AUC/D(h?mg/mL)9.5
体外研究：
PTG-0861 (compound 54) (0.1-5 μM, 6 hours) stimulates the expression of acetylated a-tubulin and has inhibitory activity against HDAC6 with the IC50 value of 0.59 μM.PTG-0861 (compound 54) (0-4 μM, 18 hours) can induce apoptosis in a dose-dependent manner and has some cytotoxic effect.
PTG-0861 is a selective histone deacetylase 6 (HDAC6) inhibitor with the IC50 value of 5.92 nM. PTG-0861 induces apoptosis and can be used in the study of acute myeloid leukemia, multiple myeloma and other hematological cancers.
体内研究：
PTG-0861 (compound 54) (oral administration, 20 mg/kg, everyday, 5 days) has no effect on weight and no obvious toxicity in CD1 mice.Animal Model:CD1 mice
Dosage:20 mg/kg
Administration:Oral administration; everyday; 5 days
Result:No weight loss in mice and no obvious toxicity.
Animal Model:Male CD1 mice
Dosage:20 mg/kg
Administration:Intraperitoneal injection; once
Result:The pharmacokinetic parameters of PTG-0861 in vivo ParameterPTG-0861
half-life0.25 h
Cmax526 ng/mL
AUClast190 h?ng/mL
AUCinf219 h?ng/mL
AUC Extr(%)0.324
MRT(h)0.350
AUC/D(h?mg/mL)9.5
体外研究：
PTG-0861 (compound 54) (0.1-5 μM, 6 hours) stimulates the expression of acetylated a-tubulin and has inhibitory activity against HDAC6 with the IC50 value of 0.59 μM.PTG-0861 (compound 54) (0-4 μM, 18 hours) can induce apoptosis in a dose-dependent manner and has some cytotoxic effect.
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