Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PTG-0861 is a highly specific inhibitor of histone deacetylase 6 (HDAC6), demonstrating an impressive IC50 value of 5.92 nm. This compound effectively triggers apoptosis and holds potential for research pertaining to acute myeloid leukemia, multiple myeloma, and other hematological cancers [1].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | PTG-0861 is a highly specific inhibitor of histone deacetylase 6 (HDAC6), demonstrating an impressive IC50 value of 5.92 nm. This compound effectively triggers apoptosis and holds potential for research pertaining to acute myeloid leukemia, multiple myeloma, and other hematological cancers [1]. |
体外活性 | 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 IC 50 value of 0.59 μM [1]. PTG-0861 (compound 54) (0-4 μM, 18 hours) can induce apoptosis in a dose-dependent manner and has some cytotoxic effect [1]. Western Blot Analysis [1] Cell Line: MV4-11 cells Concentration: 0.1-5 μM Incubation Time: 6 hours Result: Induced the accumulation of acetylated a-tubulin expression at 500 nM. Immunofluorescence [1] Cell Line: HeLa cells Concentration: 0-2 μM Incubation Time: 6 hours Result: Increased levels of acetylated a-tubulin at 0.1 μM. Apoptosis Analysis [1] Cell Line: MV4-11 cells Concentration: 0-4 μM Incubation Time: 18 hours Result: Induced about 18% cells late apoptosis at 4 μM while at low dose 0.25 μM only about 5%. Cell Cytotoxicity Assay [1] Cell Line: Hematological cancer cell lines MV4-11, MM.1S, and RPMI 8226 Concentration: 1.24-4.94 μM Incubation Time: 72 hours Result: Showed cytotoxic effects on MV4-11, MM.1S, and RPMI 8226 with the IC 50 value of 1.85 μM,1.9 μM,4.94 μM, respectively. Cell Line: Concentration: Incubation Time: Result: Result: The pharmacokinetic parameters of PTG-0861 in vitro Parameter PTG-0861 Percent Remaining (%) 0 min 100.00 Percent Remaining (%) 30 min 96.41 Percent Remaining (%) 60 min 97.98 Percent Remaining (%) 120 min 97.08 T1/2 (min) ∞ T1/2 (min) 50.85 ± 3.37 CLint (mL/min/106 cells) 27.32 ± 1.81 -Log Pe 5.66 ± 0.02 Papp (A-B) (10 6, cm/s) 1.33 ± 0.03 Papp (B-A) (10 6, cm/s) 0.94 ± 0.13 Efflux Ratio 0.71 ± 0.08 |
体内活性 | PTG-0861 (compound 54) (oral administration, 20 mg/kg, everyday, 5 days) has no effect on weight and no obvious toxicity in CD1 mice [1]. Animal Model: CD1 mice [1] 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 [1] Dosage: 20 mg/kg Administration: Intraperitoneal injection; once Result: The pharmacokinetic parameters of PTG-0861 in vivo Parameter PTG-0861 half-life 0.25 h C max 526 ng/mL AUC last 190 h ng/mL AUC inf 219 h ng/mL AUC Extr(%) 0.324 MRT(h) 0.350 AUC/D(h mg/mL) 9.5 |
分子量 | 360.24 |
分子式 | C15H9F5N2O3 |
CAS No. | 2494082-34-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PTG-0861 2494082-34-5 Inhibitor inhibitor inhibit