化合物 PTG-0861 T61337

Product Introduction
Bioactivity


英文名: PTG-0861

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

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途