PTG-0861 是一种选择性的组蛋白去乙酰酶 (HDAC6) 抑制剂，其IC50值为 5.92 nM。PTG-0861 可诱导细胞凋亡 (apoptosis)，用于急性髓性白血病、多发性骨髓瘤等血液癌症相关疾病的研究。
| 生物活性 | PTG-0861 is a selective histone deacetylase 6 (HDAC6) inhibitor with theIC50value of 5.92 nM. PTG-0861 inducesapoptosisand can be used in the study of acute myeloid leukemia, multiple myeloma and other hematological cancers[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | 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 IC50value 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 IC50value 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 | |
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体内研究
(In Vivo) | 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 | | Cmax | 526 ng/mL | | AUClast | 190 h*ng/mL | | AUCinf | 219 h*ng/mL | | AUC Extr(%) | 0.324 | | MRT(h) | 0.350 | | AUC/D(h*mg/mL) | 9.5 | |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
