PARP1-IN-5 是一种低毒、具有口服活性、有效的和有选择性的PARP-1抑制剂 (IC50=14.7 nM)。PARP1-IN-5 可用于癌症研究。
| 生物活性 | PARP1-IN-5 is a low toxicity, orally active, potent and selectivePARP-1inhibitor (IC50=14.7 nM). PARP1-IN-5 can be used for the research ofcancer[1]. |
| IC50& Target[1] | PARP-1 14.7 nM (IC50) | PARP-2 0.9 μM (IC50) |
|
体外研究
(In Vitro) | PARP1-IN-5 (0.1~10 μM; A549 cells) can significantly increase the cytotoxicity of CBP on A549 cells in a dose-dependent manner. PARP1-IN-5 (0.1~10 μM; SK-OV-3 cells) decreases the expressions of MCM2-7. PARP1-IN-5 (0.1~320 μM; A549 cells) has little cytotoxic effects on A549 cells. PARP1-IN-5 (SK-OV-3 cells) can significantly decrease the PAR level[1].
PARP1-IN-5 exerts antitumor effects through PARP-1. PARP1-IN-5 could increase the γ-H2AX expression[1].
|
体内研究
(In Vivo) | PARP1-IN-5 (1000 mg/kg; p.o.) shows that there is no significant difference in the body weight and blood routine[1].
PARP1-IN-5 (25 and 50 mg/kg; p.o.; 12 days) significantly enhances the inhibitory effect of carboplatin on A549 cells at 50 mg/kg[1].
PARP1-IN-5 (50 mg/kg; p.o.) positively correlates with the expression of PARP-1[1].
PARP1-IN-5 can upregulate the expression of γ-H2AX and decrease the expression of PAR[1].
| Animal Model: | Mice[1] | | Dosage: | 1000 mg/kg | | Administration: | P.o. | | Result: | There was no significant difference in the body weight and blood routine. |
| Animal Model: | Mice[1] | | Dosage: | 25 and 50 mg/kg | | Administration: | P.o.; 12 days | | Result: | Significantly enhanced the inhibitory effect of CBP on A549 cells at 50 mg/kg. |
| Animal Model: | Male Sprague–Dawley (SD) rats[1] | | Dosage: | 50 mg/kg (Pharmacokinetic Analysis) | | Administration: | P.o.; 12 days | | Result: | Positively correlated with the expression of PARP-1. |
|
| 分子量 | |
| Formula | |
| 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. |
