产品
编 号：F755105
分子式：C25H24N2O5S
分子量：464.53
分子式：C25H24N2O5S
分子量：464.53
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CAS No: 2735645-53-9
产品详情
生物活性：
PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer.
体内研究：
PARP1-IN-5 (1000 mg/kg; p.o.) shows that there is no significant difference in the body weight and blood routine.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.PARP1-IN-5 (50 mg/kg; p.o.) positively correlates with the expression of PARP-1.PARP1-IN-5 can upregulate the expression of γ-H2AX and decrease the expression of PAR.Animal Model:Mice
Dosage:1000 mg/kg
Administration:P.o.
Result:There was no significant difference in the body weight and blood routine.
Animal Model:Mice
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
Dosage:50 mg/kg (Pharmacokinetic Analysis)
Administration:P.o.; 12 days
Result:Positively correlated with the expression of PARP-1.
体外研究：
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.PARP1-IN-5 exerts antitumor effects through PARP-1. PARP1-IN-5 could increase the γ-H2AX expression.
PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer.
体内研究：
PARP1-IN-5 (1000 mg/kg; p.o.) shows that there is no significant difference in the body weight and blood routine.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.PARP1-IN-5 (50 mg/kg; p.o.) positively correlates with the expression of PARP-1.PARP1-IN-5 can upregulate the expression of γ-H2AX and decrease the expression of PAR.Animal Model:Mice
Dosage:1000 mg/kg
Administration:P.o.
Result:There was no significant difference in the body weight and blood routine.
Animal Model:Mice
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
Dosage:50 mg/kg (Pharmacokinetic Analysis)
Administration:P.o.; 12 days
Result:Positively correlated with the expression of PARP-1.
体外研究：
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.PARP1-IN-5 exerts antitumor effects through PARP-1. PARP1-IN-5 could increase the γ-H2AX expression.
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