PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.
IC50&Target
PARP-1
14.7 nM (IC50)
PARP-2
0.9 μM (IC50)
体外研究
PARP1-IN-5 dihydrochloride (0.1~10 μM; A549 cells) can significantly increase the cytotoxicity of CBP on A549 cells in a dose-dependent manner. PARP1-IN-5 dihydrochloride (0.1~10 μM; SK-OV-3 cells) decreases the expressions of MCM2-7. PARP1-IN-5 dihydrochloride (0.1~320 μM; A549 cells) has little cytotoxic effects on A549 cells. PARP1-IN-5 dihydrochloride (SK-OV-3 cells) can significantly decrease the PAR level.
PARP1-IN-5 dihydrochloride exerts antitumor effects through PARP-1. PARP1-IN-5 dihydrochloride could increase the γ-H2AX expression.
体内研究
PARP1-IN-5 dihydrochloride (1000 mg/kg; p.o.) shows that there is no significant difference in the body weight and blood routine.
PARP1-IN-5 dihydrochloride (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 dihydrochloride (50 mg/kg; p.o.) positively correlates with the expression of PARP-1.
PARP1-IN-5 dihydrochloride 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.
Result:
Positively correlated with the expression of PARP-1.
运输条件
Room temperature in continental US; may vary elsewhere.