PARP1-IN-5 dihydrochloride?

Research use only, not for human use.

PARP1-IN-5 dihydrochloride is an orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.

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.

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.

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.

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Cell Cycle/DNA Damage

PARP

PARP

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2823308-89-8

537.46

C25H26Cl2N2O5S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (232.58 mM; Ultrasonic )H2O : 1 mg/mL (1.86 mM; Ultrasonic (<60°C)

O=C1C=C(C2=CC=C(O)C=C2)OC3=C(CN4CCN(CC5=CC=CS5)CC4)C(O)=CC(O)=C31.Cl[H].Cl[H]

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(-20℃)

With Ice Pack

≥ 2 years