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[1].
in vivo
PARP1-IN-5 dihydrochloride (1000 mg/kg; p.o.) shows that there is no significant difference in the body weight and blood routine[1].
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[1].
PARP1-IN-5 dihydrochloride (50 mg/kg; p.o.) positively correlates with the expression of PARP-1[1].
PARP1-IN-5 dihydrochloride 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 SpragueDawley (SD) rats[1]
Dosage:
50 mg/kg (Pharmacokinetic Analysis)
Administration:
P.o.
Result:
Positively correlated with the expression of PARP-1.
IC 50
PARP-1: 14.7 nM (IC50); PARP-2: 0.9 μM (IC50)
References
[1] Long H, et al. Discovery of Novel Apigenin-Piperazine Hybrids as Potent and Selective Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors for the Treatment of Cancer. J Med Chem. 2021;64(16):12089-12108. DOI:10.1021/acs.jmedchem.1c00735
