APE1-IN-1

APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 ( APE1 ) inhibitor with an IC 50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide to cancer cells In Vitro APE1-IN-1 (compound 3) exhibits an IC 50 of 2 μM in the qHTS assay and an IC 50 of 12 μM in a radiotracer incision assay (RIA). APE1-IN-1 (0, 1, 3, 10, 30, or 100 μM; 15 min) inhibits HeLa whole cell extract AP site incision in a dose-dependent manner. APE1-IN-1 (5-30 μM; 24 h) exhibits cytotoxic activity against HeLa cells, and potentiates the activity of methyl methansulfonate and Temozolomide . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cytotoxicity AssayCell Line: HeLa cells Concentration: 5-30 μM Incubation Time: 24 h Result: Exhibited cytotoxic activity against HeLa cells with a 50% reduction in cell viability occurring at ~15 μM. Greatly potentiated the activity of methyl methansulfonate (0.4 mM) and Temozolomide (1 mM) with optimal synergy occurring at ~5 μM and ~10 μM, respectively. In Vivo APE1-IN-1 (30 mpk; IP; single dosage) exhibits favorable pharmacokinetic property . Pharmacokinetic Parameters of APE1-IN-1 (compound 3) (IP; 30 mpk) in CD1 mice . Plasma Brain t 1/2 (h) 2.1 1 brain/plasma 21 C max (μM) 16 217 t max (h) 0.25 0.25 CLogP 2.83 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: CD1 male mice (n = 3) Dosage: 30 mpk Administration: IP; single dosage Result: Showed lipophilic (CLogP = 2.8), crossed the BBB quite readily, giving rise to a B/P ratio of 21. Form:Solid IC50& Target:IC 50 : 2 μM (APE1)

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