APE1-IN-1 是一种有效且具有血脑屏障透过性的无嘌呤/嘧啶内切酶 1 (APE1) 抑制剂，IC50为 2 μM。APE1-IN-1 可增强烷基化剂甲基甲烷磺酸盐 (Methylmethane sulfonate) 和Temozolomide 对癌细胞的细胞毒性。

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 [1].

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) [1]. 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 [1]. APE1-IN-1 (5-30 μM; 24 h) exhibits cytotoxic activity against HeLa cells, and potentiates the activity of methyl methansulfonate and Temozolomide [1]. Cell Cytotoxicity Assay [1] Cell 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.

APE1-IN-1 (30 mpk; IP; single dosage) exhibits favorable pharmacokinetic property [1]. Pharmacokinetic Parameters of APE1-IN-1 (compound 3) (IP; 30 mpk) in CD1 mice [1]. 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 Animal Model: CD1 male mice (n = 3) [1] 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.

524708-03-0

C19H21N3OS2

371.52

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years