产品
编 号：F572246
分子式：C19H21N3OS2
分子量：371.52
分子式：C19H21N3OS2
分子量：371.52
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
结构图
CAS No: 524708-03-0
产品详情
生物活性：
APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells.
体内研究：
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.PlasmaBrain
t1/2 (h)2.11
brain/plasma21
Cmax (μM)16217
tmax (h)0.250.25
CLogP2.83
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.
体外研究：
APE1-IN-1 (compound 3) exhibits an IC50 of 2 μM in the qHTS assay and an IC50 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 (HY-17364).
APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells.
体内研究：
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.PlasmaBrain
t1/2 (h)2.11
brain/plasma21
Cmax (μM)16217
tmax (h)0.250.25
CLogP2.83
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.
体外研究：
APE1-IN-1 (compound 3) exhibits an IC50 of 2 μM in the qHTS assay and an IC50 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 (HY-17364).
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