APE1-IN-1|cas:524708-03-0|西域试剂

APE1-IN-1,99.0%

产品编号：Bellancom-136731| CAS NO：524708-03-0| 分子式：C₁₉H₂₁N₃OS₂| 分子量：371.52

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货号	价格	库存与货期
Bellancom-136731	￥1250.00	杭州北京（现货）
Bellancom-136731	￥2000.00	杭州北京（现货）
Bellancom-136731	￥6000.00	杭州北京（现货）

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APE1-IN-1

产品介绍

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 (HY-17364) 对癌细胞的细胞毒性。

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay

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 (HY-17364) (1 mM) with optimal synergy occurring at ~5 μM and ~10 μM, respectively.

体内研究
(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

西域 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.

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.

	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

西域 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.

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.

	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

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 22 mg/mL (59.22 mM; ultrasonic and warming and heat to 80°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6916 mL	13.4582 mL	26.9165 mL
5 mM	0.5383 mL	2.6916 mL	5.3833 mL
10 mM	0.2692 mL	1.3458 mL	2.6916 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式