APE1-IN-1
目录号 : GC67876APE1-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。
Cas No.:524708-03-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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 to cancer cells[1].
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)[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 | |
| t1/2 (h) | 2.1 | 1 |
| brain/plasma | 21 | |
| Cmax (μM) | 16 | 217 |
| tmax (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. |
[1]. Rai G, et al. Synthesis, biological evaluation, and structure-activity relationships of a novel class of apurinic/apyrimidinic endonuclease 1 inhibitors. J Med Chem. 2012 Apr 12;55(7):3101-12.
| Cas No. | 524708-03-0 | SDF | Download SDF |
| 分子式 | C19H21N3OS2 | 分子量 | 371.52 |
| 溶解度 | 储存条件 | Store at -20°C | |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。