RAD51 Inhibitor B02
(Synonyms: B02) 目录号 : GC19306
A RAD51 inhibitor
Cas No.:1290541-46-6
Sample solution is provided at 25 µL, 10mM.
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RAD51 Inhibitor B02 (B02) is an inhibitor of human RAD51 with an IC50 of 27.4 uM.
RAD51 Inhibitor B02 specifically inhibits human RAD51 (IC50=27.4 uM), but not its E. coli homologue RecA (IC50>250 uM)[1]. The combination of B02 with cisplatin has the strongest killing effect on the human breast cancer cells MDA-MB-231[2].
B02 significantly enhances the therapeutic effect of cisplatin on tumor cells in vivo. B02 is tolerated by mice at doses up to 50 mg/kg without obvious body weight loss. No inhibition of tumor growth is observed on mice solely treated by B02. Mice treated with 4 mg/kg cisplatin, however, shows a 33% inhibition of tumor growth. Finally, mice treated with 50 mg/kg B02 and 4 mg/kg cisplatin shows a 66% inhibition of tumor growth[2].
References:
[1]. Huang F, et al. Identification of specific inhibitors of human RAD51 recombinase using high-throughput screening. ACS Chem Biol. 2011 Jun 17;6(6):628-35.
[2]. Huang F, et al. A small molecule inhibitor of human RAD51 potentiates breast cancer cell killing by therapeutic agents in mouse xenografts. PLoS One. 2014 Jun 27;9(6):e100993.
Cell experiment: | The cells are exposed for 1 h, then the cells are ished by PBS three times and refreshed by the media containing B02 (5 µM). After 7-10 days, cells are fixed and stained with staining solution (0.05% crystal violet, 50% methanol in PBS); finally cell colonies are counted[2]. |
Animal experiment: | Mice: Cisplatin and B02 are dissolved in NS and cremophor/DMSO/NS (1:1:3) vehicle, respectively, immediately before injection. In a combination treatment group, the mice are injected with B02 (50 mg/kg or indicated otherwise) and cisplatin (4 mg/kg or indicated otherwise). In B02 group, mice are injected with B02 and NS; in cisplatin group, mice are injected with cisplatin and B02 vehicle. Cisplatin (or NS) is administrated 3 h after B02 (or its vehicle) injection. All the treatments are executed through I.P. injections on day 11, 13, 15 and 17 after tumor cells inoculations[2]. |
References: [1]. Huang F, et al. Identification of specific inhibitors of human RAD51 recombinase using high-throughput screening. ACS Chem Biol. 2011 Jun 17;6(6):628-35. | |
| Cas No. | 1290541-46-6 | SDF | |
| 别名 | B02 | ||
| Canonical SMILES | O=C1N(CC2=CC=CC=C2)C(/C=C/C3=CC=CN=C3)=NC4=C1C=CC=C4 | ||
| 分子式 | C22H17N3O | 分子量 | 339.39 |
| 溶解度 | DMSO : ≥ 37 mg/mL (109.02 mM) | 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 | 2.9465 mL | 14.7323 mL | 29.4646 mL |
| 5 mM | 0.5893 mL | 2.9465 mL | 5.8929 mL |
| 10 mM | 0.2946 mL | 1.4732 mL | 2.9465 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。
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet