RAD51 Inhibitor B02 (B02) is an inhibitor of human RAD51 with an IC₅₀ of 27.4 μM.

IC50: 27.4 μM (hRAD51)^[1]

RAD51 Inhibitor B02 specifically inhibits human RAD51 (IC₅₀=27.4 μM), but not its E. coli homologue RecA (IC₅₀>250 μM)^[1]. The combination of B02 with cisplatin has the strongest killing effect on the human breast cancer cells MDA-MB-231^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

339.39

C₂₂H₁₇N₃O

1290541-46-6

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : ≥ 37 mg/mL (109.02 mM)

* “≥” means soluble, but saturation unknown.

*

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2 mg/mL (5.89 mM); Clear solution

  此方案可获得 ≥ 2 mg/mL (5.89 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2 mg/mL (5.89 mM); Clear solution

  此方案可获得 ≥ 2 mg/mL (5.89 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.