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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERAD51 Inhibitor B02Cat. No.: HY-101462CAS No.: 1290541-46-6Synonyms: B02分式: CHNO分量: 339.39作靶點: RAD51作通路: Cell Cycle/DNA Damage儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 37 mg/mL (109.0
2、2 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.9465 mL 14.7323 mL 29.4646 mL5 mM 0.5893 mL 2.9465 mL 5.8929 mL10 mM 0.2946 mL 1.4732 mL 2.9465 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑配制儲備液,并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?,配制前請先配制澄清的儲備液,再依次添加助溶?為保證實驗結(jié)果的可靠
3、性,體內(nèi)實驗的作液,建議您現(xiàn)現(xiàn)配,當(dāng)天使;澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占):1. 請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2 mg/mL (5.89 mM); Clear solution2. 請依序添加每種溶劑: 10% DMSO 90% corn oilSolubility: 2 mg/mL (5.89 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBI
4、OLOGICAL ACTIVITY物活性 RAD51 Inhibitor B02 (B02)RAD51的抑制劑,IC50值為27.4 M。IC50 & Target IC50: 27.4 M (hRAD51) 1體外研究 RAD51 Inhibitor B02 specifically inhibits human RAD51 (IC50=27.4 M), but not its E. coli homologue RecA(IC50250 M) 1. The combination of B02 with cisplatin has the strongest killing effect
5、on the human breastcancer cells MDA-MB-231 2.體內(nèi)研究 B02 significantly enhances the therapeutic effect of cisplatin on tumor cells in vivo. B02 is tolerated by miceat doses up to 50 mg/kg without obvious body weight loss. No inhibition of tumor growth is observed on micesolely treated by B02. Mice trea
6、ted 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.PROTOCOLCell Assay 2 The cells are exposed for 1 h, then the cells are ished by PBS three times and refreshed by the medi
7、acontaining B02 (5 M). 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.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Cisplatin and B02 are
8、 dissolved in NS and cremophor/DMSO/NS (1:1:3) vehicle, respectively,Administration 2 immediately before injection. In a combination treatment group, the mice are injected with B02 (50 mg/kg orindicated otherwise) and cisplatin (4 mg/kg or indicated otherwise). In B02 group, mice are injected with B
9、02and NS; in cisplatin group, mice are injected with cisplatin and B02 vehicle. Cisplatin (or NS) is administrated3 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.MCE has not independently confi
10、rmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Mol Med (Berl). 2019 Jun 14.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Huang F, et al. Identification of specific inhibitors of human RAD51 recombinase using high-throughput screening. ACS Chem Biol. 2011Jun 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 mousexenografts. PLoS One. 2014 Jun 27;9(6):e100993.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMcePdfHeightCaution: Product has not be
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