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| Cas No.: | 1290541-46-6 |
| Chemical Name: | RAD51 inhibitor B02 |
| Synonyms: | RAD51 inhibitor B02;(E)-3-benzyl-2-(2-(pyridin-3-yl)vinyl)quinazolin-4(3H)-one;B02;3-(Phenylmethyl)-2-[(1E)-2-(3-pyridinyl)ethenyl]-4(3H)-quinazolinone;BO 2;MLS000709026;3-benzyl-2-[(E)-2-pyridin-3-ylethenyl]quinazolin-4-one;SMR000289793;3-Benzyl-2-[(E)-2-(3-pyridinyl)ethenyl]-4(3H)-quinazolinone;RAD51 Inhibitor B02; BO2;BDBM48804;cid_5738263;HMS2612I15;BCP19688;s8434;STK856883;B- |
| SMILES: | O=C1C2=C([H])C([H])=C([H])C([H])=C2N=C(/C(/[H])=C(\[H])/C2=C([H])N=C([H])C([H])=C2[H])N1C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H] |
| Formula: | C22H17N3O |
| M.Wt: | 339.3899 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | B02 is a cell-permeable pyridinylvinyl-quinazolinone compound that is shown to specifically inhibit human RAD51 (IC50 = 27.4 µM). Does not affect RecA even at much higher concentration (~250 µM). Directly interacts with RAD51 (Kd = 5.6 µM), and disrupts its binding to DNA and nucleoprotein filament formation. Blocks double-strand break-induced homologous recombination and enhances sensitivity of cells to Cisplatin and Mitomycin C . Diminishes co-aggregate formation between RAD51-ssDNA filament. |
| In Vivo: | 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]. |
| In Vitro: | 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]. |
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| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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