1290541-46-6
1290541-46-6 structure
- Name: B02
- Chemical Name: (E)-3-benzyl-2-(2-(pyridin-3-yl)vinyl)quinazolin-4(3H)-one
- CAS Number: 1290541-46-6
- Molecular Formula: C22H17N3O
- Molecular Weight: 339.39000
- Catalog: Signaling Pathways Cell Cycle/DNA Damage RAD51
- Create Date: 2016-04-22 09:46:54
- Modify Date: 2024-01-05 09:49:29
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RAD51 Inhibitor B02 (B02) is an inhibitor of human RAD51 with an IC50 of 27.4 μM.
| Name | (E)-3-benzyl-2-(2-(pyridin-3-yl)vinyl)quinazolin-4(3H)-one |
|---|---|
| Synonyms |
(E)-3-BENZYL-2-(2-(PYRIDIN-3-YL)VINYL)QUINAZOLIN-4(3H)-ONE
3-(Phenylmethyl)-2-[(1E)-2-(3-pyridinyl)ethenyl]-4(3H)-quinazolinone RAD51 inhibitor B02 B02 |
| Description | RAD51 Inhibitor B02 (B02) is an inhibitor of human RAD51 with an IC50 of 27.4 μM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 27.4 μM (hRAD51)[1] |
| 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]. |
| 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]. |
| Cell Assay | 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 Admin | 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 |
| Molecular Formula | C22H17N3O |
|---|---|
| Molecular Weight | 339.39000 |
| Exact Mass | 339.13700 |
| PSA | 47.78000 |
| LogP | 4.01020 |
| Storage condition | -20℃ |
