RAD51 Inhibitor B02

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

Product information

CAS Number: 1290541-46-6

Molecular Weight: 339.39

Formula: C22H17N3O

Synonym:

B02

Chemical Name: 3-benzyl-2-[(E)-2-(pyridin-3-yl)ethenyl]-3, 4-dihydroquinazolin-4-one

Smiles: O=C1C2=CC=CC=C2N=C(/C=C/C2=CN=CC=C2)N1CC1C=CC=CC=1

InChiKey: GEKDQXSPTHHANP-OUKQBFOZSA-N

InChi: InChI=1S/C22H17N3O/c26-22-19-10-4-5-11-20(19)24-21(13-12-17-9-6-14-23-15-17)25(22)16-18-7-2-1-3-8-18/h1-15H,16H2/b13-12+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 37 mg/mL (109.02 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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

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.

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.

Products are for research use only. Not for human use.