B02

Modify Date: 2024-01-05 09:49:29

B02 Structure
B02 structure
Common Name B02
CAS Number 1290541-46-6 Molecular Weight 339.39000
Density N/A Boiling Point N/A
Molecular Formula C22H17N3O Melting Point N/A
MSDS Chinese USA Flash Point N/A
Symbol GHS07
GHS07
Signal Word Warning

 Use of B02


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

 Names

Name (E)-3-benzyl-2-(2-(pyridin-3-yl)vinyl)quinazolin-4(3H)-one
Synonym More Synonyms

 B02 Biological Activity

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

[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.

 Chemical & Physical Properties

Molecular Formula C22H17N3O
Molecular Weight 339.39000
Exact Mass 339.13700
PSA 47.78000
LogP 4.01020
Storage condition -20℃

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
RIDADR NONH for all modes of transport

 Articles2

More Articles
A novel role for non-ubiquitinated FANCD2 in response to hydroxyurea-induced DNA damage.

Oncogene 35 , 22-34, (2016)

Fanconi anemia (FA) is a genetic disease of bone marrow failure, cancer susceptibility, and sensitivity to DNA crosslinking agents. FANCD2, the central protein of the FA pathway, is monoubiquitinated ...

Survival of the replication checkpoint deficient cells requires MUS81-RAD52 function.

PLoS Genet. 9 , e1003910, (2013)

In checkpoint-deficient cells, DNA double-strand breaks (DSBs) are produced during replication by the structure-specific endonuclease MUS81. The mechanism underlying MUS81-dependent cleavage, and the ...

 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
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