B02
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MedKoo CAT#: 530630

CAS#: 1290541-46-6

Description: B02, also known as RAD51-IN-02, is a RAD51 inhibitor. B02 can enhance DOX sensitivity of MM cells. Combining low-toxicity doses of DOX and B02 resulted in significant synthetic lethality, observed as increased apoptosis and reduced viability compared to either agent alone, or to the product of their individual effects.


Price and Availability

Size
Price

100mg
USD 750
1g
USD 2950
Size
Price

200mg
USD 1250
2g
USD 3950
Size
Price

500mg
USD 2150
5g
USD 5850

B02, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 530630
Name: B02
CAS#: 1290541-46-6
Chemical Formula: C22H17N3O
Exact Mass: 339.1372
Molecular Weight: 339.398
Elemental Analysis: C, 77.86; H, 5.05; N, 12.38; O, 4.71


Synonym: B02; B-02; B 02; RAD51-IN-02

IUPAC/Chemical Name: 3-Benzyl-2-[(E)-2-(3-pyridinyl)ethenyl]-4(3H)-quinazolinone

InChi Key: GEKDQXSPTHHANP-OUKQBFOZSA-N

InChi Code: 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+

SMILES Code: O=C1N(CC2=CC=CC=C2)C(/C=C/C3=CC=CN=C3)=NC4=C1C=CC=C4


Technical Data

Appearance:
Solid powder

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

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

high RAD51 expression in vivo is associated with chemoresistance and poor patient survival. specific inhibition of RAD51 may be an effective means to block DNA repair in MM cells and thus to enhance the efficacy of chemotherapy.


References

1: Alagpulinsa DA, Ayyadevara S, Shmookler Reis RJ. A Small-Molecule Inhibitor of RAD51 Reduces Homologous Recombination and Sensitizes Multiple Myeloma Cells to Doxorubicin. Front Oncol. 2014 Oct 30;4:289. doi: 10.3389/fonc.2014.00289. eCollection 2014. PubMed PMID: 25401086; PubMed Central PMCID: PMC4214226.

2: Bachelier R, Confavreux CB, Peyruchaud O, Croset M, Goehrig D, van der Pluijm G, Clézardin P. Combination of anti-angiogenic therapies reduces osteolysis and tumor burden in experimental breast cancer bone metastasis. Int J Cancer. 2014 Sep 15;135(6):1319-29. doi: 10.1002/ijc.28787. Epub 2014 Mar 3. PubMed PMID: 24615579.

3: Huang F, Mazin AV. 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. doi: 10.1371/journal.pone.0100993. eCollection 2014. PubMed PMID: 24971740; PubMed Central PMCID: PMC4074124.

4: Garcia T, Jackson A, Bachelier R, Clément-Lacroix P, Baron R, Clézardin P, Pujuguet P. A convenient clinically relevant model of human breast cancer bone metastasis. Clin Exp Metastasis. 2008;25(1):33-42. Epub 2007 Sep 28. PubMed PMID: 17902030.

5: Ma H, Takahashi A, Yoshida Y, Adachi A, Kanai T, Ohno T, Nakano T. Combining carbon ion irradiation and non-homologous end-joining repair inhibitor NU7026 efficiently kills cancer cells. Radiat Oncol. 2015 Nov 9;10:225. doi: 10.1186/s13014-015-0536-z. PubMed PMID: 26553138; PubMed Central PMCID: PMC4638098.

6: Takahashi A, Mori E, Nakagawa Y, Kajihara A, Kirita T, Pittman DL, Hasegawa M, Ohnishi T. Homologous recombination preferentially repairs heat-induced DNA double-strand breaks in mammalian cells. Int J Hyperthermia. 2016 Nov 13:1-7. [Epub ahead of print] PubMed PMID: 27776457.

7: David M, Sahay D, Mege F, Descotes F, Leblanc R, Ribeiro J, Clézardin P, Peyruchaud O. Identification of heparin-binding EGF-like growth factor (HB-EGF) as a biomarker for lysophosphatidic acid receptor type 1 (LPA1) activation in human breast and prostate cancers. PLoS One. 2014 May 14;9(5):e97771. doi: 10.1371/journal.pone.0097771. eCollection 2014. PubMed PMID: 24828490; PubMed Central PMCID: PMC4020852.

8: Bellahcène A, Bachelier R, Detry C, Lidereau R, Clézardin P, Castronovo V. Transcriptome analysis reveals an osteoblast-like phenotype for human osteotropic breast cancer cells. Breast Cancer Res Treat. 2007 Jan;101(2):135-48. Epub 2006 Oct 7. PubMed PMID: 17028989.

9: David M, Wannecq E, Descotes F, Jansen S, Deux B, Ribeiro J, Serre CM, Grès S, Bendriss-Vermare N, Bollen M, Saez S, Aoki J, Saulnier-Blache JS, Clézardin P, Peyruchaud O. Cancer cell expression of autotaxin controls bone metastasis formation in mouse through lysophosphatidic acid-dependent activation of osteoclasts. PLoS One. 2010 Mar 17;5(3):e9741. doi: 10.1371/journal.pone.0009741. PubMed PMID: 20305819; PubMed Central PMCID: PMC2840030.

10: Croset M, Goehrig D, Frackowiak A, Bonnelye E, Ansieau S, Puisieux A, Clézardin P. TWIST1 expression in breast cancer cells facilitates bone metastasis formation. J Bone Miner Res. 2014 Aug;29(8):1886-99. doi: 10.1002/jbmr.2215. PubMed PMID: 24619707.

11: Nissen MD, Marshall HS, Richmond PC, Jiang Q, Harris SL, Jones TR, Jansen KU, Perez JL. A randomized, controlled, phase 1/2 trial of a Neisseria meningitidis serogroup B bivalent rLP2086 vaccine in healthy children and adolescents. Pediatr Infect Dis J. 2013 Apr;32(4):364-71. doi: 10.1097/INF.0b013e31827b0d24. PubMed PMID: 23114369.

12: Kischel P, Bellahcene A, Deux B, Lamour V, Dobson R, DE Pauw E, Clezardin P, Castronovo V. Overexpression of CD9 in human breast cancer cells promotes the development of bone metastases. Anticancer Res. 2012 Dec;32(12):5211-20. PubMed PMID: 23225418.

13: Zhu Z, Ghose T, Hoskin D, Lee CL, Fernandez LA, Lee SH, Mammen M. Radioimmunotherapy of human B-cell chronic lymphocytic leukemia in nude mice. Cancer Res. 1994 Oct 1;54(19):5111-7. PubMed PMID: 7923127.

14: Huang F, Motlekar NA, Burgwin CM, Napper AD, Diamond SL, Mazin AV. Identification of specific inhibitors of human RAD51 recombinase using high-throughput screening. ACS Chem Biol. 2011 Jun 17;6(6):628-35. doi: 10.1021/cb100428c. Epub 2011 Mar 23. PubMed PMID: 21428443; PubMed Central PMCID: PMC3117970.

15: Fournier PG, Stresing V, Ebetino FH, Clézardin P. How do bisphosphonates inhibit bone metastasis in vivo? Neoplasia. 2010 Jul;12(7):571-8. PubMed PMID: 20651986; PubMed Central PMCID: PMC2907583.

16: Peyruchaud O, Winding B, Pécheur I, Serre CM, Delmas P, Clézardin P. Early detection of bone metastases in a murine model using fluorescent human breast cancer cells: application to the use of the bisphosphonate zoledronic acid in the treatment of osteolytic lesions. J Bone Miner Res. 2001 Nov;16(11):2027-34. PubMed PMID: 11697798.

17: Blair MW, Astudillo C, Rengifo J, Beebe SE, Graham R. QTL analyses for seed iron and zinc concentrations in an intra-genepool population of Andean common beans (Phaseolus vulgaris L.). Theor Appl Genet. 2011 Feb;122(3):511-21. doi: 10.1007/s00122-010-1465-8. Epub 2010 Nov 27. PubMed PMID: 21113704.

18: Contié S, Voorzanger-Rousselot N, Litvin J, Clézardin P, Garnero P. Increased expression and serum levels of the stromal cell-secreted protein periostin in breast cancer bone metastases. Int J Cancer. 2011 Jan 15;128(2):352-60. doi: 10.1002/ijc.25591. Epub 2010 Oct 13. PubMed PMID: 20715172.

19: Morita K, Kimura S, Saito M, Shinoyama H, Usami T, Amemiya Y, Shishido M. Generation and characterization of reduced virulence Fusarium oxysporum f. sp. lycopersici mutants through plasmid-vector insertion. Mycopathologia. 2005 Aug;160(1):67-73. PubMed PMID: 16160771.

20: King HO, Brend T, Payne HL, Wright A, Ward TA, Patel K, Egnuni T, Stead LF, Patel A, Wurdak H, Short SC. RAD51 Is a Selective DNA Repair Target to Radiosensitize Glioma Stem Cells. Stem Cell Reports. 2017 Jan 10;8(1):125-139. doi: 10.1016/j.stemcr.2016.12.005. PubMed PMID: 28076755; PubMed Central PMCID: PMC5233453.