BMN-673 8R,9S

Catalog #

27610-1

$335 *

Size: 10 mg

Qty

Bulk/Custom

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Description

BMN 673 is a novel PARP inhibitor with IC50 of 0.58 nM(PARP1). It does not inhibit PARG and is highly sensitive to PTEN mutation. BMN-673 (8R,9S) is the (8R,9S) enantiomer of BMN-673.

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Synonyms

(8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one

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Product Data Gallery

Product Info

Storage and Usage

Citations

Purity

≥98% by HPLC

Target(s)

PARP1

Formula

C₁₉H₁₄F₂N₆O

380.4 Da

Solubility

Soluble in DMSO

CAS Registry #

1207456-00-5

Background

BMN-673 is an orally bioavailable inhibitor of the nuclear enzyme poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. PARP inhibitor BMN-673 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability and eventually leads to apoptosis. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other proteins to repair damaged DNA and is activated by single-strand DNA breaks. BMN-673 has been proven to be highly active in mouse models of human cancer and also appears to be more selectively cytotoxic with a longer half-life and better bioavailability as compared to other compounds in development.

References

1. Shen Y, et al. Clin Cancer Res 2013; 19: 5003-5015.
2. Cardnell RJ, et al. Clin Cancer Res 2014; 20: 2237.
3. Murai J, et al. Mol Cancer Ther 2014; 13: 433-443.
4. Cardnell RJ, et al. Clin Cancer Res 2013; 19: 6322-6328.

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BMN-673 8R,9S

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