BMN 673

Catalog #

27609-1

$395 *

Size: 10 mg

Qty

Bulk/Custom

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Description

BMN673 is a potent and selective PARP1/2 inhibitor with Ki of 1.2 and 0.9 nM, respectively.

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Synonyms

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

Biological Activity

BMN673 showed IC50 value of 0.57 nM in enzymatic assay of PARP1 1. In in vitro assay, it exhibited greater potency than other existing PARP inhibitors, such as veliparib, rucaparib, and olaparib. It is much more potent at trapping PARP-DNA complexes than other PARP inhibitors.

CAS Registry #

1207456-01-6

Background

BMN673 has shown anti-tumor activity both in vitro and in vivo. It inhibited proliferation of tumor cells and xenografts with defects in homologous recombination. The combination of BMN673 and DNA-damaging agents demonstrated synergistic anti-tumor effects. In addition, study showed that the expression levels of DNA repair proteins and status of PI3K pathway predict response to BMN673 in small cell lung cancer. BMN673 is currently under investigation in multiple clinical trials for advanced solid tumors or hematological malignancies, either as monotherapy or in combination with other anti-tumor agents.

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

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