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BMN 673Potent PARP inhibitor

BMN 673

Catalog No. A4153
Size Price Stock Qty
Evaluation Sample $28.00 In stock
10mg $250.00 In stock
50mg $650.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

BMN 673

Related Biological Data

BMN 673

Related Biological Data

BMN 673

Biological Activity

BMN673 is a potent and selective inhibitor of PARP1,PARP2 with Ki of 1.2 and 0.9 nM, respectively .
Targets PARP          
IC50 0.58 nM          

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Chemical Properties

Cas No. 1207456-01-6 SDF Download SDF
Chemical Name (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
Canonical SMILES FC1=CC2=N[C@@H](C(C=C3)=CC=C3F)[C@H](C4=NC=NN4C)C(NNC5=O)=C2C5=C1
Formula C19H14F2N6O M.Wt 380.35
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

BMN673 is a potent and selective PARP1/2 inhibitor with Ki of 1.2 and 0.9 nM, respectively 1. It had no effect on panels of 72 receptors, ion channels, and enzymes 1. 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 2. It is also much more potent at trapping PARP-DNA complexes than other PARP inhibitors 3.

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 1. The combination of BMN673 and DNA-damaging agents demonstrated synergistic anti-tumor effects 1. 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 4.

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, Rehman FL, Feng Y et al. BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency. Clin Cancer Res 2013; 19: 5003-5015.
2. Cardnell RJ, Byers LA. Proteomic Markers of DNA Repair and PI3K Pathway Activation Predict Response to the PARP Inhibitor BMN 673 in Small Cell Lung Cancer--Response. Clin Cancer Res 2014; 20: 2237.
3. Murai J, Huang SY, Renaud A et al. Stereospecific PARP trapping by BMN 673 and comparison with olaparib and rucaparib. Mol Cancer Ther 2014; 13: 433-443.
4. Cardnell RJ, Feng Y, Diao L et al. Proteomic markers of DNA repair and PI3K pathway activation predict response to the PARP inhibitor BMN 673 in small cell lung cancer. Clin Cancer Res 2013; 19: 6322-6328.