Name: BMN 673
Price: 325.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    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.
    
    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.
- Properties
  - Alternative Name
    
    (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
    
    CAS Number
    
    1207456-01-6
    
    Molecular Formula
    
    C19H14F2N6O
    
    Molecular Weight
    
    380.35
    
    Appearance
    
    A solid
    
    Purity
    
    98.01%
    
    Solubility
    
    insoluble in H2O; ≥14.2 mg/mL in EtOH with gentle warming and ultrasonic; ≥19.02 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Ganesh Pai Bellare, Bhaskar Saha, et al. "Targeting autophagy reverses de novo resistance in homologous recombination repair proficient breast cancers to PARP inhibition." Br J Cancer. 2021 Mar;124(7):1260-1274. PMID:33473172

BMN 673

BMN 673

Background

We Also Recommend

Iniparib (BSI-201)

Olaparib (AZD2281, Ku-0059436)

Rucaparib (AG-014699,PF-01367338)