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BMN 673
Cat No.
CEI-1247
Product Overview
BMN673 is a potent and selective PARP1/2 inhibitor with Ki of 1.2 and 0.9 nM, respectively. It had no effect on panels of 72 receptors, ion channels, and enzymes. BMN673 showed IC50 value of 0.57 nM in enzymatic assay of PARP1. In in vitro assay, it exhibited greater potency than other existing PARP inhibitors, such as veliparib, rucaparib, and olaparib. It is also much more potent at trapping PARP-DNA complexes than other PARP inhibitors. 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.
CAS No.
1207456-01-6
Molecular Weight
380.35
Purity
0.9801
Storage
Store at -20°C
Targets
PARP
IC50
0.58 nM
Molecular Formula
C19H14F2N6O
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
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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