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BMN-673 8R,9S
Cat No.
CEI-1248
Product Overview
PARP1/2 inhibitors are a class of anticancer agents that target tumor-specific defects in DNA repair. BMN 673 is a highly potent PARP1/2 inhibitor. Clinical trial: Pharmacokinetics (PK), pharmacodynamics (PD), safety and anti-tumor activity of BMN 673 were evaluated in a 2-stage dose-escalation study with 3-6 patients (pts)/dose level. Results showed BMN 673 was well tolerated with impressive anti-tumor activity in pts with BRCA mut with a single agent recommended Phase II trial dose of 1000 μg/d due to dose-limiting thrombocytopenia.
CAS No.
1207456-00-5
Molecular Weight
380.35
Purity
0.98
Storage
Store at -20°C
Synonyms
(8R,9S)-BMN-673
Targets
PARP
Molecular Formula
C19H14F2N6O
Chemical 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
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
In vitro
BMN 673 is a potent PARP1/2 inhibitor, but it does not inhibit other enzymes that we have tested. BMN673 exhibits selective antitumor cytotoxicity and elicits DNA repair biomarkers at much lower concentrations than earlier generation PARP1/2 inhibitors. BMN 673 targeted tumor cells with BRCA1, BRCA2, or PTEN gene defects selectively with 20-to more than 200-fold greater potency than existing PARP1/2 inhibitors in vitro.
In vivo
BMN 673 is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in CMC. Orally BMN 673 elicited remarkable antitumor activity in mice; xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency were profoundly sensitive to oral BMN 673 treatment at well-tolerated doses. Synergistic antitumor effects were also found when BMN 673 was combined with temozolomide, SN38, or platinum drugs.
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