|BMN-673 8R,9S PARP inhibitor|
Sample solution is provided at 25 µL, 10mM.
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Related Biological Data
Related Biological Data
|BMN 673 is a novel PARP inhibitor with IC50 of 0.58 nM(PARP1). It does not inhibit PARG and is highly sensitive to PTEN mutation.|
|Cas No.||1207456-00-5||SDF||Download SDF|
|Canonical SMILES||O=C1C2=CC(F)=CC(N[[email protected]@H](C3=CC=C(F)C=C3)[[email protected]@H]4C5=NC=NN5C)=C2C4=NN1|
|Solubility||>38mg/ml in DMSO||Storage||Store at -20°C|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|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.|
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.
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 .
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.
 Shen Y, Rehman FL, Feng Y, Boshuizen J, Bajrami I, Elliott R, Wang B, Lord CJ, Post LE, Ashworth A. 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(18):5003-15.