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BMN-673 8R,9SPARP inhibitor

BMN-673 8R,9S

Catalog No. A3246
Size Price Stock Qty
5mg $185.00 Ship Within 10-14 Days
10mg $252.00 Please Inquire
50mg $570.00 Please Inquire
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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

BMN-673 8R,9S

Related Biological Data

BMN-673 8R,9S

Related Biological Data

BMN-673 8R,9S

Biological Activity

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.
Targets PARP          
IC50 0.58 nM          

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Chemical Properties

Cas No. 1207456-00-5 SDF Download SDF
Synonyms (8R,9S)-BMN-673
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
Canonical SMILES O=C1C2=CC(F)=CC(N[C@H](C3=CC=C(F)C=C3)[C@H]4C5=NC=NN5C)=C2C4=NN1
Formula C19H14F2N6O M.Wt 380.35
Solubility Soluble in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

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 [1].
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 [1].
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.
Reference:
[1] 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.