BMN 673

Catalog No.S7048

BMN 673 is a novel PARP inhibitor with IC50 of 0.58 nM. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 1.

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BMN 673 Chemical Structure

BMN 673 Chemical Structure
Molecular Weight: 380.35

Validation & Quality Control

Quality Control & MSDS

PARP Inhibitors with Unique Features

  • Selective PARP Inhibitors

    AG-14361 PARP1-selective, Ki<5 nM. UPF 1069 PARP2-selective, IC50=0.3 μM.

  • Most Potent PARP Inhibitor

    MK-4827 (Niraparib) PARP1, IC50=3.8 nM; PARP2, IC50=2.1 nM.

  • Inhibitor in Clinical Trial

    Iniparib (BSI-201) Phase III for solid tumors.

  • Newest PARP Inhibitor

    PJ34 HCl PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

Product Information

  • Inhibition Profile
  • Compare PARP Inhibitors
    Compare PARP Inhibitors
  • Research Area

Product Description

Biological Activity

Description BMN 673 is a novel PARP inhibitor with IC50 of 0.58 nM. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 1.
Targets PARP
IC50 0.58 nM [1]
In vitro BMN-673 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability and eventually leads to apoptosis. BMN 673 selectively kills cancer cells with BRCA-1 or BRCA-2 mutations. BMN 673 demonstrates single-agent cytotoxicityin BRCA-1 mutant (MX-1, IC50 = 0.3 nM) and BRCA-2 mutant cells (Capan-1, IC50 = 5 nM). In contrast, in MRC-5 normal human fibroblastand other tumor cell lines with wild-type BRCA-1 and BRCA-2 genes, IC50 of BMN 673 ranges between 90 nM and 1.9 μM. [1] In cultured human cancer cells, BMN 673 also significantly enhances the cytotoxic efficacy of both Temozolomide and SN-38. Off-target molecular screening did not identify significant non-specific activity for this class of PARP inhibitors. [2]
In vivo In rat pharmacokinetic studies, BMN 673 displays >50% oralbioavailability and pharmacokinetic properties that enable singledaily dosing. In MX-1 xenograft tumor model studies, daily oral dosingof BMN 673 significantly enhances the antitumor effects ofcytotoxic therapies in a dose-dependent manner. [2]
Features Most potent and selective PARPi reported thus far.

Protocol(Only for Reference)

Animal Study: [2]

Animal Models MX-1 model (BRCA-1 deficient)
Dosages 0.33 mg/kg/day, once daily
Administration Oral
1

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01286987 Recruiting Advanced or Recurrent Solid Tumors|Breast Neoplasms|Ovarian Cancer, Epithelial|Ewing Sarcoma|Small Cell Lung Carcinoma|Prostate Cancer|Pancreas Cancer BioMarin Pharmaceutical 2010-12 Phase 1
NCT01399840 Active, not recruiting Acute Myeloid Leukemia|Myelodysplastic Syndrome|Chronic Lymphocytic Leukemia|Mantle Cell Lymphoma BioMarin Pharmaceutical 2011-06 Phase 1
NCT01776437 Active, not recruiting Human Volunteers BioMarin Pharmaceutical 2013-02 Phase 1

Chemical Information

Molecular Weight (MW) 380.35
Formula

 

C19H14F2N6O
 
CAS No. 1207456-01-6
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms LT-673
Solubility (25°C) * In vitro DMSO 76 mg/mL (199 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 3H-Pyrido[4,3,2-de]phthalazin-3-one, 5-fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-methyl-1H-1,2,4-triazol-5-yl)-, (8S,9R)-

Preparing Stock Solutions

Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.38035 3.8035 7.607 11.4105

Research Area

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

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Related PARP Inhibitors

  • BMN 673

    BMN 673 is a novel PARP inhibitor with IC50 of 0.58 nM. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 1.

    Features:Most potent and selective PARPi reported thus far.

  • UPF 1069

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    Features:The most selective PARP2 inhibitor available to date.

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    Features:Increases the efficacy of common cancer therapies such as radiation and alkylating agents.

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  • Iniparib (BSI-201)

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