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 3.

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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

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  • Most Potent PARP Inhibitor

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  • Inhibitor in Clinical Trial

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

  • Newest PARP Inhibitor

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Product Information

  • Inhibition Profile
  • Compare PARP Inhibitors
    Compare PARP Products
  • 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 3.
Targets PARP [1]
IC50 0.58 nM
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)
Formulation
Dosages 0.33 mg/kg/day, once daily
Administration Oral
1

References

[1] Wang B, et al. Molecular Cancer Therapeutics, 2009, 8 (12 Suppl), A121.

[2] Shen YQ, et al. Cancer Research, 2010, 70 (8 Suppl), Abstract nr 3514.

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

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01989546 Recruiting Advanced Ovarian Cancer|Primary Peritoneal Cancer|Advanced Breast Cancer|Advanced Solid Tumors National Institutes of Health Clinical Center (CC)|National Cancer Institute (NCI) 2013-11 Phase 1|Phase 2
NCT02034916 Recruiting Breast Neoplasms|BRCA 1 Gene Mutation|BRCA 2 Gene Mutation BioMarin Pharmaceutical|Translational Research in Oncology|Myriad Genetics, Inc. 2014-01 Phase 2
NCT02116777 Not yet recruiting Recurrent Adult Acute Lymphoblastic Leukemia; Recurrent Childhood Acute Lymphoblastic Leukemia; Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor; Unspecified Adult Solid Tumor, Protocol Specific; Unspecified Childhood Solid Tumor, Protocol Specific National Cancer Institute (NCI) 2014-04 Phase 1|Phase 2
NCT02049593 Not yet recruiting Metastatic Cancer|Unspecified Adult Solid Tumor Jonsson Comprehensive Cancer Center|Translational Research in Oncology-US (TRIO-US) 2014-04 Phase 1
NCT02127151 Not yet recruiting Endometrial Cancer University College, London|BioMarin Pharmaceutical 2014-08 Phase 2

Chemical Information

Molecular Weight (MW) 380.35
Formula

 

C19H14F2N6O
 
CAS No. 1207456-01-6
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms LT-673
Solubility (25°C) * In vitro DMSO 76 mg/mL heating (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)-

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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