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

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Product Information

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  • Research Area
  • Inhibition Profile

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
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, updated on 2014-10-24)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02127151 Not yet recruiting Endometrial Cancer University College, London|BioMarin Pharmaceutical August 2014 Phase 2
NCT02049593 Recruiting Metastatic Cancer|Unspecified Adult Solid Tumor Jonsson Comprehensive Cancer Center|National Cancer Insti  ...more Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) June 2014 Phase 1
NCT02116777 Recruiting Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Lymphoblastic Leukemia|Recurrent Ewing Sarcoma/Peripheral Primitive Neuroect  ...more 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) May 2014 Phase 1|Phase 2
NCT01989546 Recruiting Advanced Ovarian Cancer|Primary Peritoneal Cancer|Advanced Breast Cancer|Advanced Solid Tumors National Cancer Institute (NCI)|National Institutes of He  ...more National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) November 2013 Phase 1|Phase 2
NCT01776437 Completed Human Volunteers BioMarin Pharmaceutical February 2013 Phase 1

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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.

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