Talazoparib (BMN 673)

Catalog No.S7048

Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM in a cell-free assay. 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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Talazoparib (BMN 673) Chemical Structure

Talazoparib (BMN 673) Chemical Structure
Molecular Weight: 380.35

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Product Information

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  • Research Area
  • Inhibition Profile

Product Description

Biological Activity

Description Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM in a cell-free assay. 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]
(Cell-free assay)
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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
MIA PaCa-2M3rjTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NFXhOZdKSzVyPUW4MlI{6oDLwsJihKk5NjIkgJpCuW3DqA>?NGPvVHkzPTh4NEW5NC=>

... Click to View More Cell Line Experimental Data

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

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

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
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] 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 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02836028 Not yet recruiting Ovarian Cancer Medivation, Inc. October 2016 Phase 2
NCT02567396 Not yet recruiting Estrogen Receptor Negative|Head and Neck Squamous Cell Carcinoma|HER2/Neu Negative|Hormone-Resistant Prostate Cancer|Metastatic Pancreatic Adenocar  ...more Estrogen Receptor Negative|Head and Neck Squamous Cell Carcinoma|HER2/Neu Negative|Hormone-Resistant Prostate Cancer|Metastatic Pancreatic Adenocarcinoma|Progesterone Receptor Negative|Solid Neoplasm|Stage III Mesothelioma|Stage IIIA Gastric Cancer|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIA Ovarian Cancer|Stage IIIA Small Cell Lung Carcinoma|Stage IIIB Gastric Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IIIB Ovarian Cancer|Stage IIIB Small Cell Lung Carcinoma|Stage IIIC Gastric Cancer|Stage IIIC Ovarian Cancer|Stage IV Mesothelioma|Stage IV Non-Small Cell Lung Cancer|Stage IV Ovarian Cancer|Stage IV Small Cell Lung Carcinoma|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) July 2016 Phase 1
NCT02627430 Withdrawn Adult Solid Neoplasm|Estrogen Receptor Negative|Fallopian Tube Serous Neoplasm|HER2/Neu Negative|Ovarian Serous Adenocarcinoma|Ovarian Serous Tumor  ...more Adult Solid Neoplasm|Estrogen Receptor Negative|Fallopian Tube Serous Neoplasm|HER2/Neu Negative|Ovarian Serous Adenocarcinoma|Ovarian Serous Tumor|Primary Peritoneal Serous Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) March 2016 Phase 1
NCT02537561 Withdrawn Solid Tumors|Carcinoma, Non-Small Cell Lung|Non-Small Cell Lung Cancer|Non-Small-Cell Lung Carcinoma|Nonsmall Cell Lung Cancer Washington University School of Medicine|BioMarin Pharmac  ...more Washington University School of Medicine|BioMarin Pharmaceutical December 2015 Phase 1
NCT02401347 Recruiting Advanced Breast Cancer|HER2/Neu Negative|Triple-Negative Breast Cancer Melinda Telli|National Cancer Institute (NCI)|Stanford Un  ...more Melinda Telli|National Cancer Institute (NCI)|Stanford University August 2015 Phase 2

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Chemical Information

Molecular Weight (MW) 380.35


CAS No. 1207456-01-6
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms LT-673
Solubility (25°C) * In vitro DMSO 38 mg/mL warming (99.9 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo
* <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)-

Frequently Asked Questions

  • Question 1
    Which solvent do you recommend to dilute the inhibitor for in vivo study in mice?

    Answer: BMN673 (S7048) can be dissolved in vehicle (10% DMAc, 6% Solutol, and 84% PBS) according to the paper: http://clincancerres.aacrjournals.org/content/19/18/5003.full. Quote from Method and Material section "Xenograft experiments: BMN 673 (various doses as indicated), or vehicle (10% DMAc, 6% Solutol, and 84% PBS) was administered by oral gavage"

Tech Support

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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