Talazoparib (BMN 673)

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

Validation & Quality Control

Customer Product Validation(2)

Quality Control & MSDS

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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-2NFjab4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Mm\aTWM2OD13OD6yN-KBkcLz4pEJPE4y6oDLwsXNxsA>MWmyOVg3PDV7MB?=

... 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 2015-11-14)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
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
NCT02537561 Not yet recruiting 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
NCT02317874 Recruiting Adult Solid Neoplasm National Cancer Institute (NCI) July 2015 Phase 1
NCT02316834 Recruiting Fallopian Tube Cancer|Ovarian Cancer|Peritoneal Cancer M.D. Anderson Cancer Center|BioMarin Pharmaceutical June 2015 Phase 0

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Chemical Information

Molecular Weight (MW) 380.35


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

Customer Product Validation (2)

Click to enlarge
Source Cell Cycle, 2015, 14(14): 2323-32. Talazoparib (BMN 673) purchased from Selleck
Method MTT Assay Analysis
Cell Lines BT-549 cells
Concentrations 0-20 µM
Incubation Time 5 d
Results We determined that WT PTEN cells displayed decreased sensitivity to the PARP inhibitor, BMN673. However, similar sensitivity to BMN673 was observed in control and both PTEN Y336* and PTEN-HP1aKD mutant reconstituted BT-549 cells.

Click to enlarge
Source Front Oncol, 2014, 4: 368. Talazoparib (BMN 673) purchased from Selleck
Method MTT Assay Analysis
Cell Lines H1299D2-down、H1299E、A549D2-down、A549E cells
Concentrations 0.5 µM
Incubation Time 24、48、72 h
Results Cell viability analysis showed that BMN673 was overall a more potent inhibitor (10-fold difference in active doses) compared to veliparib. H1299 FANCD2 knock-down cancer cells were also more sensitive to BMN673 compared to empty vectors transfected control cells (25 vs.62% viable cells, respectively) 72 h post treatment. A549D2-down cell had 29% viable cells and the A549E had 46% viable cells 72 h post treatment.

Product Use Citation (3)

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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