Talazoparib (BMN 673)

Catalog No.S7048 3 Product Use Citation

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

Quality Control & MSDS

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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]
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)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
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

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 2015-08-29)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
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
NCT02127151 Not yet recruiting Endometrial Cancer University College, London|BioMarin Pharmaceutical June 2015 Phase 2
NCT02282345 Recruiting Breast Cancer M.D. Anderson Cancer Center|BioMarin Pharmaceutical April 2015 Phase 2

view more

Chemical Information

Molecular Weight (MW) 380.35
Formula

 

C19H14F2N6O
 
CAS No. 1207456-01-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms LT-673
Solubility (25°C) * In vitro DMSO 76 mg/mL warmed (199.81 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)-

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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