Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib shows EC50s of 0.3 nM, 5 nM and 0.31 for MX-1 cells (BRCA1 mutant), Capan-1 cells (BRCA2 mutant) and MRC-5 cells (normal).
In vivo, Talazoparib (0.33 mg/kg; i.g.; once daily; for 28 days) exhibits antitumor activity against BRCA1 mutant breast cancer model in mice
cancers. 2023 Aug 16.
Development of a Patient-Derived 3D Immuno-Oncology Platform to Potentiate Immunotherapy Responses in Ascites-Derived Circulating Tumor Cells
Talazoparib (BMN-673) purchased from AbMole
Front Oncol. 2023 May 9;13:1175617.
Sustained delivery of PARP inhibitor Talazoparib for the treatment of BRCA-deficient ovarian cancer
Talazoparib (BMN-673) purchased from AbMole
Front Oncol. 2022 Aug 16;12:940377.
Effectiveness of PARP inhibition in enhancing the radiosensitivity of 3D spheroids of head and neck squamous cell carcinoma
Talazoparib (BMN-673) purchased from AbMole
BMC Biol. 2021 May 20;19(1):108.
Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
Talazoparib (BMN-673) purchased from AbMole
Clin Cancer Res. 2020 Oct 15;26(20):5462-5476.
A Preclinical Trial and Molecularly Annotated Patient Cohort Identify Predictive Biomarkers in Homologous Recombination-deficient Pancreatic Cancer
Talazoparib (BMN-673) purchased from AbMole
Nat Commun. 2019 Dec 20;10(1):5799.
Novel approach reveals genomic landscapes of single-strand DNA breaks with nucleotide resolution in human cells.
Talazoparib (BMN-673) purchased from AbMole
Proc Natl Acad Sci U S A. 2019 Nov 5;116(45):22609-22618.
DNA methyltransferase inhibitors induce a BRCAness phenotype that sensitizes NSCLC to PARP inhibitor and ionizing radiation.
Talazoparib (BMN-673) purchased from AbMole
US Patent. 2019 Jul 30.
THERAPY REGIMEN AND METHODS TO SENSITIZE CANCER CELLS TREATED WITH EPIGENETIC THERAPY TO PARP INHIBITORS IN MULTIPLE CANCERS
Talazoparib (BMN-673) purchased from AbMole
Nat Commun. 2018 Nov 12;9(1):4760.
Defective DNA damage repair leads to frequent catastrophic genomic events in murine and human tumors.
Talazoparib (BMN-673) purchased from AbMole
University of Maryland. 2017.
Developing a Novel Combination Therapy and Elucidating Mechanisms of Increased ALT-NHEJ in Acute Myeloid Leukemia
Talazoparib (BMN-673) purchased from AbMole
Cancer Cell. 2016 Oct 10;30(4):637-650.
Enhancing the Cytotoxic Effects of PARP Inhibitors with DNA Demethylating Agents – A Potential Therapy for Cancer
Talazoparib (BMN-673) purchased from AbMole
Cancer Lett. 2015 Aug 1;364(1):8-16.
Increased in vitro and in vivo sensitivity of BRCA2-associated pancreatic cancer to the poly(ADP-ribose) polymerase-1/2 inhibitor BMN 673.
Talazoparib (BMN-673) purchased from AbMole
Cell Rep. 2014 Nov 6;9(3):829-41.
Targeting the DNA repair pathway in Ewing sarcoma.
Talazoparib (BMN-673) purchased from AbMole
Cell Experiment | |
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Cell lines | Capan-1 and MIA PaCa-2 |
Preparation method | Real-time cell analysis (xCELLigence) |
Concentrations | |
Incubation time | 48 h |
Animal Experiment | |
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Animal models | Patient-derived xenograft (PDX) model |
Formulation | Solubilized in DMSO and diluted with PBS containing 10% dimethylacetamide (Sigma-Aldrich) and 6% Solutol (Sigma-Aldrich). |
Dosages | 0.33 mg/kg, 0.05 cc, once daily |
Administration | oral gavage |
Molecular Weight | 380.35 |
Formula | C19H14F2N6O |
CAS Number | 1207456-01-6 |
Solubility (25°C) | DMSO 25 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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DSB-1522
DSB-1522 is a PARP1 inhibitor that can be used in tumor-related studies. |
DM-5167
DM-5167 is a PARP1 inhibitor that can be used in studies related to triple negative breast cancer. |
NMS-03305293
NMS-03305293 is a PARP inhibitor with high selectivity for PARP1 isoforms and low DNA capture effect, which specifically kills BRCA mutated tumor cells. In addition, NMS-03305293 can penetrate the blood-brain barrier and can be used in studies related to CNS tumors and brain metastatic tumors. |
SNV1521
SNV1521 is a potential best-in-class (BIC), highly selective and CNS-permeable PARP1 inhibitor. |
Basroparib
Basroparib is an orally active selective inhibitor of end-anchor polymerase (TNKS) and an inhibitor of ribose polymerase (PARP) with antitumor activity. |
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