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Purity: ≥98%
Talazoparib tosylate (formerly called BMN673 and MDV3800; trade name: Talzenna), the tosylate salt of talazoparib, is an inhibitor of PARP1/2 [poly(ADP-ribose) polymerase] with potential antineoplastic activity. It inhibits PARP in a cell-free assay with an IC50 of 0.58 nM. Its pharmacokinetic characteristics, oral bioavailability, and metabolic stability are all favorable. Patients with a germline BRCA mutation who have locally advanced or metastatic breast cancer can now receive talazoparib thanks to an FDA approval on October 16, 2018.
| Targets |
PARP1 ( IC50 = 0.57 nM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
Enzyme assays were carried out in 96-well FlashPlates with 0.5 U PARP1 enzyme, 0.25x activated DNA, 0.2 mCi [3H] NAD, and 5 mmol/L cold NAD (Sigma) in a final volume of 50 mL reaction buffer that contained 10% glycerol (v/v), 25 mmol/L HEPES, 12.5 mmol/L MgCl2, 50 mmol/L KCl, 1 mmol/L dithiothreitol (DTT), and 0.01% NP-40 (v/v), pH 7.6. NAD, either with or without inhibitors, was added to the PARP reaction mixture to start the reaction, which was then allowed to sit at room temperature for a minute. To halt the reaction, 50 microliter of ice-cold 20% trichloroacetic acid (TCA) was subsequently added to each well. Centrifugation took place after the plate was sealed and shaken for an additional 120 minutes at room temperature. Top-Count was used to identify the radioactive signal bound to the FlashPlate. Using the Michaelis–Menten equation, PARP1 Km was calculated for a range of substrate concentrations (1–100 mmol/L NAD). Utilizing the formula Ki ¼ IC50/[1þ (substrate)/Km], compound Ki was computed from the enzyme inhibition curve. The PARP2 enzyme Km and compound Ki were determined using the same assay protocol, with the exception of using 30 ng of PARP2, 0.25x activated DNA, 0.2 mCi [3H] NAD, and 20 mmol/L of cold NAD during the reaction's 30-minute room temperature duration.
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| Cell Assay |
For five days, temozolomide (TMZ) and talazoparib (10, 40 nM) are administered either alone or in combination to LoVo cells. CellTiter-Glo assay is used to determine the survivability fraction. [1]
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| Animal Protocol |
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| References |
| Molecular Formula |
C26H22F2N6O4S
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| Molecular Weight |
552.56
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| Exact Mass |
552.14
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| Elemental Analysis |
C, 56.52; H, 4.01; F, 6.88; N, 15.21; O, 11.58; S, 5.80
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| CAS # |
1373431-65-2
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CC1=CC=C(C=C1)S(=O)(=O)O.CN1C(=NC=N1)[C@@H]2[C@H](NC3=CC(=CC4=C3C2=NNC4=O)F)C5=CC=C(C=C5)F
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| InChi Key |
QUQKKHBYEFLEHK-QNBGGDODSA-N
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| InChi Code |
InChI=1S/C19H14F2N6O.C7H8O3S/c1-27-18(22-8-23-27)15-16(9-2-4-10(20)5-3-9)24-13-7-11(21)6-12-14(13)17(15)25-26-19(12)28;1-6-2-4-7(5-3-6)11(8,9)10/h2-8,15-16,24H,1H3,(H,26,28);2-5H,1H3,(H,8,9,10)/t15-,16-;/m1./s1
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| Chemical Name |
(11S,12R)-7-fluoro-11-(4-fluorophenyl)-12-(2-methyl-1,2,4-triazol-3-yl)-2,3,10-triazatricyclo[7.3.1.05,13]trideca-1,5(13),6,8-tetraen-4-one;4-methylbenzenesulfonic acid
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| Synonyms |
BMN 673 tosylate; BMN673; BMN-673; LT673 tosylate; LT 673; LT-673 tosylate; MDV-3800 tosylate; MDV 3800; MDV3800 tosylate; trade name: Talzenna
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 5%DMSO+ 40%PEG300+ 5%Tween 80+ 50%ddH2O: 2.5mg/ml (6.57mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8098 mL | 9.0488 mL | 18.0976 mL | |
| 5 mM | 0.3620 mL | 1.8098 mL | 3.6195 mL | |
| 10 mM | 0.1810 mL | 0.9049 mL | 1.8098 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04173507 | Active Recruiting |
Drug: Talazoparib Drug: Talazoparib Tosylate |
Stage IV Lung Cancer AJCC v8 Stage IVA Lung Cancer AJCC v8 |
SWOG Cancer Research Network | February 14, 2020 | Phase 2 |
| NCT04207190 | Active Recruiting |
Drug: Talazoparib Drug: Talazoparib Tosylate |
Recurrent Acute Myeloid Leukemia Refractory Acute Myeloid Leukemia |
Roswell Park Cancer Institute | October 23, 2020 | Phase 1 |
| NCT05873192 | Not yet recruiting | Drug: Talazoparib Drug: Degarelix |
Prostate Cancer | M.D. Anderson Cancer Center | September 30, 2023 | Phase 2 |
| NCT04693468 | Recruiting | Drug: Talazoparib Tosylate Drug: Crizotinib |
Advanced Malignant Solid Neoplasm Recurrent Malignant Solid Neoplasm |
M.D. Anderson Cancer Center | December 1, 2020 | Phase 1 |
| NCT04756765 | Recruiting | Drug: Talazoparib Tosylate | Breast Cancer Advanced Breast Cancer |
Stanford University | February 23, 2023 | Phase 2 |
 BMN 673 is a potent PARP inhibitor.Clin Cancer Res.2013 Sep 15;19(18):5003-15. |
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 A, siRNAs targeting homologous recombination genes sensitize to PARP1/2 inhibitors.Clin Cancer Res.2013 Sep 15;19(18):5003-15. |
 BMN 673 exhibits antitumor activity against a BRCA-mutant tumor model in mice.Clin Cancer Res.2013 Sep 15;19(18):5003-15. |
 BMN 673 potentiates the effects of DNA-damaging cytotoxic agents.Clin Cancer Res.2013 Sep 15;19(18):5003-15. |
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