Talazoparib [1207456-01-6]

Cat# HY-16106-5mg

Size : 5mg

Brand : MedChemExpress

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Description

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 has antitumor activity[1].

IC50 & Target[1]

PARP2

0.87 nM (Ki)

PARP1

1.2 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
CAPAN-1 IC50
1.8 nM
Compound: 5; BMN-673
Antiproliferative activity against human Capan1 cells after 7 days by CCK8 or SRB assay
Antiproliferative activity against human Capan1 cells after 7 days by CCK8 or SRB assay
[PMID: 28692916]
DLD-1 IC50
0.002 μM
Compound: 4
Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days
Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days
[PMID: 34570508]
LoVo EC50
2.5 nM
Compound: 9, BMN 673
Inhibition of PARP in human LoVo cells assessed as inhibition of hydrogen peroxide-induced PARylation treated for 30 mins prior to incubation with H2O2 for 5 mins by fluorescence analysis
Inhibition of PARP in human LoVo cells assessed as inhibition of hydrogen peroxide-induced PARylation treated for 30 mins prior to incubation with H2O2 for 5 mins by fluorescence analysis
[PMID: 25761096]
LoVo EC50
2.51 nM
Compound: (8S,9R)-47; BMN 673; Talazoparib
Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay
Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay
[PMID: 26652717]
LoVo GI50
4 nM
Compound: (8S,9R)-47; BMN 673; Talazoparib
Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay
Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay
[PMID: 26652717]
MDA-MB-436 IC50
0.012 nM
Compound: 2; BMN-673
Cytotoxicity against human MDA-MB-436 cells assessed as inhibition of cell viability incubated for 14 days with three intermittent intervals by CellTiterGlo luminescence assay
Cytotoxicity against human MDA-MB-436 cells assessed as inhibition of cell viability incubated for 14 days with three intermittent intervals by CellTiterGlo luminescence assay
[PMID: 33120078]
MDA-MB-436 IC50
0.38 nM
Compound: 2; BMN-673
Cytotoxicity against human MDA-MB-436 cells assessed as inhibition of cell viability incubated for 4 days by CellTiterGlo luminescence assay
Cytotoxicity against human MDA-MB-436 cells assessed as inhibition of cell viability incubated for 4 days by CellTiterGlo luminescence assay
[PMID: 33120078]
MDA-MB-436 IC50
0.7 nM
Compound: 5; BMN-673
Antiproliferative activity against human MDA-MB-436 cells after 7 days by CCK8 or SRB assay
Antiproliferative activity against human MDA-MB-436 cells after 7 days by CCK8 or SRB assay
[PMID: 28692916]
SUM149PT EC50
1.6 nM
Compound: Talazoparib
Cytotoxicity against BRCA1-deficient human SUM149 cells measured after 6 days by microscopic analysis
Cytotoxicity against BRCA1-deficient human SUM149 cells measured after 6 days by microscopic analysis
[PMID: 31042381]
SUM149PT EC50
23.2 nM
Compound: Talazoparib
Cytotoxicity against BRCA1-proficient human SUM149 cells measured after 6 days by microscopic analysis
Cytotoxicity against BRCA1-proficient human SUM149 cells measured after 6 days by microscopic analysis
[PMID: 31042381]
V79 IC50
5011.4 nM
Compound: 5; BMN-673
Cytotoxicity against BRCA2 expressing Chinese hamster V79 cells after 3 days by CCK8 or SRB assay
Cytotoxicity against BRCA2 expressing Chinese hamster V79 cells after 3 days by CCK8 or SRB assay
[PMID: 28692916]
In Vitro

Talazoparib shows an EC50 of 2.51 nM in cellular PARylation assay[1].
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)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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[1].
Talazoparib exhibits moderate oral bioavailability (rat 56%) and Cmax (rat 7948 ng/mL) following oral administration (rat 10 mg/kg)[1]. Talazoparib exhibits the terminal elimination half-life (rat 2.25 h) due to plasma clearance (2 mL/min/kg) following intravenous administration (rat 5 mg/kg)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nu/nu mice (8-10 weeks old), with MX-1 xenograft-bearing mice[1]
Dosage: 0.33 mg/kg
Administration: Oral gavage, once daily, for 28 days
Result: Significantly inhibited xenograft MX-1 tumor growth.
Animal Model: Sprague-Dawley rats[1]
Dosage: 5mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (56%), Cmax (7948 ng/mL), T1/2 (2.25 h).
Clinical Trial
Molecular Weight

380.35

Formula

C19H14F2N6O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NN=C2C3=C1C=C(F)C=C3N[C@H](C4=CC=C(F)C=C4)[C@H]2C5=NC=NN5C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (65.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6292 mL 13.1458 mL 26.2916 mL
5 mM 0.5258 mL 2.6292 mL 5.2583 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: 1.25 mg/mL (3.29 mM); Suspended solution; Need ultrasonic

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMAc    6% Solutol HS-15    84% PBS

    Solubility: 5 mg/mL (13.15 mM); Suspended solution; Need ultrasonic

Purity & Documentation
References

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