Talazoparib (Synonyms: BMN-673; LT-673)

Name: Talazoparib
Brand: MedChemExpress
SKU: HY-16106
Rating: 5.0 (76 reviews)

Cat. No.: HY-16106 Purity: 99.64%: Data Sheet
SDS

COA
Handling Instructions
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Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with K_is of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity.

For research use only. We do not sell to patients.

Talazoparib Chemical Structure

CAS No. : 1207456-01-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	Get quote
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Customer Review

Based on 76 publication(s) in Google Scholar

Other Forms of Talazoparib:

75 Publications Citing Use of MCE Talazoparib

: Talazoparib purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2020 Sep;59:102923. [Abstract]; Western Blot analyses of TP53, p21 and RAD51 in PARP inhibitor sensitive (SKCO1 and LS513) and resistant cell lines (SW1222 and SNU61) after treatment with Talazoparib for 48 h. Talazoparib decreases RAD51 protein expression in the two TP53 wild-type cell lines SKCO1 and LS513.

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View All Isoforms

PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

Biological Activity
Purity & Documentation
References
Customer Review

Description

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 C_max (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%), C_max (7948 ng/mL), T_1/2 (2.25 h).

Clinical Trial

Molecular Weight

380.35

Formula

C₁₉H₁₄F₂N₆O

CAS No.

1207456-01-6

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
10 mM	0.2629 mL	1.3146 mL	2.6292 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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
Protocol 3

Add each solvent one by one: 2% DMSO 40% PEG300 5% Tween-80 53% Saline
Solubility: ≥ 0.5 mg/mL (1.31 mM); Clear solution
Protocol 4

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.25 mg/mL (0.66 mM); Clear solution

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.89%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (254 KB) LCMS (125 KB) Elemental Analysis Report (112 KB)

Handling Instructions (2659 KB)

References

[1]. Wang B, et al. Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent. J Med Chem. 2016 Jan 14;59(1):335-57. [Content Brief]

[2]. Shen Y, et al. BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency.Clin Cancer Res. 2013 Sep 15;19(18):5003-15. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6292 mL	13.1458 mL	26.2916 mL	65.7289 mL
	5 mM	0.5258 mL	2.6292 mL	5.2583 mL	13.1458 mL
	10 mM	0.2629 mL	1.3146 mL	2.6292 mL	6.5729 mL
	15 mM	0.1753 mL	0.8764 mL	1.7528 mL	4.3819 mL
	20 mM	0.1315 mL	0.6573 mL	1.3146 mL	3.2864 mL
	25 mM	0.1052 mL	0.5258 mL	1.0517 mL	2.6292 mL
	30 mM	0.0876 mL	0.4382 mL	0.8764 mL	2.1910 mL
	40 mM	0.0657 mL	0.3286 mL	0.6573 mL	1.6432 mL
	50 mM	0.0526 mL	0.2629 mL	0.5258 mL	1.3146 mL
	60 mM	0.0438 mL	0.2191 mL	0.4382 mL	1.0955 mL

Talazoparib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Talazoparib (Synonyms: BMN-673; LT-673)

Customer Review

Other Forms of Talazoparib:

75 Publications Citing Use of MCE Talazoparib

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•Related Small Molecules:

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View All PARP Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

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Complete Stock Solution Preparation Table

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Talazoparib (Synonyms: BMN-673; LT-673)

Customer Review

Other Forms of Talazoparib:

Talazoparib Related Antibodies

75 Publications Citing Use of MCE Talazoparib

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•Related Screening Libraries:

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•Related Proteins:

View All PARP Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Talazoparib Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Talazoparib Related Classifications

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