Talazoparib (BMN 673)

Catalog No.S7048 Synonyms: LT-673

Talazoparib (BMN 673) Chemical Structure

Molecular Weight(MW): 380.35

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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2 Customer Reviews

  • BT-549 cells reconstituted with Vet, WT, 336* or PTEN WT HP1aKD were treated with BMN673. Relative cell viability was determined by MTT assay. The results were presented as mean of 3 independent experiments. Error bars indicate s.d.

    Cell Cycle, 2015, 14(14): 2323-32. Talazoparib (BMN 673) purchased from Selleck.

    We treated the FA defective and control lung cancer cell lines H1299D2-down/H1299E and A549D2 down/A549E with BMN673 (0.5 µM). MTT assay was used for the cell viability analysis and an averaged absorbance was recorded 24, 48 and 72 h post treatment.

    Front Oncol, 2014, 4: 368. Talazoparib (BMN 673) purchased from Selleck.

Purity & Quality Control

Choose Selective PARP Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.
Features Most potent and selective PARPi reported thus far.
Targets
PARP [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BR5FVB1-Akt MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFO3RZAxNjFvMUCwJI5O NWnLdWl3OjRxNEivO|IhcA>? NXnSUmFrcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MmCyNlYxPDd4OUe=
BR5FVB1-Akt NFnVTZNCeG:ydH;zbZMhSXO|YYm= NI\UN|kxNjFvMUCwJI5O MU[3NkBp MknWbY5lfWOnczDhdI9xfG:|aYO= MWmyOlA1PzZ7Nx?=
Capan-1 Ml3GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTF4LkFihKnDueLCiUWuOQKBkcL3TdMg M2ThXlI2QDZ2NUmw
MIA PaCa-2 MkTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XWeGlEPTB;NUiuNlPjiIoEsfMAjVgvOeLCidM1UeKh MlHuNlU5PjR3OUC=
RD NVXsXlBYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rhOmlEPTB;OD63JI5O M3fTTlI2OjZ|NUO5
Rh41 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XLbWlEPTB;OD6xJI5O NWHqb2V5OjV{NkO1N|k>
Rh18 M{XDUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvjTW9KSzVyPUSuPUBvVQ>? NFnqT2YzPTJ4M{WzPS=>
Rh30 NUXPWIt3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXez[IJrUUN3ME2zNU4yKG6P NXL4fHdPOjV{NkO1N|k>
BT-12 MkO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRuLCiUGsNFAxKG6P NFvacYgzPTJ4M{WzPS=>
CHLA-266 Ml3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\JUGlEPTB-4pEJNUwxODBibl2= NUn4[45EOjV{NkO1N|k>
TC-71 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzpd2xKSzVyPUOuO{BvVQ>? NWHXeo5COjV{NkO1N|k>
CHLA-9 NUjwdIh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\FSGI1UUN3ME24MlIhdk1? MlrONlUzPjN3M{m=
CHLA-10 NEm5colIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE[zOYtKSzVyPU[3Mlghdk1? NUH2UFhUOjV{NkO1N|k>
CHLA-258 M2LYcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlyxTWM2OD12Lk[gcm0> MXOyOVI3OzV|OR?=
SJ-GBM2 NUj1ZWdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrJTWM2OD1zNj6yJI5O MYqyOVI3OzV|OR?=
NB-1643 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1H3XGlEPTB;MUiuOEBvVQ>? NXf5bYhQOjV{NkO1N|k>
NB-EBc1 MknvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v3d2lEPTB;MkWuPEBvVQ>? MV2yOVI3OzV|OR?=
CHLA-90 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;xTWM2OD8kgJmxMFAxOCCwTR?= Mnj6NlUzPjN3M{m=
CHLA-136 NXHYO|loT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTF2LkKgcm0> NXftRXhbOjV{NkO1N|k>
NALM-6 NVnYZ3hZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojHTWM2OD12OTDuUS=> NXvEPVN3OjV{NkO1N|k>
COG-LL-317 M2e5b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH2zXJlKSzVyPUmuOEBvVQ>? NHfaR5MzPTJ4M{WzPS=>
RS4;11 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXBTWM2OD13Mj62JI5O M{fyZ|I2OjZ|NUO5
MOLT-4 NVTQb21NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HoVGlEPTB;MU[uOkBvVQ>? M3rETlI2OjZ|NUO5
CCRF-CEM MlSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn:4TWM2OD14OUeuN{BvVQ>? M4G2RVI2OjZ|NUO5
Kasumi-1 MkXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLHTWM2OD15OE[uNkBvVQ>? M{HMe|I2OjZ|NUO5
Karpas-299 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEf1NGtKSzVyPUe1Mlchdk1? NYPCbWFKOjV{NkO1N|k>
Ramos-RA1 NUPEVmw1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\oeFZKSzVyPU[4MlMhdk1? M{jT[|I2OjZ|NUO5
DT40 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4P0OmlEPTB;NDDuUS=> NUHGeZZHOjR|NU[4NVM>
DU145 MmLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTFzIH7N NV;Lc2N5OjR|NU[4NVM>
H209 Mle5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkP2TWM2OD1zLkegcm0> MYeyOFA4PzN3MB?=
H1048 M2XEN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2L3UWlEPTB;Mj6yJI5O NXmxcVl7OjRyN{ezOVA>
H524 M2jUPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGmwOoRKSzVyPUOuNUBvVQ>? MlnONlQxPzd|NUC=
H1930 NYfiO2JTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHHdXVSUUN3ME20MlEhdk1? NXTLSIdYOjRyN{ezOVA>
H69 NHn5SmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1niXWlEPTB;NT6yJI5O MlHONlQxPzd|NUC=
H2081 NHW5R5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TLUGlEPTB;Nj6zJI5O NXPPeJNuOjRyN{ezOVA>
H2107 M2D3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\GTFFXUUN3ME23MlMhdk1? MVyyOFA4PzN3MB?=
H1092 NUTjZnlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvITWM2OD16Lkmgcm0> NXfQ[YV6OjRyN{ezOVA>
DMS-79 MmToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrVN2FQUUN3ME25MlMhdk1? NWju[nFyOjRyN{ezOVA>
H446 NF7LTYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTF|IH7N MWGyOFA4PzN3MB?=
COR-L279 M4n4R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XhT2lEPTB;MUWgcm0> M13oelI1ODd5M{Ww

... Click to View More Cell Line Experimental Data

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]

Protocol

Solubility (25°C)

In vitro DMSO 38 mg/mL (99.9 mM) warming
Water <1 mg/mL
Ethanol <1 mg/mL
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 Information

Molecular Weight 380.35
Formula

 

C19H14F2N6O
 
CAS No. 1207456-01-6
Storage powder
in solvent
Synonyms LT-673

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02836028 Not yet recruiting Ovarian Cancer Medivation, Inc. October 2016 Phase 2
NCT02567396 Not yet recruiting Estrogen Receptor Negative|Head and Neck Squamous Cell Carcinoma|HER2/Neu Negative|Hormone-Resistant Prostate Cancer|Metastatic Pancreatic Adenocarcinoma|Progesterone Receptor Negative|Solid Neoplasm|Stage III Mesothelioma|Stage IIIA Gastric Cancer|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIA Ovarian Cancer|Stage IIIA Small Cell Lung Carcinoma|Stage IIIB Gastric Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IIIB Ovarian Cancer|Stage IIIB Small Cell Lung Carcinoma|Stage IIIC Gastric Cancer|Stage IIIC Ovarian Cancer|Stage IV Mesothelioma|Stage IV Non-Small Cell Lung Cancer|Stage IV Ovarian Cancer|Stage IV Small Cell Lung Carcinoma|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) July 2016 Phase 1
NCT02627430 Withdrawn Adult Solid Neoplasm|Estrogen Receptor Negative|Fallopian Tube Serous Neoplasm|HER2/Neu Negative|Ovarian Serous Adenocarcinoma|Ovarian Serous Tumor|Primary Peritoneal Serous Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) March 2016 Phase 1
NCT02537561 Withdrawn Solid Tumors|Carcinoma, Non-Small Cell Lung|Non-Small Cell Lung Cancer|Non-Small-Cell Lung Carcinoma|Nonsmall Cell Lung Cancer Washington University School of Medicine|BioMarin Pharmaceutical December 2015 Phase 1
NCT02401347 Recruiting Advanced Breast Cancer|HER2/Neu Negative|Triple-Negative Breast Cancer Melinda Telli|National Cancer Institute (NCI)|Stanford University August 2015 Phase 2
NCT02317874 Recruiting Solid Neoplasm National Cancer Institute (NCI) July 2015 Phase 1

Tech Support

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.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    Which solvent do you recommend to dilute the inhibitor for in vivo study in mice?

  • Answer:

    BMN673 (S7048) can be dissolved in vehicle (10% DMAc, 6% Solutol, and 84% PBS) according to the paper: http://clincancerres.aacrjournals.org/content/19/18/5003.full. Quote from Method and Material section "Xenograft experiments: BMN 673 (various doses as indicated), or vehicle (10% DMAc, 6% Solutol, and 84% PBS) was administered by oral gavage"

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID