(rac)-Talazoparib
(rac)-Talazoparib ((rac)-BMN-673) (Compound 47) is the orally active inhibitor for PARP1/2 with Ki of 1.2 nM and 0.87 nM. (rac)-Talazoparib inhibits cellular PARylation with an EC50 of 2.51 nM. (rac)-Talazoparib causes the accumulation of DNA damage, inhibits proliferation of BRCA1/2-mutated MX-1 cell and Capan-1 cell with IC50 of 0.3 nM and 5 nM. (rac)-Talazoparib exhibits antitumor efficacy in mouse models.
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- CAS No.: 1207454-56-5
- Formule: C19H14F2N6O
- Masse moléculaire:380.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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PARP2 0.87 nM (Ki) |
PARP1 1.2 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CAPAN-1 | EC50 |
0.008 μM
Compound: 47
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Cytotoxicity against BRCA2-deficient human Capan1 cells
Cytotoxicity against BRCA2-deficient human Capan1 cells
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[PMID: 26652717] |
| LoVo | EC50 |
5.48 nM
Compound: 47
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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
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[PMID: 26652717] |
| LoVo | GI50 |
19 μM
Compound: 47
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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
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[PMID: 26652717] |
Chemical Information
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CAS No. 1207454-56-5
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Masse moléculaire 380.35
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Formule C19H14F2N6O
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SMILES
O=C1NN=C2C(C(NC3=CC(F)=CC1=C32)C4=CC=C(C=C4)F)C5=NC=NN5C
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Synonyms
(rac)-BMN-673; (rac)-LT-673
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(rac)-Talazoparib Related Classifications
HY-14687 Related Classifications
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