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Talazoparib
- BMN 673 - LT 00673
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C19H14F2N6O
- MW: 380.35
Description
Talazoparib (BMN 673) is a highly potent, selective and orally available PARP1/2 inhibitor with an IC50 value of 0.57 nM for PARP1. Talazoparib is recognized as one of the most potent PARP inhibitors reported and exhibits substantially greater antitumor activity than earlier-generation PARP inhibitors.
PARP1 and PARP2 are key mediators of DNA damage repair and genome stability. Inhibition of PARP activity results in the accumulation of DNA damage and has become a widely used strategy for studying synthetic lethality in tumors with homologous recombination repair deficiencies. Talazoparib demonstrates exceptional potency against tumor cells harboring BRCA1, BRCA2, or PTEN defects and has shown 20- to more than 200-fold greater cytotoxic potency than earlier-generation PARP inhibitors. In addition to catalytic PARP inhibition, Talazoparib is widely recognized for its potent PARP-trapping activity, making it an important tool for investigating DNA repair mechanisms, replication stress, and cancer cell vulnerability.
Key Features
- Highly potent and selective PARP1/2 inhibitor
- IC50: 0.57 nM for PARP1
- Orally available small molecule
- Potent inducer of synthetic lethality in DNA repair-deficient cells
- Widely used tool for BRCA-deficient cancer research
Applications
- PARP1/2 and DNA repair research
- Synthetic lethality studies
- BRCA1-, BRCA2-, and PTEN-deficient cancer models
- Genome stability and replication stress investigations
- Cancer biology and oncology research
Related Products
Researchers interested in PARP biology may also consider Olaparib (Axon 1464), a widely used PARP1/2 inhibitor for DNA repair and synthetic lethality studies, and KU-0058948 hydrochloride (Axon 2001), a potent PARP1-selective inhibitor useful for investigating PARP-dependent signaling pathways.
More Information
| Parent CAS No. | 1207456-01-6 |
|---|---|
| Chemical Name | (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one |
| SMILES | C1(=O)C2=C3C(N[C@H](C4=CC=C(F)C=C4)[C@@H](C4N(C)N=CN=4)C3=NN1)=CC(F)=C2 |&1:6,14,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C19H14F2N6O/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/h2-8,15-16,24H,1H3,(H,26,28)/t15-,16-/m1/s1 |
| InChiKey | HWGQMRYQVZSGDQ-HZPDHXFCSA-N |
| CID | 135565082 |
| Short Description | PARP inhibitor |
References
- M.A. Smith et al. Synergistic activity of PARP inhibition by talazoparib (BMN 673) with temozolomide in pediatric cancer models in the pediatric preclinical testing program. Clin Cancer Res. 2015 Feb 15;21(4):819-32.
- Y. Shen 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.
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