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Talazoparib
- BMN 673 - LT 00673
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C19H14F2N6O
- MW: 380.35
Description
Potent, selective, and orally available PARP1/2 inhibitor (IC50 value 0.57 nM for PARP1) that shows antitumor cytotoxicity with 20- to more than 200-fold greater potency than earlier-generation PARP1/2 inhibitors and with selectivity for tumor cells with BRCA1, BRCA2, or PTEN gene defects.
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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