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Description: Talazoparib (formerly BMN-673 and MDV-3800; trade name: Talzenna), is a novel, highly potent and orally bioavailable PARP1/2 poly(ADP-ribose) polymerase inhibitor approved for cancer treatment. It has favorable metabolic stability, oral bioavailability, and pharmacokinetic properties. As a novel PARP inhibitor, Talazoparib has an IC50 of 0.58 nM in a cell-free assay. It 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. On Oct 16 2018, Talazoparib was approved by the US FDA for the treatment of locally advanced or metastatic breast cancer patients with a germline BRCA mutation.
References: Clin Cancer Res. 2013 Sep 15; 19(18):5003-15; Clin Cancer Res. 2014 Apr 15; 20(8):2237.
Related CAS: 1373431-65-2 (tosylate); 1207454-56-5; 1207456-00-5 (racemic mixture); 1207456-01-6 (free base)
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 Code: O=C1NN=C2C3=C1C=C(F)C=C3N[CH](C4=CC=C(F)C=C4)[CH]2C5=NC=NN5C
Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.
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