Talazoparib [1207456-01-6]

Catalog number: HY-16106_200mg
Brand: MedChem Express
Packing: 200 mg
Other sizes: 5 mg
10 mM
10 mg
50 mg
100 mg
Price: € 565.00
Expected delivery time: 10 days

Product specifications for - Talazoparib [1207456-01-6]

Product group: Chemicals
Category: Other
CAS No.: 1207456-01-6
Purity: >98%
Molecular Formula: C19H14F2N6O
Molecular weight: 380.35
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: BMN-673 is a novel PARP1/2 inhibitor with IC50 of 0.57 nM for PARP1. IC50 & Target: IC50: 0.57 nM (PARP1)[1] Ki: 1.2/0.87 nM (PARP1/2)[1] In Vitro: BMN-673 demonstrates excellent potency, inhibiting PARP1 and PARP2 enzyme activity with Ki=1.2 and 0.87 nM, respectively[1]. BMN 673 exhibits selective antitumor cytotoxicity and elicits DNA repair biomarkers at much lower concentrations than earlier generation PARP1/2 inhibitors (such as Olaparib, Rucaparib, and Veliparib)[2]. In Vivo: BMN-673 (1 mg/kg, p.o.) is orally available, displaying favorable pharmacokinetic (PK) properties and remarkable antitumor efficacy in the BRCA1 mutant MX-1 breast cancer xenograft model following oral administration as a single-agent or in combination with chemotherapy agents such as temozolomide and cisplatin[1]. BMN 673 is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in carboxylmethyl cellulose. Oral administration of BMN 673 elicits remarkable antitumor activity, xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency are profoundly sensitive to oral BMN 673 treatment at well-tolerated doses in mice[2].
Safety information: 
PARP inhibitors enhance replication stress and cause mitotic catastrophe in MYCN-dependent neuroblastoma', Colicchia V. Oncogene. 2017 Aug 17;36(33):4682-4691. Read more
Ubiquitin Modification by the E3 Ligase/ADP-Ribosyltransferase Dtx3L/Parp9', Yang CS. Mol Cell. 2017 May 18;66(4):503-516.e5. Read more