Talazoparib CAS# 1207456-01-6 他拉唑帕利
Talazoparib, also known as BMN-673 and MDV-3800, is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity (PARP1 IC50 = 0.57 nmol/L). Talazoparib acts as an inhibitor of poly ADP ribose polymerase(PARP) which aids in single strand DNA repair. Cells that have BRCA1/2 mutations are susceptible to the cytotoxic effects of PARP inhibitors because of an accumulation of DNA damage. Talazoparib is theorized to have a higher potency than olaparib due to the additional mechanism of action called PARP trapping. PARP trapping is the mechanism of action where the PARP molecule is trapped on the DNA, which interferes with the cells ability to replicate. Talazoparib is found to be ~100 fold more efficient in PARP trapping than olaparib
📌 参考资料/链接：
Reference: Wang, Bing; Chu, Daniel; Feng, Ying; Shen, Yuqiao; Aoyagi-Scharber, Mika; Post, Leonard E. Journal of Medicinal Chemistry. 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. Journal of Medicinal Chemistry. Volume 59. Issue 1. Pages 335-357. Journal; Online Computer File. (2016).
Reference: Wang, Bing; Chu, Daniel; Feng, Ying; Shen, Yuqiao; Aoyagi-Scharber, Mika; Post, Leonard E. Journal of Medicinal Chemistry. 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. Journal of Medicinal Chemistry. Volume 59. Issue 1. Pages 335-357. Journal; Online Computer File. (2016).
📄 详细内容
CAS No. 1207456-01-6 他拉唑帕利Talazoparib synthetic routes
Wang, Bing; Chu, Daniel; Feng, Ying; Shen, Yuqiao; Aoyagi-Scharber, Mika; Post, Leonard E. Journal of Medicinal Chemistry. 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. Journal of Medicinal Chemistry. Volume 59. Issue 1. Pages 335-357. Journal; Online Computer File. (2016).
产品链接: CAS No. 1207456-01-6 ››
Wang, Bing; Chu, Daniel; Feng, Ying; Shen, Yuqiao; Aoyagi-Scharber, Mika; Post, Leonard E. Journal of Medicinal Chemistry. 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. Journal of Medicinal Chemistry. Volume 59. Issue 1. Pages 335-357. Journal; Online Computer File. (2016).
产品链接: CAS No. 1207456-01-6 ››