| Description | PSB-12379 ditriethylamine salt, a nucleotide analogue, is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human). |
| In vitro | 在所施加的条件下，PSB-12379 (10g) 的代谢率相对较低，小于23%的化合物遭到代谢，而超过77%在8小时的长时间孵化后保持未变。PSB-12379 (10g) 的稳定性稍逊，8小时内有56%的化合物被代谢。观察到主要反应为典型的核苷和核苷酸的第一阶段反应——糖苷键的水解裂解[1]。 |
| molecular weight | 717.73 |
| Molecular formula | C30H53N7O9P2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 11 mg/mL (15.33 mM) |
| References | 1. Bhattarai S, et al. α,β-Methylene-ADP (AOPCP) Derivatives and Analogues: Development of Potent and Selective ecto-5'-Nucleotidase (CD73) Inhibitors. J Med Chem. 2015 Aug 13;58(15):6248-63. 2. X-Ray Co-Crystal Structure Guides the Way to Subnanomolar Competitive Ecto-5 -Nucleotidase (CD73) Inhibitors for Cancer Immunotherapy Sanjay Bhattarai. Adv. Therap. 2019, 2, 1900075. |