| Description | Talabostat mesylate (PT100) is an orally active, selective inhibitor of dipeptidyl peptidases IV (DPP4, IC50: 0.18 nM), including tumor-associated fibroblast activation protein. This agent may also stimulate the production of colony stimulating factors, such as granulocyte colony-stimulating factor (G-CSF), resulting in the stimulation of hematopoiesis. |
| Target activity | DPP4:0.18 nM |
| Synonyms | Val-boroPro, PT100 |
| molecular weight | 310.18 |
| Molecular formula | C10H23BN2O6S |
| CAS | 150080-09-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 60 mg/mL (193.44 mM) 5% DMSO+95% Saline: 2 mg/mL (6.45 mM) |
| References | 1. Cristillo AD, et al. HIV-1 Env vaccine comprised of electroporated DNA and protein co-administered with Talabostat. Biochem Biophys Res Commun. 2008 May 23;370(1):22-6. 2. Huang Y., et al. Fibroblast activation protein-α promotes tumor growth and invasion of breast cancer cells through non-enzymatic functions. Clin Exp Metastasis. 2011 Aug;28(6):567-79. 3. Meany H, et al. Pediatric phase I trial design using maximum target inhibition as the primary endpoint. J Natl Cancer Inst. 2010 Jun 16;102(12):909-12. |
| Citations | 1. Luo Y, Zeng Z, Shan T, et al. Fibroblast activation protein α activatable theranostic pro-photosensitizer for accurate tumor imaging and highly-specific photodynamic therapy. Theranostics. 2022, 12(8): 3610 |