| Description | ABBV-CLS-484 (Osunprotafib) is a potent PTPN2 inhibitor with subnanomolar activity and antitumor activity that enhances T-cell anti-tumor immunity.ABBV-CLS-484 can be used for the treatment of neoplasms, esophageal cancer, and digestive disorders. |
| In vitro | ABBV-CLS-484 acts simultaneously on tumor cells and the host immune system, inducing unique transcriptional changes in myeloid and lymphocyte populations in the tumor microenvironment, enhancing the activation and effector functions of CD8+ T cells, while reducing T cell exhaustion and dysfunction. Expression of classical genes.[2] |
| In vivo | ABBV-CLS-484 promotes anti-tumor immunity as a single agent, and when combined with anti-PD-1, results in significant tumor regression, even in models that are resistant to anti-PD-1 treatment, such as 4T1 and EMT6.[3] |
| Synonyms | AC 484, Osunprotafib, AC484, ABBV-CLS-484 |
| molecular weight | 385.45 |
| Molecular formula | C17H24FN3O4S |
| CAS | 2489404-97-7 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 56.2 mg/mL (145.9 mM), Sonication is recommended. |
| References | 1. Philip R, et al. Protein tyrosine phosphatase inhibitors and methods of use thereof. WO2022056281A1. 2. Arvin Iracheta-Vellve, et al. Targeting the immune checkpoint PTPN2 with ABBV-CLS-484 inflames the tumor microenvironment and unleashes potent CD8+ T cell immunity. Cancer Res (2022) 82 (12_Supplement): 606. 3. Christina K, et al. ABBV-CLS-484: An active site PTPN2/N1 inhibitor that augments the immune response and sensitizes tumors to immune-mediated killing. Cancer Res (2022) 82 (12_Supplement): ND06. 4. Baumgartner C K, et al. The PTPN2/PTPN1 inhibitor ABBV-CLS-484 unleashes potent anti-tumour immunity[J]. Nature, 2023: 1-13. |