For research use only. Not for therapeutic Use.
Osunprotafib (ABBV-CLS-484) is a potent PTPN1 and PTPN2 inhibitor with subnanomolar activity. Osunprotafib has antitumor activity, enhances the immune response and increases the sensitivity of tumors to immune-mediated killing[1].
Osunprotafib acts on both tumor cells and the host immune system, inducing unique transcriptional changes in the myeloid and lymphocyte populations of the tumor microenvironment, enhancing CD8+ T cell activation and effector functions while reducing the expression of genes classically associated with T cell depletion and dysfunction[2].
Osunprotafib promotes anti-tumor immunity as a monotherapy and, when combined with anti-PD-1, leads to significant tumor regression, even in models resistant to anti-PD-1 treatment, such as 4T1 and EMT6[3].
| Catalog Number | I043970 |
| CAS Number | 2489404-97-7 |
| Synonyms | 5-[(7R)-1-fluoro-3-hydroxy-7-(3-methylbutylamino)-5,6,7,8-tetrahydronaphthalen-2-yl]-1,1-dioxo-1,2,5-thiadiazolidin-3-one |
| Molecular Formula | C17H24FN3O4S |
| Purity | ≥95% |
| InChI | InChI=1S/C17H24FN3O4S/c1-10(2)5-6-19-12-4-3-11-7-14(22)17(16(18)13(11)8-12)21-9-15(23)20-26(21,24)25/h7,10,12,19,22H,3-6,8-9H2,1-2H3,(H,20,23)/t12-/m1/s1 |
| InChIKey | DVFCRTGTEXUFIN-GFCCVEGCSA-N |
| SMILES | CC(C)CCNC1CCC2=CC(=C(C(=C2C1)F)N3CC(=O)NS3(=O)=O)O |
| Reference | [1]. Philip R. Kym, 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. |
