Osunprotafib (hydrochloride)

Osunprotafib (ABBV-CLS-484) hydrochloride is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2 (IC50: 1.8 nM) inhibitor. Osunprotafib hydrochloride has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib hydrochloride increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib hydrochloride generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction[1][2][3][4].

Product Specifications

CAS Number

[2986745-48-4]

Product Name Alternative

ABBV-CLS-484 (hydrochloride)

UNSPSC

12352005

Target

JAK; Phosphatase; STAT

Related Pathways

Epigenetics; JAK/STAT Signaling; Metabolic Enzyme/Protease; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Field of Research

Cancer; Inflammation/Immunology

Smiles

O=C(CN1C2=C(C=C3CC[C@@H](NCCC(C)C)CC3=C2F)O)NS1(=O)=O.Cl

Molecular Formula

C17H25ClFN3O4S

Molecular Weight

421.91

References & Citations

[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.|[4]Baumgartner CK, et al. The PTPN2/PTPN1 inhibitor ABBV-CLS-484 unleashes potent anti-tumour immunity. Nature. 2023 Oct;622 (7984) :850-862.