Osunprotafib hydrochloride  (Synonyms: ABBV-CLS-484 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].

421.91

C₁₇H₂₅ClFN₃O₄S

2986745-48-4

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]