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Osunprotafib

CAT: 0804-HY-145923-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-145923-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
Osunprotafib (ABBV-CLS-484) is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2 (IC50: 1.8 nM) inhibitor. Osunprotafib has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction[1][2][3][4].
CAS Number
2489404-97-7
Product Name Alternative
ABBV-CLS-484
UNSPSC
12352005
Target
JAK; Phosphatase; STAT
Type
Reference compound
Related Pathways
Epigenetics; JAK/STAT Signaling; Metabolic Enzyme/Protease; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/osunprotafib.html
Purity
99.43
Solubility
DMSO : 58.33 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
FC1=C(C[C@@H](CC2)NCCC(C)C)C2=CC(O)=C1N3CC(NS3(=O)=O)=O
Molecular Formula
C17H24FN3O4S
Molecular Weight
385.45
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1