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Osunprotafib (ABBV-CLS-484) is a potent, orally bioavailable PTP1B/PTPN2 inhibitor in clinical trials for solid tumors. [1] Osunprotafib (ABBV-CLS-484) stimulates the tumor microenvironment and promotes natural killer cell and CD8 T cell function and enhances T cell anti-tumor immunity by enhancing JAK-STAT signaling and reducing T cell dysfunction. [2]

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $455 | In Stock | In Stock | |
| 5 mg | $1,360 | In Stock | In Stock | |
| 10 mg | $2,150 | In Stock | In Stock | |
| 25 mg | $3,730 | In Stock | In Stock | |
| 50 mg | $4,930 | In Stock | In Stock |
| Description | Osunprotafib (ABBV-CLS-484) is a potent, orally bioavailable PTP1B/PTPN2 inhibitor in clinical trials for solid tumors. [1] Osunprotafib (ABBV-CLS-484) stimulates the tumor microenvironment and promotes natural killer cell and CD8 T cell function and enhances T cell anti-tumor immunity by enhancing JAK-STAT signaling and reducing T cell dysfunction. [2] |
| Targets&IC50 | PTP1N:2.5 nM, PTP2N:1.8 nM, PTPN2/PTPN1:0.176 μM (EC50) |
| In vitro | Osunprotafib (ABBV-CLS-484) dose-dependently increased STAT5 phosphorylation to similar levels in whole blood from healthy donors and cancer patients; Osunprotafib (ABBV-CLS-484) increased IFNγ-induced STAT1 phosphorylation and CXCL10 production in blood samples from healthy donors and cancer patients, suggesting that Osunprotafib (ABBV-CLS-484)-enhanced pathway engagement leads to enhanced downstream functional effects; Osunprotafib (ABBV-CLS-484) increased T cell activation and function in human whole blood, as indicated by dose-dependent increases in CD69 expression and IFNγ and TNF production after TCR stimulation; Osunprotafib (ABBV-CLS-484) inhibition of PTPN2/N1 enhances human immune cell activation. [2] |
| In vivo | METHODS: Mice with systemic Ptpn2 deletion were administered oral doses of Osunprotafib (ABBV-CLS-484) at 3/10/100 mg/kg twice daily in an attempt to determine whether oral systemic inhibition of PTPN2/N1 could be a safe and effective immunotherapy RESULTS Circulating chemokines, including CXCL10 and CXCL9, increased 2-3-fold at a dose of 10 mg kg-1 twice daily; a dose of 100 mg/kg twice daily resulted in significant Systemic immune activation, manifested by significant increases in circulating cytotoxic granzyme B (GZMB) CD8 T cells and cytokines such as CXCL10 and CXCL9. METHODS: Animals with tumors were evaluated at doses of 50, 100, and 150 mg/kg-1 once daily and significant changes in body condition score or body weight were observed. RESULTS No significant changes in body weight were observed with Osunprotafib (ABBV-CLS-484), which was tolerated in naive rats at doses up to 300 mg kg-1/day for 28 days. The most notable finding was a dose-dependent infiltration of immune cells in the kidneys, joints and liver, and it was also found that Osunprotafib (ABBV-CLS-484) has a relatively short half-life, allowing for rapid discontinuation of treatment, and thus faster than antibody-based therapies. effectively resolve inflammatory conditions. [2] |
| Synonyms | Osunprotafib, AC484, AC 484, ABBV-CLS-484 |
| Molecular Weight | 385.45 |
| Formula | C17H24FN3O4S |
| Cas No. | 2489404-97-7 |
| Smiles | CC(C)CCN[C@@H]1CCc2cc(O)c(N3CC(=O)NS3(=O)=O)c(F)c2C1 |
| Storage | keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 19 mg/mL (49.29 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1.5 mg/mL (3.89 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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