| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Osunprotafib targets protein tyrosine phosphatase non-receptor type 2 (PTPN2) and PTPN1. It acts as an active-site inhibitor. By inhibiting PTPN2 and PTPN1, it enhances JAK-STAT signaling and reduces T cell dysfunction, thereby stimulating the tumor microenvironment and promoting natural killer cell and CD8 T cell function. This enhances T cell anti-tumor immunity.
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|---|---|
| ln Vitro |
By stimulating a distinct activation of myeloid cells in the tumor microenvironment and directly improving the activation and effector functions of CD8+ T cells, osunprotafib acts on tumor cells as well as the immune system. This reduces the traditional symptoms linked to T-depletion cell depletion and dysfunction. expression of genes [2].
In vitro, Osunprotafib inhibits PTPN2 and PTPN1 with IC50 values of 1.8 nM and 2.5 nM, respectively. It enhances the sensitivity of tumor cells to IFNγ and promotes T cell activation and function. The compound shows potent anti-tumor activity through immune modulation. |
| ln Vivo |
Osunprotafib enhances anti-tumor immunity as a single drug, and when combined with anti-PD-1, tumors markedly retreat, even in models resistant to anti-PD-1 treatment, such as 4T1 and EMT6 [3].
In vivo activity data for Osunprotafib are not extensively detailed in the available sources. The compound is in clinical trials for solid tumors. It stimulates the tumor microenvironment and promotes natural killer cell and CD8 T cell function, enhancing T cell anti-tumor immunity. |
| Enzyme Assay |
The in vitro enzyme assay for Osunprotafib involves measuring the inhibition of PTPN2 and PTPN1 phosphatase activity. Recombinant enzymes are incubated with a phosphopeptide substrate in the presence of varying compound concentrations. The IC50 values are determined by quantifying the reduction in phosphate release using colorimetric or fluorescence-based assays.
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| Cell Assay |
Cellular assays are performed using tumor cells and T cells. Tumor cells are treated with Osunprotafib, and IFNγ sensitivity is assessed by measuring cell viability or MHC class I expression. T cell activation and function are evaluated by measuring cytokine production (e.g., IFNγ, TNFα) and proliferation.
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| Animal Protocol |
In vivo animal studies for Osunprotafib are not detailed in the available sources. The compound is in clinical trials for solid tumors. Specific animal models and dosing regimens are not described.
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| ADME/Pharmacokinetics |
Osunprotafib is an orally active compound. It is in clinical trials, indicating favorable pharmacokinetic properties. Specific PK parameters such as half-life, bioavailability, and clearance are not detailed in the available sources.
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| Toxicity/Toxicokinetics |
Toxicity data for Osunprotafib are not reported in the available sources. As an investigational compound in clinical trials, it has been evaluated for safety, but specific toxicological profiles are not available.
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| References | |
| Additional Infomation |
Osunprotafib is an orally bioavailable T-cell-specific tyrosine protein phosphatase non-receptor type 2 (PTPN2) inhibitor with potential immunomodulatory and antitumor activities. After oral administration, Osunprotafib specifically targets and binds to PTPN2, thereby blocking PTPN2-mediated signal transduction pathways and potentially activating antitumor T-cell immune responses. Furthermore, it may enhance the sensitivity of tumor cells to immunotherapy. PTPN2 negatively regulates T-cell receptor (TCR) and cytokine signaling, which are crucial for T-cell function, homeostasis, and differentiation.
Osunprotafib is an investigational immuno-oncology agent in clinical trials for solid tumors. It is a first-in-class PTPN2/PTPN1 inhibitor with a novel mechanism of action that enhances anti-tumor immunity. The compound is available for research purposes. |
| Molecular Formula |
C17H24FN3O4S
|
|---|---|
| Molecular Weight |
385.45
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| Exact Mass |
385.147
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| CAS # |
2489404-97-7
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| PubChem CID |
155103607
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| Appearance |
Off-white to light yellow solid powder
|
| LogP |
2.1
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
26
|
| Complexity |
624
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C1[C@H](NCCC(C)C)CCC2=CC(O)=C(N3S(=O)(=O)NC(=O)C3)C(F)=C12
|
| InChi Key |
DVFCRTGTEXUFIN-GFCCVEGCSA-N
|
| InChi Code |
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
|
| Chemical Name |
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
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~162.15 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5944 mL | 12.9719 mL | 25.9437 mL | |
| 5 mM | 0.5189 mL | 2.5944 mL | 5.1887 mL | |
| 10 mM | 0.2594 mL | 1.2972 mL | 2.5944 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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