| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
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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].
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|---|---|
| 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].
|
| References | |
| Additional Infomation |
Osunprotafib is an orally bioavailable inhibitor of the T-cell specific tyrosine-protein phosphatase non-receptor type 2 (PTPN2), with potential immunomodulating and antineoplastic activities. Upon oral administration, osunprotafib specifically targets and binds to PTPN2. This prevents PTPN2-mediated signal transduction pathways and may activate anti-tumor T-cell immune responses. It may also sensitize tumor cells to immunotherapeutics. PTPN2 negatively regulates TCR and cytokine signaling needed for T cell function, homeostasis and differentiation.
|
| Molecular Formula |
C17H24FN3O4S
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|---|---|
| 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
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
624
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| Defined Atom Stereocenter Count |
1
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| 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
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| 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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