| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
PTPN2 (protein tyrosine phosphatase non-receptor type 2) and PTPN1 (protein tyrosine phosphatase non-receptor type 1). PTPN2/1-IN-2 is an antagonist of both enzymes, modulating immune responses and cellular processes related to inflammation.
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| ln Vitro |
PTPN2/1-IN-2 is an antagonist (inhibitor) of the phosphatases PTPN2 and PTPN1. By inhibiting these enzymes, it modulates immune cell signaling pathways. Inhibition of PTPN2/N1 is a potent strategy to enhance anti-tumor immunity, offering significant potential for cancer immunotherapy, both as a monotherapy and in combination with anti-PD-1 therapy.
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| ln Vivo |
In vivo, PTPN2/1-IN-2 has not been specifically described in the search results, but the class of PTPN2/1 inhibitors has demonstrated in vivo efficacy in animal models of cancer. They function by promoting the activation and proliferation of cytotoxic T cells within the tumor microenvironment, leading to enhanced tumor control. They are being investigated as novel immunotherapies.
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| Enzyme Assay |
For non-cellular assays, the activity of recombinant PTPN2 or PTPN1 is measured using a fluorogenic phospho-tyrosine peptide substrate (e.g., DiFMUP). The enzyme is incubated with the substrate in an assay buffer. PTPN2/1-IN-2 is added at varying concentrations (1-1000 nM). The dephosphorylation of the substrate leads to an increase in fluorescence, which is measured to determine the inhibitory activity. IC50 values for each enzyme are calculated from dose-response curves.
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| Cell Assay |
For cell-based assays, primary immune cells (e.g., T cells or dendritic cells) are treated with PTPN2/1-IN-2 (0.1-10 uM) for 24-72 hours. T cell activation and proliferation are measured by flow cytometry using markers such as CD69, CD25, and Ki-67, or by CFSE dilution. Cytokine production (e.g., IFN-gamma, TNF-alpha, IL-2) is measured by ELISA or intracellular cytokine staining. The phosphorylation status of key signaling molecules (e.g., JAK, STAT) is assessed by Western blot.
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| Animal Protocol |
For animal studies, PTPN2/1-IN-2 can be administered intraperitoneally or orally to syngeneic mouse tumor models (e.g., MC38 colon carcinoma, B16-F10 melanoma). Doses are typically in the range of 10-50 mg/kg, given daily or every other day. Tumor growth is monitored over time. The compound can be evaluated as a monotherapy or in combination with checkpoint inhibitors (e.g., anti-PD-1). T cell infiltration and activation in the tumor microenvironment are assessed by flow cytometry and immunohistochemistry at the end of the study.
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| ADME/Pharmacokinetics |
PTPN2/1-IN-2 has a molecular weight of 398.41 g/mol and a molecular formula of C17H19FN2O6S. It is soluble in DMSO (100 mg/mL). The compound can be formulated in a vehicle such as 0.5% methylcellulose or a mixture of DMSO/PEG300/Tween-80/saline for oral administration. It is stored as a powder at -20degC, protected from light and under nitrogen, and in solution at -80degC for up to 6 months.
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| Toxicity/Toxicokinetics |
Toxicological data for PTPN2/1-IN-2 are not detailed in the available literature. As an investigational research compound targeting immune checkpoints, it is intended for research use only and is not for human use. Standard safety precautions for handling research chemicals should be followed. Material safety data sheets (MSDS) for the compound may be available for safety information.
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| References | |
| Additional Infomation |
PTPN2/1-IN-2 is a chemical probe for studying the PTPN2 and PTPN1 phosphatases. These enzymes are intracellular immune checkpoints that suppress anti-tumor immunity. Preclinical studies have shown that PTPN2/1 inhibitors can enhance the efficacy of existing cancer immunotherapies and may even be effective as monotherapies in some tumor models. The compound is not an FDA-approved drug.
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| Molecular Formula |
C17H19FN2O6S
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|---|---|
| Molecular Weight |
398.41
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| Exact Mass |
398.094
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| CAS # |
2407611-02-1
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| PubChem CID |
155103226
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
1.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
667
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(OCCC(C)(O)C)C=C2C(=CC=1)C=C(O)C(N1CC(NS1(=O)=O)=O)=C2F
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| InChi Key |
KJYRSQLWJMEJNM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H19FN2O6S/c1-17(2,23)5-6-26-11-4-3-10-7-13(21)16(15(18)12(10)8-11)20-9-14(22)19-27(20,24)25/h3-4,7-8,21,23H,5-6,9H2,1-2H3,(H,19,22)
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| Chemical Name |
5-[1-fluoro-3-hydroxy-7-(3-hydroxy-3-methylbutoxy)naphthalen-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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5100 mL | 12.5499 mL | 25.0998 mL | |
| 5 mM | 0.5020 mL | 2.5100 mL | 5.0200 mL | |
| 10 mM | 0.2510 mL | 1.2550 mL | 2.5100 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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