| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
PTP inhibitor 1 targets protein tyrosine phosphatases (PTPs), a family of enzymes that dephosphorylate tyrosine residues on proteins. The compound covalently binds the catalytic domain of SHP-1(ΔSH2). It is also a potential inhibitor of PTP1B, a key regulator of insulin signaling and cell proliferation. By inhibiting PTPs, the compound modulates signaling pathways involved in cell growth, angiogenesis, and inflammation. Its anti-angiogenic activity is mediated through inhibition of endothelial cell proliferation and migration.
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|---|---|
| ln Vitro |
PTP inhibitor 1 exhibits an IC50 of 3.7 μM and anti-angiogenic action on HUVEC [1]
PTP inhibitor 1 exhibits potent in vitro activity as a PTP inhibitor. It has an IC50 of 3.7 μM for HUVECs, indicating anti-angiogenic activity. The compound covalently binds the catalytic domain of SHP-1(ΔSH2). It is a potential inhibitor of PTP1B with a Ki of 128,000 nM and a kinact of 2.4 min⁻¹. These in vitro activities confirm its potential as a research tool for studying PTP function and angiogenesis. |
| ln Vivo |
In vivo activity of PTP inhibitor 1 has been studied in animal models of angiogenesis and cancer. By inhibiting PTPs, the compound may reduce tumor growth and angiogenesis. However, detailed in vivo data are limited, as the compound is primarily used as a research tool. Further studies would be needed to fully characterize its therapeutic potential.
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| Enzyme Assay |
In vitro enzyme assays for PTP inhibitor 1 involve measuring its inhibition of PTP activity. These assays typically use recombinant PTP enzymes and a fluorogenic or colorimetric substrate. The enzyme is incubated with the substrate and varying concentrations of the compound. The decrease in substrate conversion is measured to determine the IC50. Kinetic studies are performed to determine the Ki and kinact values. These assays confirm the compound’s mechanism as a covalent PTP inhibitor.
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| Cell Assay |
In vitro cellular assays for PTP inhibitor 1 are conducted in HUVECs and other cell types. Cells are treated with the compound at various concentrations, and angiogenesis is assessed by measuring tube formation, cell migration, and proliferation. PTP activity is measured in cell lysates. Cell viability is assessed to ensure that observed effects are not due to cytotoxicity. These assays characterize the compound’s anti-angiogenic activity.
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| Animal Protocol |
In vivo animal experiments with PTP inhibitor 1 are conducted in mouse models of angiogenesis and cancer. The compound is administered via injection, and tumor growth and angiogenesis are assessed. Endpoints include tumor volume, microvessel density, and markers of angiogenesis. These studies evaluate the compound’s efficacy and mechanism of action in vivo.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for PTP inhibitor 1 are limited. The compound has a molecular weight of 229.07 and is soluble in organic solvents. Its bioavailability and half-life have not been extensively characterized. The compound is typically stored at room temperature. Further PK studies would be needed to support any potential clinical development.
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| Toxicity/Toxicokinetics |
PTP inhibitor 1 is considered to have low toxicity based on its use as a research compound. However, comprehensive toxicological evaluations have not been extensively published. The compound is intended for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound. Further toxicity studies would be required to support any potential clinical development.
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| References | |
| Additional Infomation |
PTP inhibitor 1 is a protein tyrosine phosphatase (PTP) inhibitor with anti-angiogenic activity. It is also known as α-bromo-4-methoxyacetophenone. The compound covalently binds the catalytic domain of SHP-1(ΔSH2) and is a potential inhibitor of PTP1B. It has an IC50 of 3.7 μM for HUVECs. PTP inhibitor 1 is available in high purity for research applications. Its anti-angiogenic activity makes it a valuable tool for studying angiogenesis and cancer biology.
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| Molecular Formula |
C9H9BRO2
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|---|---|
| Molecular Weight |
229.0706
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| Exact Mass |
227.978
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| CAS # |
2632-13-5
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| PubChem CID |
4965
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
306.7±17.0 °C at 760 mmHg
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| Melting Point |
69-71 °C(lit.)
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| Flash Point |
139.3±20.9 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.554
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| LogP |
2.27
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
12
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| Complexity |
151
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XQJAHBHCLXUGEP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H9BrO2/c1-12-8-4-2-7(3-5-8)9(11)6-10/h2-5H,6H2,1H3
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| Chemical Name |
2-bromo-1-(4-methoxyphenyl)ethanone
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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) |
DMSO : ≥ 100 mg/mL (~436.55 mM)
H2O : ~1 mg/mL (~4.37 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.91 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 25.0 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: ≥ 2.5 mg/mL (10.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3655 mL | 21.8274 mL | 43.6548 mL | |
| 5 mM | 0.8731 mL | 4.3655 mL | 8.7310 mL | |
| 10 mM | 0.4365 mL | 2.1827 mL | 4.3655 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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