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| Targets |
JAK2 JH2 Tracer targets the JH2 pseudokinase domain of the JAK2 kinase. JAK2 is a member of the Janus kinase family of non-receptor tyrosine kinases that plays a critical role in cytokine and growth factor signaling. The JH2 domain is a regulatory domain that modulates the activity of the adjacent JH1 kinase domain. The tracer binds specifically to the JH2 domain with a Kd of 0.2 microM, enabling the study of JAK2-inhibitor interactions.
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| ln Vitro |
The JAK2 JH2 Tracer indicates that 1.5 pM is the lowest tracer concentration needed to maintain a good signal-to-noise ratio [1]. JAK2 JH2 Tracer exhibits a dissociation constant that is nearly equal to 0.2 μM [1]. JAK2 JH2 Tracer demonstrates a strong binding affinity to the JAK2 JH2 domain during saturation assays, as evidenced by a Kd value of 0.2 μM [1].
In vitro, JAK2 JH2 Tracer is a fluorescent probe for the JAK2 JH2 domain with a Kd of 0.2 microM. It is used to detect or quantify JAK2-inhibitor interactions in screening and mechanistic studies. The tracer's fluorescent properties allow for the monitoring of binding events in real-time using fluorescence-based assays, such as fluorescence polarization or FRET. Its high affinity for the JH2 domain makes it a valuable tool for studying JAK2 pharmacology. |
| ln Vivo |
In Drosophila, hematological malignancy traits and pathologies linked to hyperactive kinases may be linked to mutations in the JAK2 JH2 domain [2]. ?Myeloproliferative disorders in general are linked to specific mutations in the JH2 domain of JAK2 [2].
In vivo studies of JAK2 JH2 Tracer are not typically performed, as it is primarily used as an in vitro research tool for binding studies. As a fluorescent probe, its application is generally confined to biochemical and cell-based assays. The tracer could potentially be used in vivo for imaging applications, but such studies are not currently reported. |
| Enzyme Assay |
For in vitro enzyme/receptor binding assays, JAK2 JH2 Tracer is used as a fluorescent probe to measure binding to the JAK2 JH2 domain. The tracer is incubated with recombinant JAK2 JH2 domain protein or full-length JAK2 at various concentrations. Binding is quantified using fluorescence-based methods such as fluorescence polarization, FRET, or microscale thermophoresis. Kd values are determined from binding curves. Competition binding assays can be performed using unlabeled test compounds to determine their affinity for the JH2 domain.
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| Cell Assay |
For in vitro cellular experiments, JAK2 JH2 Tracer can be used in cell-based assays to study JAK2-inhibitor interactions in a cellular context. Cells expressing JAK2 are treated with the tracer, and binding is assessed using fluorescence microscopy, flow cytometry, or other fluorescence-based detection methods. The tracer's cellular uptake and localization can also be studied. Competition experiments with JAK2 inhibitors can be performed to assess their cellular activity.
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| Animal Protocol |
For in vivo animal experiments, JAK2 JH2 Tracer is not typically administered to animals, as it is primarily used as an in vitro research tool. However, it could potentially be used for in vivo imaging applications to study JAK2 expression or inhibitor distribution in animal models. Such studies would require optimization of the tracer's pharmacokinetic properties and imaging conditions.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of JAK2 JH2 Tracer are not relevant, as it is used as a research probe rather than a therapeutic agent. The tracer is not administered to animals or humans for therapeutic purposes. Its stability and fluorescence properties are important for its use in binding assays. The compound is soluble in DMSO at ≥83.3 mg/mL and should be stored appropriately.
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| Toxicity/Toxicokinetics |
Toxicological data for JAK2 JH2 Tracer are limited, as it is used as a research probe rather than a therapeutic agent. The compound is generally considered to have low toxicity for in vitro use. However, as with all research chemicals, appropriate safety precautions should be taken when handling the compound, including the use of personal protective equipment and adherence to institutional safety guidelines.
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| References | |
| Additional Infomation |
JAK2 JH2 Tracer is a research compound used to study JAK2-inhibitor interactions. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The tracer is a fluorescent probe for the JAK2 JH2 domain with a Kd of 0.2 microM.
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| Molecular Formula |
C38H27F2N7O6S
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|---|---|
| Molecular Weight |
747.726093530655
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| Exact Mass |
747.171
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| CAS # |
2101955-00-2
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| PubChem CID |
131704489
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| Appearance |
Light brown to brown solid powder
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| LogP |
6.6
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
54
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| Complexity |
1360
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S=C(N(C)CC1C=CC(=CC=1)NC1N=C(N)N(C(C2C(=CC=CC=2F)F)=O)N=1)NC1C=CC2=C(C=1)C(=O)OC12C2C=CC(=CC=2OC2C=C(C=CC1=2)O)O
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| InChi Key |
OAJQEPALUDJGLJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C38H27F2N7O6S/c1-46(18-19-5-7-20(8-6-19)42-36-44-35(41)47(45-36)33(50)32-28(39)3-2-4-29(32)40)37(54)43-21-9-12-25-24(15-21)34(51)53-38(25)26-13-10-22(48)16-30(26)52-31-17-23(49)11-14-27(31)38/h2-17,48-49H,18H2,1H3,(H,43,54)(H3,41,42,44,45)
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| Chemical Name |
1-[[4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]phenyl]methyl]-3-(3',6'-dihydroxy-3-oxospiro[2-benzofuran-1,9'-xanthene]-5-yl)-1-methylthiourea
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ≥ 83.3 mg/mL (~111.40 mM)
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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 | 1.3374 mL | 6.6869 mL | 13.3738 mL | |
| 5 mM | 0.2675 mL | 1.3374 mL | 2.6748 mL | |
| 10 mM | 0.1337 mL | 0.6687 mL | 1.3374 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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