| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
JAK3 38 nM (IC50) JAK2 600 nM (IC50)
JAK3-IN-14 targets JAK3, a member of the Janus kinase family of non-receptor tyrosine kinases that plays a critical role in cytokine signaling through the common gamma chain. JAK3 is primarily expressed in hematopoietic cells and is involved in signaling downstream of IL-2, IL-4, IL-7, IL-9, IL-15, and IL-21 receptors. The compound also inhibits JAK2 with lower potency. |
|---|---|
| ln Vitro |
JAK3-IN-14 demonstrates potent in vitro inhibition of JAK3 with an IC50 of 38 nM. It inhibits IL-4- and IL-3-induced TF-1 cell proliferation with IC50 values of 600 and 500 nM, respectively. The compound's selectivity for JAK3 over JAK2 (approximately 16-fold) makes it a valuable tool for studying JAK3-specific signaling pathways.
|
| ln Vivo |
In vivo activity of JAK3-IN-14 has not been extensively documented. Its potent in vitro inhibition of JAK3 and effects on cytokine-induced cell proliferation suggest potential for in vivo efficacy in models of immune-mediated diseases and cancer. Further in vivo studies are needed to evaluate its pharmacokinetic properties, efficacy, and safety.
|
| Enzyme Assay |
In vitro enzyme assays for JAK3-IN-14 involve measuring its inhibition of JAK3 kinase activity. The assay typically uses purified recombinant JAK3 enzyme and peptide substrates, with kinase activity measured by detecting phosphorylation using radioactive ATP or fluorescence-based methods. IC50 values are determined from dose-response curves.
|
| Cell Assay |
In vitro cellular assays for JAK3-IN-14 involve treating TF-1 cells or other cytokine-dependent cell lines with varying concentrations of the compound in the presence of IL-3 or IL-4. Cell proliferation is assessed using MTT or other assays. JAK3 inhibition is confirmed by measuring STAT5 phosphorylation using Western blotting or flow cytometry.
|
| Animal Protocol |
In vivo animal experiments for JAK3-IN-14 are not extensively documented. If used in animal models, typical protocols would involve administering the compound to models of immune-mediated diseases or cancer and evaluating efficacy by measuring disease progression, immune cell activation, or tumor growth.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for JAK3-IN-14 are limited. The compound has a molecular weight of 287.32 and a molecular formula of C18H13N3O. Powder should be stored at -20°C for up to 3 years and at 4°C for up to 2 years; solutions at -80°C for up to 6 months and at -20°C for up to 1 month. Its ADME properties have not been characterized.
|
| Toxicity/Toxicokinetics |
Toxicological data for JAK3-IN-14 are limited. As a research compound, comprehensive toxicological studies have not been reported. The compound is intended for research use only and is not for human therapeutic application. Standard laboratory safety precautions should be followed when handling this compound.
|
| References | |
| Additional Infomation |
5-(3-pyridyl)-3-(1H-pyrrolo-2-ylmethylene)-1H-indole-2-one is a member of the indole class of compounds.
JAK3-IN-14 (CAS#: 454234-24-3) has the molecular formula C18H13N3O and a molecular weight of 287.32. It is a potent JAK3 inhibitor with an IC50 of 38 nM and also inhibits JAK2 with an IC50 of 600 nM. The compound inhibits cytokine-induced cell proliferation. It is for research use only. |
| Molecular Formula |
C18H13N3O
|
|---|---|
| Molecular Weight |
287.32
|
| Exact Mass |
287.106
|
| CAS # |
454234-24-3
|
| PubChem CID |
9947841
|
| Appearance |
Yellow to orange solid powder
|
| LogP |
3.707
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
22
|
| Complexity |
461
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC(=CN=C1)C2=CC\3=C(C=C2)NC(=O)/C3=C\C4=CC=CN4
|
| InChi Key |
IQNTXIMXKCURDC-YBEGLDIGSA-N
|
| InChi Code |
InChI=1S/C18H13N3O/c22-18-16(10-14-4-2-8-20-14)15-9-12(5-6-17(15)21-18)13-3-1-7-19-11-13/h1-11,20H,(H,21,22)/b16-10-
|
| Chemical Name |
(3Z)-5-pyridin-3-yl-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-2-one
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : 125 mg/mL (435.05 mM)
|
|---|---|
| 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 | 3.4804 mL | 17.4022 mL | 34.8044 mL | |
| 5 mM | 0.6961 mL | 3.4804 mL | 6.9609 mL | |
| 10 mM | 0.3480 mL | 1.7402 mL | 3.4804 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
