Home JAK/STAT JAK inhibitor Selective JAK3 inhibitor 1

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Selective JAK3 inhibitor 1 JAK inhibitor

Cat.No.S8684

Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK.
Selective JAK3 inhibitor 1 JAK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 350.37

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Quality Control

Batch: S868401 DMSO]70 mg/mL]false]Ethanol]9 mg/mL]false]Water]Insoluble]false Purity: 99.71%
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99.71

Solubility

In vitro
Batch:

DMSO : 70 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 9 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 350.37 Formula

C19H18N4O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1443235-95-7 -- Storage of Stock Solutions

Synonyms N/A Smiles CCOC(=O)C1=CNC2=NC=NC(=C12)C3=CC(=CC=C3)NC(=O)C(=C)C

Mechanism of Action

Targets/IC50/Ki
JAK3
(Cell-free assay)
0.07 nM(Ki)
JAK1
(Cell-free assay)
320 nM(Ki)
JAK2
(Cell-free assay)
740 nM(Ki)
In vitro

Selective JAK3 inhibitor 1 is a potent inhibitor of JAK3 (IC50 = 0.15 nM) and was 4300-fold selective for JAK3 over JAK1 in enzyme assays, 67-fold [interleukin (IL)-2 versus IL-6] or 140-fold [IL-2 versus erythropoietin or granulocyte-macrophage colony-stimulating factor (GMCSF)] selective in cellular reporter assays and >35-fold selective in human peripheral blood mononuclear cell assays (IL-7 versus IL-6 or GMCSF). This compound blocks cytokine signaling through JAK3, but not through other JAK family enzymes. It inhibits IL-7, IL-15, and IL-2 signaling in T cells, but does not inhibit any other cytokine signaling pathways.
In vivo

Selective JAK3 inhibitor 1 has a partial effect on reversing inflammation and bone loss in the rat CIA model when administered therapeutically during the inflammatory phase of the model at doses that meet or exceed the exposure required for complete inhibition of the phenotype when dosed prophylactically. It inhibits leukocyte proliferation, but not erythrocyte proliferation in rats. This compound could fully inhibit the development of inflammation.
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