Selective JAK3 inhibitor 1 - 99%, high purity , CAS No.1443235-95-7

  • ≥99%
Item Number
S414115
Grouped product items
SKUSizeAvailabilityPrice Qty
S414115-5mg
5mg
In stock
$199.90
S414115-25mg
25mg
In stock
$686.90
S414115-50mg
50mg
In stock
$1,098.90
S414115-100mg
100mg
In stock
$1,647.90

JAK3 Selective Inhibitors

Basic Description

Specifications & Purity≥99%
Biochemical and Physiological MechanismsSelective 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, I
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Product Description

Information

Selective JAK3 inhibitor 1 is an irreversibleJAK3inhibitor 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.


Targets

JAK3 (Cell-free assay); JAK1 (Cell-free assay); JAK2 (Cell-free assay) 0.07 nM(Ki); 320 nM(Ki); 740 nM(Ki)


In vitro

Selective JAK3 inhibitor 1 is a potent inhibitor of JAK3 (IC50 = 0.15 nM) 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). The 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.

Product Properties

ALogP2.959
HBD Count2
Rotatable Bond6

Associated Targets(Human)

JAK3 Tclin Tyrosine-protein kinase JAK3 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK3 Tclin Tyrosine-protein kinase JAK3 (8349 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
JAK3 Tclin JAK3/JAK1 (270 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Jak1 Tyrosine-protein kinase JAK1/JAK3 (5 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name ethyl 4-[3-(2-methylprop-2-enoylamino)phenyl]-7H-pyrrolo[2,3-d]pyrimidine-5-carboxylate
INCHI InChI=1S/C19H18N4O3/c1-4-26-19(25)14-9-20-17-15(14)16(21-10-22-17)12-6-5-7-13(8-12)23-18(24)11(2)3/h5-10H,2,4H2,1,3H3,(H,23,24)(H,20,21,22)
InChi Key NJPHKVOXHRAPGJ-UHFFFAOYSA-N
Canonical SMILES CCOC(=O)C1=CNC2=NC=NC(=C12)C3=CC(=CC=C3)NC(=O)C(=C)C
Isomeric SMILES CCOC(=O)C1=CNC2=NC=NC(=C12)C3=CC(=CC=C3)NC(=O)C(=C)C
PubChem CID 89629876
Molecular Weight 350.37

Certificates

Certificate of Analysis(COA)

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8 results found

Lot NumberCertificate TypeDateItem
F2306579Certificate of AnalysisApr 18, 2023 S414115
F2306580Certificate of AnalysisApr 18, 2023 S414115
F2306581Certificate of AnalysisApr 18, 2023 S414115
F2306657Certificate of AnalysisApr 18, 2023 S414115
F2306658Certificate of AnalysisApr 18, 2023 S414115
F2306659Certificate of AnalysisApr 18, 2023 S414115
F2306660Certificate of AnalysisApr 18, 2023 S414115
F2306661Certificate of AnalysisApr 18, 2023 S414115

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 70 mg/mL (199.78 mM); Ethanol: 9 mg/mL (25.68 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility70
DMSO(mM) Max Solubility199.788794702743
Water(mg / mL) Max Solubility<1

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