AZ960

Protein target name:

JAK2

Mechanism of action:

InhibitorATP Competitive

Recommended Concentration for use in cells:

100-500 nM

Probe Availability

MedChemExpress

Selleck Chemicals

Axon MedChem

Probe Information

Target and Probe Information

Target Details

Target class:

Protein kinase

Subclass:

HUGO ID:

HGNC:6192

Entrez gene ID:

3717

UNIPROT ID:

O60674

Target alias:

Janus kinase 2, JTK10, THCYT3

Probe Details

Chemical Probes Portal ID:

CPP1197

Probe alias:

AZ 960; 905586-69-8; AZ-960; Gandotinib; BMS-911543; XL019

PubChem CID:

25099184

ChEMBL ID:

CHEMBL1774055

SMILES string:

N#CC1=CC(F)=C(NC2=NNC(C)=C2)N=C1N[C@H](C3=CC=C(F)C=C3)C

InChi Key:

SUNXHXDJOIXABJ-NSHDSACASA-N

Orthogonal probe:

BMS-911543GandotibibXL019

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

Ki, IC50

0.45 nM (Ki), 3 nM (IC50) @ Km ATP

Potency assay:

Enzymatic Biochemical Competitive Assay

Off target activity

Potency (off target):

IC50

Off target protein and potency:

3 fold over JAK3

Probe Selectivity in Vitro:

AZ960 inhibited 11 kinases by greater than 50% at a concentration of 0.1 μm and 31 of 83 kinases less than 50% at a concentration 0.1 µM.

In cell validation

On target activity in cells

Potency in cells:

IC50, GI50

15 ± 6 nM IC50, 25 ± 1 nM GI50

Potency assay (cells):

Western immunoblotting determination of phospho-STAT5 and phospho-STAT3 levels. Anti-Proliferation assay using BIOSOURCE AlamarBlue Assay

Off target activity in cells

Potency in cells, off target:

GI50

Off target protein and potency (cells):

TEL-JAK1 230±74 nMTEL-JAK3 279±29 nMTEL-Tyk2 214±151 nM

Potency assay, off target (cells):

Anti-Proliferation assay using BIOSOURCE AlamarBlue Assay

Probe Selectivity in Cell:

15–30-fold selectivity for TEL-JAK2-driven STAT5 phosphorylation compared with cell lines driven by other JAK kinase family members (TEL-JAK1, -JAK3, and -TYK2)

Primary Reference

Reference (doi):

10.1074/jbc.M803813200

Reference (PMID):

18775810

AZ960

Probe Availability

Probe Information

Target Details

Janus kinase 2, JTK10, THCYT3

Probe Details

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

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AZ960

Probe Availability

Probe Information

Target Details

Janus kinase 2, JTK10, THCYT3

Probe Details

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?