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AZ-960 | AZ-960 : ATP competitive inhibitor of JAK2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
JAK2
  • Ki, IC50:0.45 nM (Ki); 3 nM (IC50) @ Km ATP
  • IC50:15 ± 6 nM
  • GI50:25 ± 1 nM
ATP competitive
100-500 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - 3 fold over JAK3

Selectivity Assessment Description:
AZ960 inhibited 11 kinases by greater than 50% at a concentration of 0.1 μm and 31 of 83 kinases ...
In Cell Selectivity Assessment

Potency: GI50 - TEL-JAK1 230±74 nM, TEL-JAK3 279±29 nM, TEL-Tyk2 214±151 nM

Potency Assay Off-Target:
Anti-Proliferation assay using BIOSOURCE AlamarBlue Assay
Selectivity Assessment Description:
15–30-fold selectivity for TEL-JAK2-driven STAT5 phosphorylation compared with cell lines driven ...

Potency
Cellular
In Vitro

JAK2

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1074/jbc.M803813200

Orthogonal Probes def

BMS-911543
GANDOTINIB
XL019

Chemical Information

Molecular Formula C18H16F2N6
SMILEs Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cc3)c(C#N)cc2F)n[nH]1
InChI InChI=1S/C18H16F2N6/c1-10-7-16(26-25-10)23-18-15(20)8-13(9-21)17(24-18)22-11(2)12-3-5-14(19)6-4-12/h3-8,11H,1-2H3,(H3,22,23,24,25,26)/t11-/m0/s1
Molecular weight 354.14 Da
AlogP 4.179700000000002
HBond acceptors 6
HBond donors 3
Atoms 42

References

Publications

Cross References

Vendors

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Expert Reviews

by SERP
(on 12 Sept 2021 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 12 Oct 2021 )
Cellular Use Rating
AZ 960 is a moderately selective, ATP competitive JAK2 inhibitor with IC50 of <3 nM and a 3-fold selectivity over JAK3. It has been tested in a panel of 83 protein kinases at three inhibitor concentrations...
by SERP
(on 22 Mar 2023 )
Cellular Use Rating
The compound shows only 3-fold selectivity over JAK3. Potentially pan-selective inhibitor. Not screened against all kinases. No target engagement data is available
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria