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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 public 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