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AZD4547 | Inhibitor of FGFR1, FGFR2, FGFR3
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (1 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
FGFR1
  • IC50:0.2 nM
  • IC50:12 nM
  • IC50:18 nM
FGFR2
  • IC50:1.8 nM
  • IC50:2 nM
  • IC50:41 nM
FGFR3
  • IC50:2.5 nM
  • IC50:40 nM
  • IC50:281 nM
Inhibitor
30-100 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - KDR 24 nM, FGFR4 165 nM, IGFR 581 nM

Selectivity Assessment Description:
Selectivity was examined against a diverse panel of representative human kinases and AZD4547 shown t ...
In Cell Selectivity Assessment

Potency: IC50 - KDR 258 nM, FGFR4 165 nM, IFGR 828 nM

Potency
Cellular
In Vitro

FGFR1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1158/0008-5472.CAN-11-3034

FGFR2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1158/0008-5472.CAN-11-3034

FGFR3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1158/0008-5472.CAN-11-3034

In Vivo Validations

Other Organism
Dose:

DOI Reference: 10.1158/0008-5472.CAN-11-3034

Orthogonal Probes def

BGJ-398

Chemical Information

Molecular Formula C26H33N5O3
SMILEs COc1cc(CCc2cc(NC(=O)c3ccc(N4C[C@H](C)N[C@H](C)C4)cc3)[nH]n2)cc(OC)c1
InChI InChI=1S/C26H33N5O3/c1-17-15-31(16-18(2)27-17)22-9-6-20(7-10-22)26(32)28-25-13-21(29-30-25)8-5-19-11-23(33-3)14-24(12-19)34-4/h6-7,9-14,17-18,27H,5,8,15-16H2,1-4H3,(H2,28,29,30,32)/t17-,18+
Molecular weight 463.26 Da
AlogP 3.6510000000000025
HBond acceptors 8
HBond donors 3
Atoms 67

References

Publications

Cross References

Vendors

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Expert Reviews

by SERP
(on 20 Dec 2021 )
Cellular Use Rating
This probe has a long history of use to study FGFR signaling, especially with regards to its importance in various tumors. Cancer-cell profiling revealed that AZD4547 is quite specific in killing only...
by SERP+
(on 22 Mar 2023 )
Cellular Use Rating
In Model Organisms
Established selectivity is excellent for 3 combined kinases vs kinome with insufficient selectivity within the 3 kinases. The compound shows in vivo efficacy. Tumor growth dose response has been measured...
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