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BGJ-398 | Inhibitor of FGFR1, FGFR2, FGFR3, FGFR4
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
  • IC50:0.9 nM
  • IC50:5 nM
FGFR2
  • IC50:1.4 nM
  • IC50:5 nM
FGFR3
  • IC50:1 nM
  • IC50:5 nM
FGFR4
  • IC50:60 nM
  • IC50:5 nM
Inhibitor
Up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
BGJ-398 was tested against an in-house panel of 76 kinases
Selectivity Assessment Description:
BGJ-398 was tested against CYP450 enzymes 3A4, 2C9, 2C19, 2D6 and 1A2 all with IC50 > 10 uM

Potency
Cellular
In Vitro

FGFR1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/jm2006222

FGFR2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/jm2006222

FGFR3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/jm2006222

FGFR4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/jm2006222

In Vivo Validations

Mouse
Dose: 5 IV, 20 PO mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 9.3 h (IV), 4.3 h (oral)
Systemic clearance: 3.3 L/h/kg (IV)
Organ of interest (O): xenograft
Target engagement assay: Indirect: inhibition of substrate phosphorylation in xenograft tissue

DOI Reference: 10.1021/jm2006222

Orthogonal Probes def

AZD4547

Chemical Information

Molecular Formula C26H31Cl2N7O3
SMILEs CCN1CCN(c2ccc(Nc3cc(N(C)C(=O)Nc4c(Cl)c(OC)cc(OC)c4Cl)ncn3)cc2)CC1
InChI InChI=1S/C26H31Cl2N7O3/c1-5-34-10-12-35(13-11-34)18-8-6-17(7-9-18)31-21-15-22(30-16-29-21)33(2)26(36)32-25-23(27)19(37-3)14-20(38-4)24(25)28/h6-9,14-16H,5,10-13H2,1-4H3,(H,32,36)(H,29,30,31)
Molecular weight 559.19 Da
AlogP 5.3544
HBond acceptors 10
HBond donors 2
Atoms 69
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 23 May 2016 )
Cellular Use Rating
In Model Organisms
This probe is a potent and selective inhibitor of FGFR1/2/3 (though less potent against FGFR4). It acts as an adequate in vitro and in vivo inhibitor tool for these kinases.
by SERP
(on 1 Jun 2016 )
Cellular Use Rating
In Model Organisms
This compound is a pan FGFR inhibitor in the nM range with other kinases only being inhibited at high (triple digit) nM or low uM in cells. I think this probe is the best so far though, ideally, there...
by SERP
(on 7 Jun 2016 )
Cellular Use Rating
In Model Organisms
This probe has single-digit nM potency on FGFR1,2,3 in both in vitro biochemical and cell-based assays. It shows potency against only 76 other kinases assayed with most significant activity on FGFR4...
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