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GNF-5837 | Inhibitor of NTRK1, NTRK2, NTRK3
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
NTRK1
  • IC 50:8 nM
  • IC 50:11 nM
NTRK2
  • IC 50:12 nM
  • IC 50:9 nM
NTRK3
  • IC 50:NA
  • IC 50:7 nM
Inhibitor
50-500 nM
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Highly selective in a Biochemical Kinase Panel (Invitrogen).
In Cell Selectivity Assessment
Potency Assay Off-Target:
Ba/F3 Cellular assay
Selectivity Assessment Description:
In Ba/F3 Cellular Kinase Panel of 25 Kinases fused with Tel dimerisation partner showed IC50 > ...

Potency
Cellular
In Vitro

NTRK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/ml200261d

NTRK2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/ml200261d

NTRK3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/ml200261d

In Vivo Validations

Mouse, Rat
Dose: 50-100 mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 4.4, 4.5 (M) h , 7.5, 7.1 (R) h
Systemic clearance: 8.2 (M), 9 (R) mL/min/kg

DOI Reference: 10.1021/ml200261d

Chemical Information

Molecular Formula C28H21F4N5O2
SMILEs Cc1ccc(NC(=O)Nc2cc(C(F)(F)F)ccc2F)cc1Nc1ccc2c(c1)NC(=O)/C2=C\c1ccc[nH]1
InChI InChI=1S/C28H21F4N5O2/c1-15-4-6-19(35-27(39)37-25-11-16(28(30,31)32)5-9-22(25)29)13-23(15)34-18-7-8-20-21(12-17-3-2-10-33-17)26(38)36-24(20)14-18/h2-14,33-34H,1H3,(H,36,38)(H2,35,37,39)/b21-12-
Molecular weight 535.16 Da
AlogP 7.36132
HBond acceptors 7
HBond donors 5
Atoms 60

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 26 Jul 2021 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 4 Aug 2021 )
Cellular Use Rating
In Model Organisms
There are more well-characterized tools, in particular Laratrectinib which is both approved for human use and better profiled for selectivity against more kinases (link)or perhaps clinical compounds...
by SERP
(on 26 Aug 2021 )
Cellular Use Rating
In Model Organisms
Together the two reference documents provide acceptable evidence that cell-based and organism-based anticancer activity may be due to pan TRK inhibition, and the E-R Cancer study shows evidence of target...
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