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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

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 public 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