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AZD1332 | AZD1332 : ATP competitive inhibitor of NTRK1 and NTRK2
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Names: AZD1332, AZ-23, T1; AZ-23, V4Z, canSAR1988291, Kinome_3819, cpd 10z

Targets Biochemical/Biophysical Potency Cellular Potency
NTRK1
  • IC 50:2 nM
  • EC 50:1.2 nM
NTRK2
  • IC 50:8 nM
  • EC 50:1.2 nM
Inhibitor
50-100 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - FGFR1 24 nM

Selectivity Assessment Description:
In vitro selectivity profiling across a broad panel of 177 kinases (Millipore's Kinase Profiler) sho ...
In Cell Selectivity Assessment

Potency: EC50 - FGFR1 41 nM

Selectivity Assessment Description:
Cell selectivity (EC50): 4077 nM (IGF1R), >1000 nM (Aurora), >3000 (CSF1R), >5000 nM (InsR, Akt, p70 ...

Potency
Cellular
In Vitro

NTRK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm800343j

NTRK2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm800343j

In Vivo Validations

Rat, Dog
Dose: 3 mg/Kg IV, 10 mg/Kg PO, Reviewer suggest 50-100 mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 1.4 (R), 7.5 (D) h
Systemic clearance: 17 (R), 9 (D) mL/min/kg

DOI Reference: 10.1021/jm800343j

Chemical Information

Molecular Formula C17H19ClFN7O
SMILEs CC(C)Oc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)ncc2Cl)[nH]n1
InChI InChI=1S/C17H19ClFN7O/c1-9(2)27-15-6-14(25-26-15)23-16-12(18)8-21-17(24-16)22-10(3)13-5-4-11(19)7-20-13/h4-10H,1-3H3,(H3,21,22,23,24,25,26)/t10-/m0/s1
Molecular weight 391.13 Da
AlogP 4.091100000000002
HBond acceptors 8
HBond donors 3
Atoms 46

Vendors

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Expert Reviews

by SERP
(on 10 Apr 2021 )
Cellular Use Rating
In Model Organisms
The two cited publications provide a range of biochemical, cell-based, and in vivo assays demonstrating NTRK1/2/3 inhibition. Biochemical and cellular potency is very high for this small kinase family,...
by SERP
(on 19 Apr 2021 )
Cellular Use Rating
In Model Organisms
AZD1332 is an excellent selective Tropomyosin-related kinase A inhibitor, with proven in vitro and in vivo efficacy.
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