AZD1332
AZD1332 : ATP competitive inhibitor of NTRK1 and NTRK2
Structure
In Cells
In Model Organisms
Probe AZD1332 is in the process of SERP review.
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SERP ratings and comments
SERP Ratings
SERP Comments:
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, and selectivity for NTRK enzymes vs other kinases appears reasonable, with FGFR kinases notable off-targets. While explicit PK parameters were not reported in mice, doses of 50 or 100 mpk QD appear effective in strongly suppressing NTRK activity in vivo. PK data for AZD1332 in rat and dog are available, but additional PK/PD data might be necessary to choose an optimal dosing regimen for studies using these species.
(last updated: 10 Apr 2021 )
SERP Ratings
SERP Comments:
AZD1332 is an excellent selective Tropomyosin-related kinase A inhibitor, with proven in vitro and in vivo efficacy.
(last updated: 19 Apr 2021 )