Central China Normal Univ. TRKA G595R compound 5c

Central China Normal Univ. TRKA G595R compound 5c: sourced facts only. name: "The best TRK inhibitor 5c had IC50 values of 0.75 and 0.96 nM against TRKAG595R and TRKAG667C, showing better potency than drugs larotrectinib (approximately 87- and 46-fold improvement) and selitrectinib (approximately 10- and 13-fold improvement)." [PMID:41666629]; target: "The best TRK inhibitor 5c had IC50 values of 0.75 and 0.96 nM against TRKAG595R and TRKAG667C, showing better potency than drugs larotrectinib (approximately 87- and 46-fold improvement) and selitrectinib (approximately 10- and 13-fold improvement)." [PMID:41666629]; developer: "State Key Laboratory of Green Pesticide, College of Chemistry, Central China Normal University, Wuhan 430079, China." [PMID:41666629]; stage: "More importantly, 5c demonstrated favorable in vivo pharmacokinetic properties and antitumor efficacy (tumor growth inhibition (TGI) of 91% at 30 mg/kg and 115% at 60 mg/kg with 4 of 6 partial regression) in a BaF3-TMP3-TRKAG667C xenograft mouse model, which is greatly superior to that of selitrectinib (TGI of 2% at 30 mg/kg)." [PMID:41666629]