TRK-IN-24 

TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKA^G595R, TRKA^G667C and TRKA^F589L IC₅₀s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1^G595R and BaF3-CD74-NTRK1^G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC₅₀ of 1.43-47.56 nM^[1].

IC50: 5.21 nM (TRKA), 4.51 nM (TRKC), 6.77 nM (TRKA^G595R), 1.42 nM (TRKA^G667C), 6.13 nM (TRKA^F589L)^[1]

TRK-IN-24 (compound 10g) (3.7-300 nM) inhibits the phosphorylation of AKT, TRKA, PLCγ1, and ERK in Ba/F3 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TRK-IN-24 (compound 10g) (50 mg/kg; 10-14 days) in mice BaF3-CD74-NTRK1^G595R and BaF3-CD74-NTRK1^G667C In xenograft models, treatment resulted in 72% and 78% tumor regression after 10 or 14 days, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

659.82

C₃₉H₄₅N₇O₃

2937544-01-7

CC(C(C#CC1=CN=C2C=CC3=NN21)=CC(OCCCCCCCNC3=O)=C4)=C4C(NC5=CC(C6CC6)=CC(CN7CCN(CC7)C)=C5)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Wang Z, et al. Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations. J Med Chem. 2023 Sep 7.. .  [Content Brief]