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) 抑制 Ba/F3 细胞中 AKT、TRKA、PLCγ1、ERK 的磷酸化^[1]。

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 天) 在小鼠的 BaF3-CD74-NTRK1^G595R 和 BaF3-CD74-NTRK1^G667C 异种移植模型中，处理 10 或 14 天后分别造成 72% 和 78% 的肿瘤消退^[1]。

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

659.82

C₃₉H₄₅N₇O₃

2937544-01-7

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]