TRK-IN-24_product_DataBase

Bioactivity	TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKAG595R, TRKAG667C and TRKAF589L IC50s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1G595R and BaF3-CD74-NTRK1G667C 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].
Target	IC50: 5.21 nM (TRKA), 4.51 nM (TRKC), 6.77 nM (TRKAG595R), 1.42 nM (TRKAG667C), 6.13 nM (TRKAF589L)
Invitro	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]。 0 --> TRK-IN-24 相关抗体:
In Vivo	TRK-IN-24 (compound 10g) (50 mg/kg; 10-14 天) 在小鼠的 BaF3-CD74-NTRK1G595R 和 BaF3-CD74-NTRK1G667C 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]。
Name	TRK-IN-24
CAS	2937544-01-7
Formula	C39H45N7O3
Molar Mass	659.82
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.. .

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