D5261-DataSheet-生命科学试剂-MedChemExpress.pdf

Hotline: 400-820-3792 Inhibitors • Screening Libraries • Proteins www.MedChemE D5261 Cat. No.: HY-144690 CAS No.: 1574574-57-4 分⼦式: C₂₅H₂₉N₅O₃ 分⼦量: 447.53 作⽤靶点: Trk Receptor 作⽤通路: Neuronal Signaling; Protein Tyrosine Kinase/RTK 储存⽅式: Please store the product under the recommended conditions in the Certificate of Analysis. BIOLOGICAL ACTIVITY ⽣物活性 D5261 是⼀个有效的、类型III变构的 tropomyosin-related kinase A (TrkA) 抑制剂 [1]。 IC50 Target TrkA 体外研究 D5261 (0-10 µM, 72 h) displays favorable anti-proliferative activity in Ba/F3-MPRIP-TrkA cells (IC50 = 3.32 µM) and Ba/F3 CD74-TrkA cells (IC50 = 2.91 µM) [1]. D5261 exhibits cellular selectivity over TrkB/C to some extent (Ba/F3 IC50 10 µM, Ba/F3-QKI-TrkB IC50 6.17 µM and Ba/F3-EML4-TrkC IC50 10 µM) [1]. D5261 (0-50 µM) inhibits the TrkA autophosphorylation and downstream signaling in a concentration- dependent manner [1]. D5261 shows inhibitory activity against Ba/F3 cells harboring TrkA mutants (G667C, G667S, G667A, G595R and V573 M) [1]. Cell Viability Assay [1] Cell Line: Ba/F3-MPRIP-TrkA, Ba/F3 CD74-TrkA cells Concentration: 0-10 µM Incubation Time: 72 h