Inhibitors?Screening Libraries?ProteinsMedChemExpressType II TRK inhib itor 1Cat. No.:HY-146807分子式:C??H??F?N?O?分子量:670.68作用靶点:Trk Recept or作用通路:Neuronal Signaling; Protein Tyrosine Kinase/RTK储存方式:Please store the product under the recommended conditions inthe Certifi cate of Analysis.BIOLOGICAL ACTIVITY生物活性Type II TRK inhibitor 1 是 一种有效的 TRK 抑制剂,可抑制各种 TRK 融合蛋白变体和野生型。Type IITRK inhibitor 1 对携带 CD7 4-TRKAG667C 和 ETV6-TRKCG696C 融合蛋白的 Ba/F3 细胞具有抗增殖活性,IC 值为 50 分别为 6 nM 和 1.7 nM。IC50 & TargetTrkATrkC体外研究Type II TRK inhibitor 1 (co mpound 7b) (3.1-800 nM; 2 h) inhibits the phosphorylation of TRKA , PLCγ1, andERK [1].Western Blot Analysis [1]Cell Line:Ba/F3 engi neered cells harboring CD74-TRKA, CD74-TRKAG667C, and CD74-TRKAG5 95RConcentration:0 nM, 3.1 nM, 12.5 nM, 50 nM, 200 nM, 800 nMIncu bation Time:24 hoursResult:Decreased the protein level of p-TRKA, p-PLCγ1, p-ERK in cells.REFERENCESWang Z, et al. Discovery of th e First Highly Selective and Broadly Effective Macrocycle-Based T ype II TRK Inhibitors that Overcome Clinically Acquired Resistanc e. J Med Chem. 2022 Apr 28;65(8):6325-6337.McePdfHeight1/1Master of Bioactive Molecules — 您身边的抑制剂大师MedChemExpressCaution: Product has not been fully validated for medical applications.For researc h use only.2/1Master of Bioactive Molecules — 您身边的抑制剂大师 |
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