AZ7550 - IGF-1R 抑制剂- MedChemExpress

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Inhibitors?Agonists?Screening Librarieswww.MedChemExpress.cnAZ7550Cat. No.:CAS No.:HY-B07941421373-99-0C??H??N?O?485.58IGF-1RProtein Tyrosine Kinase/RTKPlease store the product under the recommended conditions in the COA.分?式:分?量:作?靶点:作?通路:储存?式:BIOLOGICAL ACTIVITY?物活性IC50 & TargetAZ7550 是 AZD9291 的?种活性代谢物，AZ7550 抑制 IGF1R 活性，IC50 为 1.6 μM。IC50: 1.6 μM (IGF1R), 88 nM (MLK1), 156 nM (ACK1), 195 nM (ErbB4), 228 nM (MNK2), 302 nM (FLT3), 420 nM (ALK ), 449 nM (FES), 840 nM (IRR), 843 nM (BRK), 977 nM (BLK), 995 nM (FAK), 1256 nM (Ins R), 1317 nM (TEC), 1784 nM (FLT4), 2288 nM (PYK2), 2443 nM (Txk), 5104 nM (BTK) [1]体外研究AZ7550 (Compound 28) appeares to offer a broadly similar potency and selectivity profile to the parent compound AZD9291. AZ7550 inhibits double mutant (DM) cell line H1975, activating mutant (AM) cell line PC9, and wild type (WT) cell line LoVo with IC50s of 45, 26, and 786 nM, respectively. AZ7550 inhibits DM antiproliferative cell line H1975, AM antiproliferative cell line PC9, and WT antiproliferative cell line Calu3 with GI50s of 19, 15, and 537 nM, respectively [1]. PROTOCOLKinase Assay [1]Biochemical enzyme profiling of AZD9291 and active metabolites across the kinome panel (single profiling experiment representative of two independent studies). % inhibition for kinases in the ~280 kinase panel that shows greater than 60% inhibition after 1 μM treatment with AZD9291, AZ5104 or AZ7550, and follow-up IC50s where tested, are shown. Kinases with a conserved cysteine in the analogous position within their catalytic domain as Cys797 in EGFR are also shown, highlighted in bold [1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. REFERENCES1/2Master of Small Molecules —您?边的抑制剂?师www.MedChemExpress.cn

[1]. Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67.

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