AZ7550 Mesylate (AZ7550 trimesylate salt)

An active metabolite of AZ 9291

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库存: 现货

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数量
5mg

￥3012.00

2410.00

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10mg

￥4700.00

3760.00

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Background

AZ 7550 is an active metabolite of AZ 9291 .¹ It inhibits the insulin-like growth factor 1 receptor (IGF-1R) in a cell-free assay (IC₅₀ = 1.6 ?M). It inhibits EGFR autophosphorylation in H1975 and PC-9 cells expressing the respective constitutively active mutants EGFR^T790M/L858R and EGFR^Exon19del (IC₅₀s = 0.045 and 0.026 ?M, respectively), as well as in LoVo cells expressing wild-type EGFR (IC₅₀ = 0.786 ?M).

1.Finlay, M.R., Anderton, M., Ashton, S., 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 receptorJ. Med. Chem.57(20)8249-8267(2014)

Protocol

Kinase experiment:

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].

参考文献:

[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.