AZD3759

Catalog No.S7971

AZD3759 Chemical Structure

Molecular Weight(MW): 459.90

AZD3759 is a potent, oral active, CNS-penetrant EGFR inhibitor with IC50 of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively. Phase 1.

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Biological Activity

Description AZD3759 is a potent, oral active, CNS-penetrant EGFR inhibitor with IC50 of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively. Phase 1.
Targets
EGFR (L858R) [1]
(Cell-free assay)
EGFR (exon 19Del) [1]
(Cell-free assay)
EGFR (WT) [1]
(Cell-free assay)
0.2 nM 0.2 nM 0.3 nM
In vitro

In H3255 (L858R) cells, AZD3759 inhibits EGFR phosphorylation with IC50 of 7.2 nM. AZD3759 demonstrates inhibitory effects on both the pEGFR pathway and cell proliferation of EGFR mutation-derived cells PC-9 and H3255 with IC50 of 7.7 nM and 7 nM, respectively, showing mo activity on cell proliferation of H838 cells. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H3255 cells NWnFPFBJWHKxbHnm[ZJifGmxbjDhd5NigQ>? MmfSO|IhcA>? NXzmRWl6SW62aYDyc4xq\mW{YYTpeoUh[WejaX7zeEBpfW2jbjDIN|I2PSClZXzsd{BmgHC{ZYPzbY5oKEWJRmKgUFg2QFJibYX0ZY51KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEmFNUC9NE4xODdizszN MoDMNlY{OTN{NUK=
PC9 cells NWW3UnQyTnWwY4Tpc44h[XO|YYm= MlOyTY5pcWKrdHnvckBw\iCHR1\SJIV5d25zOTDk[YxmfGmxbjDteZRidnRicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFCFOTDj[YxteyxiSVO1NF0xNjByN{Sg{txO MYSyOlMyOzJ3Mh?=
H838 cells NXy4eoo5TnWwY4Tpc44h[XO|YYm= NH3KcoZKdmirYnn0bY9vKG:oIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGg5OzhiY3XscJMtKEmFNUC9NE4xPjR3IN88US=> NHO4eVEzPjNzM{K1Ni=>

... Click to View More Cell Line Experimental Data

In vivo AZD3759 shows good oral bioavailability in dogs, and penetrates extensively into monkey brain. In a brain metastasis PC-9 (Exon19Del) model, AZD3759 (15 mg/kg) causes significant dose-dependent antitumor efficacy. [1]

Protocol

Kinase Assay:[1]
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IC50 determination of compounds against EGFR enzymes:

The inhibition potency of compounds against EGFR WT and mutant enzymes is assessed using CisBio homogenous time resolved fluorescence approach (HTRF, Cat No. 62TK0PEJ) according to manufacturer’s instruction. The final enzyme concentrations used in this assay are 0.1 nM, 0.03 nM, and 0.026 nM for EGFR wild type, L858R and Exon19Del, respectively, and 0.8 μM, 4 μM and 25 μM ATP, corresponding to the Km values of EGFR enzymes, are applied accordingly. In brief, 3 μL of ATP and 2 μM TK biotin-peptide substrate are incubated in the presence or absence of serially diluted compound at room temperature in 384-well Greiner white polystyrene assay plates. The reaction is initiated by addition of 3 μL kinase which could phosphorylate the substrate peptide, and the assay buffer contains 1 mM DTT, 5 mM MgCl2, 1 mM MnCl2, and 0.01% CHAPS. After 30 minutes incubation, the reaction is stopped by the addition of 6 μl detection reagent mix containing 250 nM Strep-XL665 and TK Ab Europium Cryptate diluted in detection buffer. The plates are incubated for 1 h before the fluorescence is then measured at 615 nm and 665 nm, respectively with excitation wavelength at 320 nm by EnVision Multilabel Reader from Perkin Elmer using standard HTRF settings. The calculated signal ratio of 665 nm/615 nm is proportional to the kinase activity. The concentration of compound producing 50% inhibition of the respective kinase (IC50) is calculated using four-parameter logistic fit.
Cell Research:[1]
+ Expand
  • Cell lines: PC-9 (exon 19Del), H3255 (L858R) and H838 (wt) cells
  • Concentrations: ~30 mM
  • Incubation Time: 72 h
  • Method: Cell proliferation assay is determined by MTS methods. Briefly, cells are seeded in 96-well plates (at a density to allow for logarithmic growth during the 72-hour assay) and incubated overnight at 37 °C and 5% CO2. Cells are then exposed to concentrations of compounds ranging from 30 to 0.0003 mM for 72 hours. For the MTS endpoint, cell proliferation is measured by the CellTiter AQueous Non-Radioactive Cell Proliferation Assay reagent in accordance with the manufacturer’s protocol. Absorbance is measured with a Tecan Ultra instrument. Predose measurements are made, and concentration needed to reduce the growth of treated cells to half that of untreated cells (GI50) values are determined using absorbance readings.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Mice bearing PC-9 (Exon19Del) tumors
  • Formulation: 1% methylcellulose
  • Dosages: ~15 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 91 mg/mL (197.86 mM)
Ethanol 20 mg/mL warmed (43.48 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 459.90
Formula

C22H23ClFN5O3

CAS No. 1626387-80-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02228369 Recruiting EGFR Mutation Positive Advanced Non Small Cell Lung Cancer AstraZeneca November 2014 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID