Osimertinib (AZD9291)

Catalog No.S7297

Osimertinib (AZD9291) Chemical Structure

Molecular Weight(MW): 499.61

Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.

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4 Customer Reviews

  • Lysates from MGH121 parental cells treated with 1 μM of the indicated TKIs except for AZD9291 (160 nM) for 6 hours were probed with the indicated antibodies.

    Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0560 . Osimertinib (AZD9291) purchased from Selleck.

    Western blot analysis for total (t-) and phosphorylated (p-) EGFR, AKT, ERK1/2, and β actin in H1975 parental and resistant (COR#3, AZDR#1) cells.

    Cancer Res, 2017.. Osimertinib (AZD9291) purchased from Selleck.

  • F, PC-9/ffluc and PC-9/LMC-GR cells (2×103 cells/well) were incubated with various concentrations of osimertinib for 72 hours. Cell viability was determined by MTT assay. Bars represent SD of quadruplicate cultures. Data shown are representative of three independent experiments with similar results.

    Mol Cancer Ther, 2017, 16(3):506-515. Osimertinib (AZD9291) purchased from Selleck.

    Western blot analysis showing phospho-EGFR (p-EGFR), total EGFR, phospho-ERK (p-ERK), total ERK, phospho-AKT (p-AKT), total AKT and β-actin as a loading control in H1975 cells treated with the indicated inhibitors. Equivalent amounts of proteins from whole cell lysates were subjected to WB analysis to detect the indicated proteins.

    J Biol Chem, 2015, 290(28): 17495-504. Osimertinib (AZD9291) purchased from Selleck.

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.
Features Orally bioavailable mutant-selective EGFR inhibitor that has been tested in Phase III clinical trials for treatment of Non-Small Cell Lung Cancer.
Targets
L858R/T790M EGFR [1]
(LoVo cells)
Exon 19 deletion EGFR [1]
(LoVo cells)
WT EGFR [1]
(LoVo cells)
11.44 nM 12.92 nM 493.8 nM
In vitro

AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC9 GR4 NInYSnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDzNE0yOCEQvF2= NYnnd4Q5PzJiaB?= NWTNN5ZmcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NIfmZW8zPTl2OE[zNy=>
PC9 NVG0fVZvTnWwY4Tpc44hSXO|YYm= NUH3fndDOC1zMDFOwG0> NF3G[HI4OiCq Mle0bY5pcWKrdIOgW3QhTUeIUjDheEBtd3diY3;uZ4VvfHKjdHnvcpM> NXX4eVlZOjV7NEi2N|M>
PC9 GR4 NUjCU3p7TnWwY4Tpc44hSXO|YYm= NHf2TnAxNTFyIN88US=> NELVbno4OiCq NVrMbmhNcW6qaXLpeJPDqEWJRmKgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKHOrZ37hcIlv\8Li NXXkZnF1OjV7NEi2N|M>
VP-2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjIXmI2OCCwTR?= MV6xNEBl NXnadHpJTE2VTx?= MVLpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHzvcocufGW{bTCoNVAu\GG7KTDndo94fGhiaX7obYJqfGmxbjDhd5NigXN? M{PsV|I2PDd5M{K1
PC-9/ERc1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkD1OVAhdk1? NXixOmdkOTBiZB?= Mmn3SG1UVw>? NH;PeFNqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= MkLLNlU1Pzd|MkW=
PC-9/BRc1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXyOVAhdk1? M1\ifFExKGR? NH73SFJFVVOR NYnYWIJ6cW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBtd26pLYTldo0hMDFyLXThfUkh\3Kxd4ToJIlvcGmkaYTpc44h[XO|YYnz MWGyOVQ4PzN{NR?=
VP-2 M3G3NmZ2dmO2aX;uJGF{e2G7 MW[1NEBvVQ>? Ml\XNlQhcA>? MorwSG1UVw>? NHS5ZllqdmS3Y3XzJIV5eHKnc4Ppc44hd2ZidHjlJJBzd2Gyb4D0c5Rq[yCEQ1ytNkBn[W2rbImgcYVu[mW{IFLJUS=> MVyyOVQ4PzN{NR?=
PC-9/ERc1 NVXQcpM6TnWwY4Tpc44hSXO|YYm= MlfwOVAhdk1? MnHyNlQhcA>? M17uR2ROW09? MlTubY5lfWOnczDlfJBz\XO|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2= NYC3UJdEOjV2N{ezNlU>
PC-9/BRc1 MoDLSpVv[3Srb36gRZN{[Xl? M37XN|UxKG6P M4LJO|I1KGh? MoqzSG1UVw>? NGrUNFdqdmS3Y3XzJIV5eHKnc4Ppc44hd2ZidHjlJJBzd2Gyb4D0c5Rq[yCEQ1ytNkBn[W2rbImgcYVu[mW{IFLJUS=> NWn0RYdYOjV2N{ezNlU>

... Click to View More Cell Line Experimental Data

In vivo AZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK in vivo. [2]

Protocol

Solubility (25°C)

In vitro DMSO 99 mg/mL warmed (198.15 mM)
Ethanol 43 mg/mL warmed (86.06 mM)
Water slightly soluble or insoluble
In vivo Add solvents individually and in order:
1% DMSO+30% PEG 300+dd H2O
30

* 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 499.61
Formula

C28 H33 N7 O2

CAS No. 1421373-65-0
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02923947 Not yet recruiting Solid Tumours AstraZeneca|Quintiles, Inc. January 2017 Phase 1
NCT02972333 Not yet recruiting EGFR-TKI Resistant Mutation|Nonsmall Cell Lung Cancer|AZD9291|Brain Metastases Shandong Cancer Hospital and Institute|AstraZeneca December 2016 Phase 3
NCT02997501 Recruiting Lung Cancer AstraZeneca|TigerMed December 2016 Phase 3
NCT02771314 Recruiting Non Small Cell Lung Cancer Hellenic Oncology Research Group June 2016 Phase 2
NCT02811354 Not yet recruiting Carcinoma, Non-Small-Cell Lung National University Hospital, Singapore|AstraZeneca|Singapore Clinical Research Institute June 2016 Phase 2
NCT02736513 Recruiting Lung Cancer Rabin Medical Center May 2016 Phase 2

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID