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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Cited by 44 Publications

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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 Mm\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXMNE0yOCEQvF2= MV63NkBp MWrpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M1HuclI2QTR6NkOz
PC9 Mm[zSpVv[3Srb36gRZN{[Xl? NH;jUZMxNTFyIN88US=> NIK3Wo04OiCq MVrpcohq[mm2czDXWEBGT0[UIHH0JIxwfyClb37j[Y51emG2aX;udy=> MXqyOVk1QDZ|Mx?=
PC9 GR4 NHPDR2lHfW6ldHnvckBCe3OjeR?= Mn2xNE0yOCEQvF2= M3LzXVczKGh? M3q5W4lvcGmkaYTzxsBGT0[UIIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUB{cWewYXzpcofDqA>? NUXGWIEzOjV7NEi2N|M>
VP-2 NH3SSGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU[1NEBvVQ>? NVzm[nNsOTBiZB?= NGPzelRFVVOR NEfBRWtqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= M2j5dFI2PDd5M{K1
PC-9/ERc1 NELSOYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX61NEBvVQ>? MWixNEBl M2PVZWROW09? NF3NTZdqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= M3PuZlI2PDd5M{K1
PC-9/BRc1 M3;yc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjjU3A2OCCwTR?= Mn2zNVAh\A>? MmnmSG1UVw>? MXTpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHzvcocufGW{bTCoNVAu\GG7KTDndo94fGhiaX7obYJqfGmxbjDhd5NigXN? NY[5[mJlOjV2N{ezNlU>
VP-2 NV3xOYd7TnWwY4Tpc44hSXO|YYm= NGPqcow2OCCwTR?= M1\Eb|I1KGh? MYDEUXNQ MkjjbY5lfWOnczDlfJBz\XO|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2= NXTJT3JpOjV2N{ezNlU>
PC-9/ERc1 Mo\VSpVv[3Srb36gRZN{[Xl? MYe1NEBvVQ>? M3nkV|I1KGh? MXvEUXNQ NXn5XphVcW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0> NUDtPGlQOjV2N{ezNlU>
PC-9/BRc1 Mn:4SpVv[3Srb36gRZN{[Xl? M3\WTlUxKG6P NFq2S5kzPCCq NHHTRYNFVVOR NIHSU3NqdmS3Y3XzJIV5eHKnc4Ppc44hd2ZidHjlJJBzd2Gyb4D0c5Rq[yCEQ1ytNkBn[W2rbImgcYVu[mW{IFLJUS=> M{m3XFI2PDd5M{K1

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-EGFR / p-AKT / p-ERK; 

PubMed: 28416483     


PC-9/BRc1 cells were treated with the indicated doses of osimertinib. Drugs were refreshed every 24 hours. Cellular lysates were probed with the indicated antibodies. Osim: osimertinib.

ABCB1; 

PubMed: 27649127     


The effect of osimertinib at 0.3 μM on the expression of ABCB1 was measured in KB-3-1 and KB-C2 cell lines for 0, 24, 48, and 72 h.

28416483 27649127
Growth inhibition assay
Cell viability; 

PubMed: 31043587     


Cells were treated with gefitinib or osimertinib for 72 h. Cell viability was measured by MTT assay. *P < 0.05, **P < 0.01, ***P < 0.005 by t-test.

31043587
Immunofluorescence
Ki67 / γH2AX / p16; 

PubMed: 29212784     


PC9ER cells were treated for 5 days with either 3×mAbs (20 μg/ml), saline (CTRL), or with a low dose of osimertinib (2.5 nM). Shown are representative images of cells fixed in paraformaldehyde and immunostained for KI67 (panel E), γH2AX (panel F), and p16 (panel G). DAPI counterstaining was used to follow nuclear localization. Scale bar, 20 μm. The box and whisker plots, where the ends of the box are the upper and lower quartiles, depict quantifications of results obtained in three independent experiments. **P ≤ 0.01, ***P ≤ 0.001, n = 4; one-way ANOVA with Tukey's test.

29212784
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

Animal Research:

[2]
+ Expand
  • Animal Models: Mice bearing PC9 and H1975 xenograft tumors
  • Formulation: --
  • Dosages: ~5 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 99 mg/mL warmed (198.15 mM)
Ethanol 43 mg/mL warmed (86.06 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing. 		30mg/mL

* 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
in solvent
Synonyms N/A

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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02841579 Active not recruiting Drug: Osimertinib Non-Small Cell Lung Cancer MedSIR|AstraZeneca August 2016 Phase 2
NCT02771314 Active not recruiting Drug: AZD9291 Non Small Cell Lung Cancer Hellenic Oncology Research Group August 2 2016 Phase 2
NCT02511106 Active not recruiting Drug: AZD9291 80 mg/40 mg|Drug: Placebo AZD9291 80 mg/40 mg Stage IB-IIIA Non-small Cell Lung Carcinoma AstraZeneca October 21 2015 Phase 3
NCT02529995 Active not recruiting Drug: AZD9291 40 mg|Drug: AZD9291 80 mg Carcinoma Non-Small-Cell Lung With EGFR Mutation Positive AstraZeneca August 24 2015 Phase 1
NCT02491944 Completed Drug: AZD9291|Drug: [14C]AZD9291 Oncology AstraZeneca July 2015 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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Frequently Asked Questions

  • Question 1:

    Can this formulation be used in mice? What are reconstitution instructions for in vivo with mice?

  • Answer:

    Osimertinib can be used for animal study. The vehicle we suggest is: 1% DMSO+30% PEG 300+dd H2O at up to 30mg/ml.

selleck catalog

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID