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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2 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 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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NFPnOIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nrOlAuOTBizszN M{jOXFczKGh? M4P4PYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NEXZT2szPTl2OE[zNy=>
PC9 NXLOeI9bTnWwY4Tpc44hSXO|YYm= NEG2V5gxNTFyIN88US=> MVy3NkBp M4rid4lvcGmkaYTzJHdVKEWJRmKgZZQhdG:5IHPvcoNmdnS{YYTpc45{ MlK4NlU6PDh4M{O=
PC9 GR4 Mn[1SpVv[3Srb36gRZN{[Xl? NInDSG0xNTFyIN88US=> NVzUe4Z[PzJiaB?= MWnpcohq[mm2c9MgSWdHWiCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gd4lodmGuaX7nxsA> MlLCNlU6PDh4M{O=
VP-2 NHHnbWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHPVGs2OCCwTR?= M1n2ZlExKGR? NUfJcXBHTE2VTx?= NHHqfIdqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= NIeyfnAzPTR5N{OyOS=>
PC-9/ERc1 M1jHZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\MSWE2OCCwTR?= NWXz[HNFOTBiZB?= NF\M[nJFVVOR NUftd2ZpcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBtd26pLYTldo0hMDFyLXThfUkh\3Kxd4ToJIlvcGmkaYTpc44h[XO|YYnz M37wUFI2PDd5M{K1
PC-9/BRc1 M4j0Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mme1OVAhdk1? NG[4fWMyOCCm NU\VXllGTE2VTx?= NWHicpY5cW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBtd26pLYTldo0hMDFyLXThfUkh\3Kxd4ToJIlvcGmkaYTpc44h[XO|YYnz M3K2WVI2PDd5M{K1
VP-2 MlzNSpVv[3Srb36gRZN{[Xl? MXu1NEBvVQ>? NVHvPGlZOjRiaB?= MUjEUXNQ NFThZnZqdmS3Y3XzJIV5eHKnc4Ppc44hd2ZidHjlJJBzd2Gyb4D0c5Rq[yCEQ1ytNkBn[W2rbImgcYVu[mW{IFLJUS=> MljHNlU1Pzd|MkW=
PC-9/ERc1 M{\JZmZ2dmO2aX;uJGF{e2G7 NXnYclc5PTBibl2= M1K0PFI1KGh? NFzOUGRFVVOR M1XnWIlv\HWlZYOg[ZhxemW|c3nvckBw\iC2aHWgdJJw[XCxcITveIlkKEKFTD2yJIZidWmueTDt[Y1j\XJiQlnN M2\ZdFI2PDd5M{K1
PC-9/BRc1 M2nZXWZ2dmO2aX;uJGF{e2G7 MnLqOVAhdk1? M1Wz[FI1KGh? M{DVfGROW09? NVnTcJVJcW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0> NWrG[o9tOjV2N{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 (198.15 mM) warming
Ethanol 43 mg/mL warmed (86.06 mM)
Water <1 mg/mL
In vivo 1% DMSO+30% PEG 300+dd H2O 30

* 1 mg/ml means slightly soluble or 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 499.61
Formula

C28 H33 N7 O2

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

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02771314 Not yet 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
NCT02511106 Recruiting Stage IB-IIIA Non-small Cell Lung Carcinoma AstraZeneca|Parexel October 2015 Phase 3
NCT02474355 Recruiting Lung Cancer AstraZeneca|Parexel September 2015 Phase 3
NCT02529995 Active, not recruiting Carcinoma, Non-Small-Cell Lung With EGFR Mutation Positive AstraZeneca August 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

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

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

  • 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.

EGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID