Osimertinib (AZD9291)

For research use only.

Catalog No.S7297 Synonyms: Mereletinib

221 publications

Osimertinib (AZD9291) Chemical Structure

CAS No. 1421373-65-0

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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Selleck's Osimertinib (AZD9291) has been cited by 221 publications

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
PC-9/BRc1 NFjDdXhHfW6ldHnvckBCe3OjeR?= NXrsXW4zPTBibl2= MUGyOEBp M1jNc2ROW09? NVfPcmxmcW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0> NG\yVlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS3O|MzPSd-MkW0O|c{OjV:L3G+
PC-9/ERc1 NF;OR45HfW6ldHnvckBCe3OjeR?= MmLxOVAhdk1? MkTQNlQhcA>? NHG5UXZFVVOR MkXubY5lfWOnczDlfJBz\XO|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2= NFPLNng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS3O|MzPSd-MkW0O|c{OjV:L3G+
VP-2 NGrZR|dHfW6ldHnvckBCe3OjeR?= MV[1NEBvVQ>? MlLJNlQhcA>? NEP0RVZFVVOR NUS2bGk1cW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0> MlTHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2N{ezNlUoRjJ3NEe3N|I2RC:jPh?=
PC-9/BRc1 M37KcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX61NEBvVQ>? MmG0NVAh\A>? MV;EUXNQ NVTMUHBrcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBtd26pLYTldo0hMDFyLXThfUkh\3Kxd4ToJIlvcGmkaYTpc44h[XO|YYnz MoLTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2N{ezNlUoRjJ3NEe3N|I2RC:jPh?=
PC-9/ERc1 MlzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7KW|dVPTBibl2= MkfYNVAh\A>? MkjoSG1UVw>? NGC5dI5qdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= MlTqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2N{ezNlUoRjJ3NEe3N|I2RC:jPh?=
VP-2 NIPSdJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVO1NEBvVQ>? NHL4eoMyOCCm NE\3ZolFVVOR NH3TPFBqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR5N{OyOUc,OjV2N{ezNlU9N2F-
PC9 GR4 NEjSfXZHfW6ldHnvckBCe3OjeR?= MYiwMVExKM7:TR?= M4DMSFczKGh? M2fjdIlvcGmkaYTzxsBGT0[UIIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUB{cWewYXzpcofDqA>? M162Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUS4OlM{Lz5{NUm0PFY{OzxxYU6=
PC9 M1HrbmZ2dmO2aX;uJGF{e2G7 MWCwMVExKM7:TR?= NVjITFRiPzJiaB?= M{GzOIlvcGmkaYTzJHdVKEWJRmKgZZQhdG:5IHPvcoNmdnS{YYTpc45{ MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl2OE[zN{c,OjV7NEi2N|M9N2F-
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H1975 Mn\YSpVv[3Srb36gZZN{[Xl? NU\SfnV1OyCq NY[4T|Y3UUN3MDC9JFAvODB{NTFOwG0> NWq4foNPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0N|M5OjlpPkK3OFM{QDJ7PD;hQi=>
H3255 MUjGeY5kfGmxbjDhd5NigQ>? M3\YUFMhcA>? M1\xbmlEPTBiPTCwMlAxPDFizszN MlfkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd2M{O4NlkoRjJ5NEOzPFI6RC:jPh?=
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NCI-H1975 NGC3TVJHfW6ldHnvckBie3OjeR?= MYG5OkBp MlfRSWM2OCB;IECuNFE6KM7:TR?= NGDjOng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEKyOVI3QSd-MkiyNlUzPjl:L3G+
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NCI-H1975 M2PLcWZ2dmO2aX;uJIF{e2G7 MYTT[Yxm[3Srdnn0fUBz[XSrbzDv[kBKSzVyIH\vdkBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNiaHHyZo9zcW6pIFXHSnIhVDh3OGKvWFc6OE1iZH;1ZoxmKG23dHHueEB1dyCLQ{WwJIZweiCqdX3hckBCPDNzIHPlcIx{KGijcnLvdolv\yC5aXzkMZR6eGViRVfGVi=> M2HWRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NEK2PVk3Lz5{OESyOlk6PjxxYU6=
human hepatocytes M4W5cmZ2dmO2aX;uJIF{e2G7 Ml\PTY51emmwc3njJINt\WG{YX7j[UBqdiCqdX3hckBp\XCjdH;jfZRmeyCjc4Pld5Nm\CCyZYKgcYltdGmxbjDj[Yxtew>? NX;LZVJuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0NlY6QTZpPkK4OFI3QTl4PD;hQi=>
rat hepatocytes NXT6XYpzTnWwY4Tpc44h[XO|YYm= M1q4OWlvfHKrboPpZ{BkdGWjcnHuZ4UhcW5icnH0JIhmeGG2b3P5eIV{KGG|c3Xzd4VlKHCncjDtbYxtcW:wIHPlcIx{ M1zUXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NEK2PVk3Lz5{OESyOlk6PjxxYU6=
A549, NCI-H1975 MYfGeY5kfGmxbjDhd5NigQ>? MXTT[Yxm[3Srdnn0fUBz[XSrbzDv[kBKSzVyIH\vdkBGT0Zvc4TpcZVt[XSnZDD3bYxlKHS7cHWgSWdHWiCrbjDoeY1idiCDNUS5JINmdGy|IITvJGlEPTBiZn;yJGVITlJiTEi1PHIwXDd7MF2g[I92[mynIH31eIFvfCCrbjDoeY1idiCQQ1mtTFE6PzViY3XscJM> NETodVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke1OlIzOid-Mk[3OVYzOjJ:L3G+
A549, PC9 MYDGeY5kfGmxbjDhd5NigQ>? MmT2V4Vt\WO2aY\peJkhemG2aX:gc4YhUUN3MDDmc5IhTUeILYP0bY12dGG2ZXSge4lt\CC2eYDlJGVITlJiaX6gbJVu[W5iQUW0PUBk\WyuczD0c{BKSzVyIH\vdkBGT0[UIHTlcIV1cW:wIH31eIFvfCCrbjDoeY1idiCSQ{mgZ4VtdHN? M4HKbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{W2NlIzLz5{Nke1OlIzOjxxYU6=
HCC827 Mn7uRZBweHSxc3nzJIF{e2G7 M2rnOmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSFPDPFI4KGOnbHzzJIhiemKxcnnu[{BGT0[UIFW3OFYhfG9iQUe1NEBl\WyndHnvckBufXSjboSgZZN{\XO|ZXSgZZMh\WG{bImgZZBweHSxdHnjJINmdGy|IHH0JFMhfU1iYX\0[ZIhOjRiaILzJIJ6KEGwbnX4bY4hXi2ISWTDM5Bzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnegZoF{\WRiZnzve{BkgXSxbXX0dpkhMFK4YjC9JFEvOzRidH:gNU43PyVr NHTaSnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi1N|M1OCd-Mkm4OVM{PDB:L3G+
NCI-H1975 M1L5UmZ2dmO2aX;uJIF{e2G7 NUnmWXljUW6qaXLpeIlwdiCxZjDFS2ZTKEx6NUjSM3Q4QTCPIHTveYJt\SCvdYThcpQheGixc4Doc5J6dGG2aX;uJIlvKEWJRj3zeIlufWyjdHXkJIh2dWGwIF7DTU1JOTl5NTDj[YxteyCjdDCxJJRwKDFyMDDuUUBjgSCZZYP0[ZJvKGKub4SgcYV1cG:m M17qU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUC2NVE1Lz5{OUmwOlEyPDxxYU6=
A431 NYDUV4hJTnWwY4Tpc44h[XO|YYm= MnHvV4Vt\WO2aY\peJkhemG2aX:sJJJifGmxIFnDOVAh\m:{IHj1cYFvKEF2M{GgZ4VtdHNib4\ldoV5eHKnc4Ppcochf2muZD30fZBmKEWJRmKgeI8hUUN3MDDmc5IhcHWvYX6gUmNKNUhzOUe1JINmdGy|IHX4dJJme3OrbnegSWdHWiCWN{mwUU9NQDV6UjDteZRidnR? NFTuS5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVY{QSd-MkexN|E3Ozl:L3G+
PC9 MlG2RY51cXS3bX;yJIFkfGm4aYT5JIF{e2G7 MUHBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{mgZ4VtdHNiaHHyZo9zcW6pIFXHSnIh\XixbjCxPUBl\WyndHnvckBi[3SrdnH0bY5oKG23dHHueEB5\W6xZ4Lh[pRm\CCrbjDTR2lFKG2xdYPlJIF{e2W|c3XkJIF{KHS3bX;yJIdzd3e2aDDpcohq[mm2aX;uJIF1KDFyIH3nM4toN2SjeTygdI8heWRiZn;yJFch\GG7czDy[YxifGm4ZTD0c{Bkd262cn;s MmCzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{N{G5OlMoRjJ3MkexPVY{RC:jPh?=
A431 MmjpRY51cXS3bX;yJIFkfGm4aYT5JIF{e2G7 NFTSdGZCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFMyKGOnbHzzJJhmdm:pcnHmeIVlKGmwIGPDTWQhdW:3c3WgZZN{\XO|ZXSgZZMhfHWvb4Kg[5Jwf3SqIHnubIljcXSrb36gZZQhPSCvZz;r[{9l[XluIIDvJJFlKG[xcjC3JIRigXNicnXsZZRqfmVidH:gZ49vfHKxbB?= NH3sSVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK3NVk3Oyd-MkWyO|E6PjN:L3G+

... 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]

- Collapse
  • Animal Models: Mice bearing PC9 and H1975 xenograft tumors
  • Dosages: ~5 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 99 mg/mL warmed (198.15 mM)
Water Insoluble
Ethanol '43 mg/mL warmed
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.
7.5mg/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 Mereletinib
Smiles CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

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

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

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

Dilution Calculator

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

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

  • C1
    V1
    C2
    V2

* 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

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02841579 Completed 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 Completed 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

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

  • * Indicates a Required Field

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.

EGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID