Osimertinib (AZD9291)

Catalog No.S7297

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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Osimertinib (AZD9291) Chemical Structure

Osimertinib (AZD9291) Chemical Structure
Molecular Weight: 499.61

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Product Description

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.
Targets L858R/T790M EGFR [1]
(LoVo cells)
Exon 19 deletion EGFR [1]
(LoVo cells)
WT EGFR [1]
(LoVo cells)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
PC9 GR4M4Hv[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M{PMNlAuOTBizszNMk\0O|IhcA>?MV\pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5NFP3WoYzPTl2OE[zNy=>
PC9MVTGeY5kfGmxbjDBd5NigQ>?Mn3vNE0yOCEQvF2=NXu0NoxuPzJiaB?=NH7vNpdqdmirYnn0d{BYXCCHR1\SJIF1KGyxdzDjc45k\W62cnH0bY9vew>?MnvyNlU6PDh4M{O=
PC9 GR4NIntXohHfW6ldHnvckBCe3OjeR?=NI\YUGUxNTFyIN88US=>NGrwZVY4OiCqMUPpcohq[mm2c9MgSWdHWiCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gd4lodmGuaX7nxsA>M3fydVI2QTR6NkOz
VP-2MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M4PWelUxKG6PNXjqTlFXOTBiZB?=NUn3cFY1TE2VTx?=NFW4TXNqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO=M4rG[|I2PDd5M{K1
PC-9/ERc1MnXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M3zaRVUxKG6PMVuxNEBlNHPHbWxFVVORNGK0PJZqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO=MWWyOVQ4PzN{NR?=
PC-9/BRc1NYjud4F7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MUe1NEBvVQ>?M3v5eFExKGR?M{S4bmROW09?M1zBN4lvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gcI9v\y22ZYLtJEgyOC2mYYmpJIdzd3e2aDDpcohq[mm2aX;uJIF{e2G7cx?=M{nMflI2PDd5M{K1
VP-2NHHXS41HfW6ldHnvckBCe3OjeR?=NFXucII2OCCwTR?=Mn;jNlQhcA>?MXPEUXNQNVTzN3ptcW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0>M{fDfFI2PDd5M{K1
PC-9/ERc1NV\BSFQ6TnWwY4Tpc44hSXO|YYm=NH;D[mY2OCCwTR?=NHj0bGozPCCqM4f6cGROW09?MWnpcoR2[2W|IHX4dJJme3Orb36gc4YhfGinIIDyc4Fxd3C2b4TpZ{BDS0xvMjDmZY1qdHlibXXtZoVzKEKLTR?=NFjQbIMzPTR5N{OyOS=>
PC-9/BRc1MXHGeY5kfGmxbjDBd5NigQ>?M{i5e|UxKG6PMlO4NlQhcA>?MXLEUXNQMlq4bY5lfWOnczDlfJBz\XO|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2=NYr4Z2p[OjV2N{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]
Features Orally bioavailable mutant-selective EGFR inhibitor that has been tested in Phase III clinical trials for treatment of Non-Small Cell Lung Cancer.

Protocol(Only for Reference)

Kinase Assay: [1]

EGFR cellular phosphorylation assay Cells are seeded (10000 cells/well) in growth medium in Corning black, clear- bottomed 384-well plates and incubated at 37°C with 5% CO2 overnight. Cells are acoustically dosed using an Echo 555, with compounds serially diluted in 100% DMSO. Plates are incubated for a further 2h, then following aspiration of medium, 40μL lx lysis buffer is added to each well. Greiner black high bind 384-well plates are coated with capture antibody and then blocked with 3% BSA. Following removal of block, 15μL of lysate are transferred to the Greiner black high bind 384-well plates and incubated for 2 hours. Following aspiration and washing of the plates with PBS, 20μL, of detection antibody were added and incubated for 2 hours. Following aspiration and washing of the plates with PBS, 20μL of QuantaBlu fluorogenic peroxidase substrate are added and incubated for 1 hour. 20μL QuantaBlu stop solution are added to plates and fluorescence read on an Envision plate reader using Excitation 352nm wavelength and emission 460nm wavelength. The data obtained with each compound is exported into a suitable software package to perform curve fitting analysis. From this data an IC50 value is determined by calculation of the concentration of compound that is required to give a 50% effect.

Animal Study: [2]

Animal Models Mice bearing PC9 and H1975 xenograft tumors
Formulation
Dosages ~5 mg/kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Patent. 2013, WO2013014448 A1.

[2] Cross, et al. Mol Cancer Ther. 2013, 12, A109.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

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|Singa  ...more 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

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Chemical Information

Download Osimertinib (AZD9291) SDF
Molecular Weight (MW) 499.61
Formula

C28 H33 N7 O2

CAS No. 1421373-65-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 99 mg/mL warming (198.15 mM)
Ethanol 43 mg/mL warming (86.06 mM)
Water <1 mg/mL (<1 mM)
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 Name 2-​Propenamide, N-​[2-​[[2-​(dimethylamino)​ethyl]​methylamino]​-​4-​methoxy-​5-​[[4-​(1-​methyl-​1H-​indol-​3-​yl)​-​2-​pyrimidinyl]​amino]​phenyl]​-

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.

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.

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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