Osimertinib (AZD9291)

For research use only.

Catalog No.S7297

213 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 213 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 M3WyRmZ2dmO2aX;uJGF{e2G7 MUS1NEBvVQ>? MkPVNlQhcA>? MmLFSG1UVw>? MkfHbY5lfWOnczDlfJBz\XO|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR5N{OyOUc,OjV2N{ezNlU9N2F-
PC-9/ERc1 MXPGeY5kfGmxbjDBd5NigQ>? MXi1NEBvVQ>? NXrhZYRHOjRiaB?= M37nSGROW09? M{Lqbolv\HWlZYOg[ZhxemW|c3nvckBw\iC2aHWgdJJw[XCxcITveIlkKEKFTD2yJIZidWmueTDt[Y1j\XJiQlnN NFHJcGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS3O|MzPSd-MkW0O|c{OjV:L3G+
VP-2 Mm\4SpVv[3Srb36gRZN{[Xl? M4nkd|UxKG6P NHm1N3ozPCCq MljlSG1UVw>? NIKxNGlqdmS3Y3XzJIV5eHKnc4Ppc44hd2ZidHjlJJBzd2Gyb4D0c5Rq[yCEQ1ytNkBn[W2rbImgcYVu[mW{IFLJUS=> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR5N{OyOUc,OjV2N{ezNlU9N2F-
PC-9/BRc1 NI\ZXIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrpb2dEPTBibl2= MXexNEBl NHjvVHNFVVOR NEDRdFZqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= M1LFXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEe3N|I2Lz5{NUS3O|MzPTxxYU6=
PC-9/ERc1 MlTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzoSpk2OCCwTR?= NYDRd2Y{OTBiZB?= Ml;TSG1UVw>? NUTv[IlRcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBtd26pLYTldo0hMDFyLXThfUkh\3Kxd4ToJIlvcGmkaYTpc44h[XO|YYnz MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR5N{OyOUc,OjV2N{ezNlU9N2F-
VP-2 M4O5SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml36OVAhdk1? MnHKNVAh\A>? NYPKRlVsTE2VTx?= M3nDd4lvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gcI9v\y22ZYLtJEgyOC2mYYmpJIdzd3e2aDDpcohq[mm2aX;uJIF{e2G7cx?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR5N{OyOUc,OjV2N{ezNlU9N2F-
PC9 GR4 NV;2UoNITnWwY4Tpc44hSXO|YYm= NYfZRWx4OC1zMDFOwG0> M1KwN|czKGh? MV;pcohq[mm2c9MgSWdHWiCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gd4lodmGuaX7nxsA> M4W4OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUS4OlM{Lz5{NUm0PFY{OzxxYU6=
PC9 MULGeY5kfGmxbjDBd5NigQ>? MUCwMVExKM7:TR?= M3PsdlczKGh? MUHpcohq[mm2czDXWEBGT0[UIHH0JIxwfyClb37j[Y51emG2aX;udy=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl2OE[zN{c,OjV7NEi2N|M9N2F-
PC9 GR4 M1fOcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInBd3MxNTFyIN88US=> NIrTV|Q4OiCq Mn\HbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NFf2fnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm0PFY{Oyd-MkW5OFg3OzN:L3G+
BAF3 MVHGeY5kfGmxbjDhd5NigQ>? NIDuNFc4OiCq MVfHTVUxKD1iMD6wNFA{KM7:TR?= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
BAF3 M2fvOWZ2dmO2aX;uJIF{e2G7 MoS2O|IhcA>? MlfVS2k2OCB;IECuNFAxOyEQvF2= NH;OTWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
BAF3 M{LLSGZ2dmO2aX;uJIF{e2G7 NXLEUYJrPzJiaB?= MYrHTVUxKD1iMD6wNFEh|ryP NXT5SmFPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
HCC827 NGXkc4RHfW6ldHnvckBie3OjeR?= NXvFeYlzPzJiaB?= Mn30S2k2OCB;IECuNFAyKM7:TR?= NFPlZY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
PC9 NH74clJHfW6ldHnvckBie3OjeR?= NVLCZoV6PzJiaB?= M33EfmdKPTBiPTCwMlAxOiEQvF2= M{\EWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
BAF3 M4nG[mZ2dmO2aX;uJIF{e2G7 NXyyS5hKPCCq NIm0cZlGSzVyIE2gNE4xODJizszN M17POVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
HCC827 NVzPe2xrTnWwY4Tpc44h[XO|YYm= NUPLN3MzOyCq NVTEWFFkUUN3MDC9JFAvODB{NTFOwG0> NXHoR21jRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0N|M5OjlpPkK3OFM{QDJ7PD;hQi=>
H1975 NUDkepg{TnWwY4Tpc44h[XO|YYm= NVHibIdoOyCq NWPZWpF4UUN3MDC9JFAvODB{NTFOwG0> NUjh[5N4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0N|M5OjlpPkK3OFM{QDJ7PD;hQi=>
H3255 M{XsOmZ2dmO2aX;uJIF{e2G7 NXX4TVl2OyCq NWj5d5dzUUN3MDC9JFAvODB2MTFOwG0> NVLCc3Y4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0N|M5OjlpPkK3OFM{QDJ7PD;hQi=>
NCI-H1975 M4Pyd2Z2dmO2aX;uJIF{e2G7 NFy4PJM4OiCq MWHHTVUxKD1iMD6wNFUh|ryP MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
PC9 NEX4dmFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MmLUO|IhcA>? NV7ZU2w4UUN3MDC9JFAvODB4NTFOwG0> Mm[4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5MU[2OFEoRjJ6N{G2OlQyRC:jPh?=
NCI-H1975 MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NXnCSFVKPzJiaB?= MWrJR|UxKD1iMD6wNVA2KM7:TR?= NVSxT21CRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3NVY3PDFpPkK4O|E3PjRzPD;hQi=>
Sf21 MV;GeY5kfGmxbjDhd5NigQ>? NEKybY5KSzVyIE2gNE4xOTJizszN NXvyNoV[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVYzPjdpPkK3PVk3OjZ5PD;hQi=>
PC9-DRH MnrJSpVv[3Srb36gZZN{[Xl? Mln3NkBp NGf3TYNKSzVyIE2gNE4xOTNizszN Mn\rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5NU[yNlIoRjJ4N{W2NlIzRC:jPh?=
BAF3 NVTpfpp2TnWwY4Tpc44h[XO|YYm= MXe3NkBp MVLHTVUxKD1iMD6wNVMh|ryP M{TU[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
HCC827 NUi3XplFTnWwY4Tpc44h[XO|YYm= NVvJO41LQTZiaB?= NELn[mFGSzVyIE2gNE4xOTRizszN NWTYO44zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyNlUzPjlpPkK4NlI2OjZ7PD;hQi=>
HCC827 M1q3[2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MlHWPVYhcA>? M1ridGVEPTBiPTCwMlAyPCEQvF2= M13xdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEWzOVc2Lz5{OEi1N|U4PTxxYU6=
NCI-H1975 MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NXrFcoVJQTZiaB?= NXrCbVlETUN3MDC9JFAvODF2IN88US=> MkH4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6NUO1O|UoRjJ6OEWzOVc2RC:jPh?=
NCI-H1975 NH\GSHVHfW6ldHnvckBie3OjeR?= M2n2VVIhcA>? NYXifYs6UUN3MDC9JFAvODF3IN88US=> NW\acYl{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3OVYzOjJpPkK2O|U3OjJ{PD;hQi=>
H1975 NUnWOXBiTnWwY4Tpc44h[XO|YYm= M4fGd|IhcA>? NFjOdmxKSzVyIE2gNE4xOTVizszN MlLZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7NkiyOVMoRjJ4OU[4NlU{RC:jPh?=
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NCI-H1975 MlHpRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NEWwSZg4OiCq MoPjTWM2OCB;IECuNFE6KM7:TR?= NFHWfWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS2Olc4Oyd-Mkm0OlY4PzN:L3G+
NCI-H1975 MUnGeY5kfGmxbjDhd5NigQ>? MUW5OkBp NX3lbVROTUN3MDC9JFAvODF7IN88US=> NF7jSYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEKyOVI3QSd-MkiyNlUzPjl:L3G+
NCI-H1975 NVvHdHg2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MUm5OkBp NGThZnpGSzVyIE2gNE4xOTlizszN NGXkSVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[wN|k6OSd-Mki2NFM6QTF:L3G+
NCI-H1975 NVPMW5QySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= M3fOVFczKGh? M17KWWlEPTBiPTCwMlAyQSEQvF2= NVHQSodJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OVM{PDBpPkK5PFU{OzRyPD;hQi=>
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human hepatocytes NFy0SmVHfW6ldHnvckBie3OjeR?= M3LaOGlvfHKrboPpZ{BkdGWjcnHuZ4UhcW5iaIXtZY4hcGWyYYTvZ5l1\XNibXXhd5Vz\WRicHXyJFExLzZiY3XscJM> M1LDfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkexPVY{Lz5{NUK3NVk3OzxxYU6=
NCI-H1975 MmToRY51cXS3bX;yJIFkfGm4aYT5JIF{e2G7 NIfJSI9CdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNiaHHyZo9zcW6pIFXHSnIhVDh3OGKvWFk4OE1iZH;1ZoxmKG23dHHueEB5\W6xZ4Lh[pRm\CCrbjDTR2lFKG2xdYPlJIF{e2W|c3XkJIF{KHS3bX;yJIdzd3e2aDDpcohq[mm2aX;uJIF1KDVibXevb4cw\GG7LDDwc{By\CCob4KgO{Bl[Xm|IILlcIF1cX[nIITvJINwdnS{b3y= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ5MUm2N{c,OjV{N{G5OlM9N2F-
NCI-H1975 MmX6SpVv[3Srb36gZZN{[Xl? NFrwUWFU\WynY4Tpeol1gSCrbnTlfEwhemG2aX:gc4YhUUN3MDDmc5IhTUeIUjDUO|kxVS:OOEW4VkBld3WkbHWgcZV1[W62IHX4dJJme3OrbnegbJVu[W5iTlPJMWgyQTd3IHPlcIx{KHSxIFnDOVAh\m:{IIfpcIQhfHmyZTDFS2ZTKGW6cILld5NqdmdiaIXtZY4hSTR|MTDj[Yxtew>? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd|MEG5Nkc,Ojl5M{CxPVI9N2F-
NCI-H1975 M3rSU2FvfGm2dX3vdkBi[3Srdnn0fUBie3OjeR?= NWSySYJlSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhTUeIUjDUO|kxVS:OOEW4VkBld3WkbHWgcZV1[W62IHX4dJJme3OrbnegbJVu[W5iTlPJMWgyQTd3IHPlcIx{KHinbn;ndoFnfGWmIHnuJGJCVEJxYzDheIh6dWmlIH71[IUhdW:3c3WgZZN{\XO|ZXSgZZMhfHWvb4Kg[5Jwf3SqIHnubIljcXSrb36gZZQhOTBibXevb4ctKHCxIHLp[EBnd3JiMkGg[IF6ew>? M1;vRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{OwNVkzLz5{OUezNFE6OjxxYU6=
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HCC827 NYTZfWN5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NEfjZnk4OiCq NH34VY9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDR|gzPyClZXzsd{BifCBzIIXNJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmgdoVt[XSrdnWgeI8h[2:wdILvcC=> M2\GWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUe2NlczLz5{OUW3OlI4OjxxYU6=
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NCI-H1975 M1vZ[2FvfGm2dX3vdkBi[3Srdnn0fUBie3OjeR?= MnfDRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgyQTd3IHPlcIx{KHinbn;ndoFnfGWmIHnuJHNVV0ONLV\vfI4ydnVxTnr1JI52\GVibX;1d4Uh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB1fW2xcjDndo94fGhiYYSgNlAhdWdxa3ev[IF6NCCybzDx[EBnd3JiMUSg[IF6eyC{ZXzheIl3\SC2bzD1cpRz\WG2ZXSgZ49vfHKxbB?= NW\GNIJsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizPVUzOTlpPkK4N|k2OjF7PD;hQi=>
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Caco2 MonsSpVv[3Srb36gZZN{[Xl? MlzvNkBp NGXiTo1CeHCjcnXueEBx\XKvZXHibYxqfHliYXPyc5N{KGGyaXPhcEB1dyCkYYPvcIF1\XKjbDDzbYRmKGmwIHj1cYFvKEOjY3:yJINmdGy|IHH0JFUhfU1iaX7jeYJifGWmIH\vdkAzKGi{cx?= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh3M{W3OUc,Ojh6NUO1O|U9N2F-
Caco2 NFT6NWtHfW6ldHnvckBie3OjeR?= MUOyJIg> MnTuRZBx[XKnboSgdIVzdWWjYnnsbZR6KGGlcn;zd{Bj[XOxbHH0[ZJidCC2bzDhdIlk[Wxic3nk[UBqdiCqdX3hckBE[WOxMjDj[YxteyCjdDC1JJVOKGmwY4XiZZRm\CCob4KgNkBpenN? M2jub|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEWzOVc2Lz5{OEi1N|U4PTxxYU6=
NCI-H1975 MX7GeY5kfGmxbjDhd5NigQ>? MnHCOEBp M4DHXmlvcGmkaYTpc44hd2ZiRVfGVkBNQDV6Uj;UO|kxVSCvdYThcpQhcW5iaIXtZY4hVkOLLVixPVc2KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDBb5QheGixc4Doc5J6dGG2aX;uJIF1KFSqckOwPE9U\XJ2N{Ogd4l1\SCjdDCxJJVOKG2nYYP1doVlKGGodHXyJFQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NYixVXZzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
HCC827 MVTGeY5kfGmxbjDhd5NigQ>? NV;JfJZmPCCq M374TmlvcGmkaYTpc44hd2ZiRVfGVkBmgG:wIEG5JIRmdGW2aX;uJI12fGGwdDDpckBpfW2jbjDIR2M5OjdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGFsfCCyaH;zdIhwenmuYYTpc44h[XRiVHjyN|A5N1OnckS3N{B{cXSnIHH0JFEhfU1ibXXhd5Vz\WRiYX\0[ZIhPCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NHvh[mM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
NCI-H1975 M1u2WGFxd3C2b4Ppd{Bie3OjeR?= NYjjSXFMPDhiaB?= NIfIWlBKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF7DTU1JOTl5NTDj[YxteyCqYYLic5JqdmdiRVfGVkBNQDV6Uj;UO|kxVSCvdYThcpQh[XO|ZYPz[YQh[XNiY3HzdIF{\TNiY3zlZZZi\2ViYYSgNUB2VSCjZoTldkA1QCCqcoOgZpkhcW2vdX7vZoxwfHSrbne= Moj4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
HCC827 NEfPXINCeG:ydH;zbZMh[XO|YYm= NInRdWU1QCCq NEO1UZBKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjDR|gzPyClZXzsd{Bp[XKkb4LpcochTUeIUjDlfI9vKDF7IHTlcIV1cW:wIH31eIFvfCCjc4Pld5Nm\CCjczDjZZNx[XOnLUOgZ4xm[X[jZ3WgZZQhOSC3TTDh[pRmeiB2ODDodpMh[nliaX3teY5w[myxdITpcoc> Mn\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
PC9 NFPNNIZCeG:ydH;zbZMh[XO|YYm= Mk\YOFghcA>? M2\xbGlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iUFO5JINmdGy|IHjhdoJwemmwZzDFS2ZTKGW6b36gNVkh\GWuZYTpc44hdXW2YX70JIF{e2W|c3XkJIF{KGOjc4Dhd4UuOyClbHXheoFo\SCjdDCxJJVOKGGodHXyJFQ5KGi{czDifUBqdW23bn;icI91fGmwZx?= NVTx[49ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
H3255 M1SyfWFxd3C2b4Ppd{Bie3OjeR?= MkfIOFghcA>? MY\JcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEh|MkW1JINmdGy|IHjhdoJwemmwZzDFS2ZTKEx6NUjSJI12fGGwdDDhd5Nme3OnZDDhd{Bk[XOyYYPlMVMh[2ynYY\h[4Uh[XRiMTD1UUBi\nSncjC0PEBpenNiYomgbY1ufW6xYnzveJRqdmd? MoP5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
NCI-H1975 MYPBdI9xfG:|aYOgZZN{[Xl? MU[0PEBp M{[4SGlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iTlPJMWgyQTd3IHPlcIx{KGijcnLvdolv\yCHR1\SJGw5PTiUL2S3PVBOKG23dHHueEBie3Onc4Pl[EBieyCSQWLQJINt\WG4YXflJIF1KDFidV2gZYZ1\XJiNEigbJJ{KGK7IHntcZVvd2Kub4T0bY5o MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
PC9 MYPBdI9xfG:|aYOgZZN{[Xl? M2q1d|Q5KGh? NIHNNmtKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIGDDPUBk\WyuczDoZZJjd3KrbnegSWdHWiCneH;uJFE6KGSnbHX0bY9vKG23dHHueEBie3Onc4Pl[EBieyCSQWLQJINt\WG4YXflJIF1KDFidV2gZYZ1\XJiNEigbJJ{KGK7IHntcZVvd2Kub4T0bY5o MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
HCC827 MkTXRZBweHSxc3nzJIF{e2G7 MoPXOFghcA>? NEW5e4hKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjDR|gzPyClZXzsd{Bp[XKkb4LpcochTUeIUjDlfI9vKDF7IHTlcIV1cW:wIH31eIFvfCCjc4Pld5Nm\CCjczDQRXJRKGOuZXH2ZYdmKGG2IEGgeW0h[W[2ZYKgOFghcHK|IHL5JIludXWwb3Lsc5R1cW6p M13ZTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
H3255 M4rh[GFxd3C2b4Ppd{Bie3OjeR?= MUS0PEBp NXXOSGJlUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIN|I2PSClZXzsd{Bp[XKkb4LpcochTUeIUjDMPFU5WiCvdYThcpQh[XO|ZYPz[YQh[XNiUFHSVEBkdGWjdnHn[UBifCBzIIXNJIFnfGW{IES4JIhzeyCkeTDpcY12dm:kbH;0eIlv\w>? NXH6[ZI6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
NCI-H1975 MlnmSpVv[3Srb36gZZN{[Xl? MoL0V4Vt\WO2aY\peJkhemG2aX:gc4YhUUN3MDDmc5IhcHWvYX6gUmNKNUhzOUe1JINmdGy|IHjhdoJwemmwZzDFS2ZTKEx6NUjSM3Q4QTCPIHTveYJt\SCvdYThcpQhfG9iSVO1NEBnd3JiaIXtZY4hSTR|MTDj[YxteyCqYYLic5Jqdmdid3ns[E11gXCnIFXHSnI> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR{Nkm5Okc,Ojh2Mk[5PVY9N2F-
human hepatocytes MU\GeY5kfGmxbjDhd5NigQ>? MkPwTY51emmwc3njJINt\WG{YX7j[UBqdiCqdX3hckBp\XCjdH;jfZRmeyCjc4Pld5Nm\CCyZYKgcYltdGmxbjDj[Yxtew>? Ml\EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2Mk[5PVYoRjJ6NEK2PVk3RC:jPh?=
rat hepatocytes NXfFUnk3TnWwY4Tpc44h[XO|YYm= MVTJcpRzcW6|aXOgZ4xm[XKjbnPlJIlvKHKjdDDo[ZBifG:leYTld{Bie3Onc4Pl[EBx\XJibXnscIlwdiClZXzsdy=> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR{Nkm5Okc,Ojh2Mk[5PVY9N2F-
A549, NCI-H1975 NUjSZpJZTnWwY4Tpc44h[XO|YYm= M1LBSnNmdGWldHn2bZR6KHKjdHnvJI9nKEmFNUCg[o9zKEWJRj3zeIlufWyjdHXkJJdqdGRidInw[UBGT0[UIHnuJIh2dWGwIFG1OFkh[2WubIOgeI8hUUN3MDDmc5IhTUeIUjDMPFU5Wi:WN{mwUUBld3WkbHWgcZV1[W62IHnuJIh2dWGwIF7DTU1JOTl5NTDj[Yxtew>? MkThQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5NU[yNlIoRjJ4N{W2NlIzRC:jPh?=
A549, PC9 MYnGeY5kfGmxbjDhd5NigQ>? M4DmdnNmdGWldHn2bZR6KHKjdHnvJI9nKEmFNUCg[o9zKEWJRj3zeIlufWyjdHXkJJdqdGRidInw[UBGT0[UIHnuJIh2dWGwIFG1OFkh[2WubIOgeI8hUUN3MDDmc5IhTUeIUjDk[YxmfGmxbjDteZRidnRiaX6gbJVu[W5iUFO5JINmdGy| MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd3NkKyNkc,OjZ5NU[yNlI9N2F-
HCC827 MofHRZBweHSxc3nzJIF{e2G7 NVnnbGhkUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIR2M5OjdiY3XscJMhcGG{Yn;ybY5oKEWJRmKgSVc1PiC2bzDBO|UxKGSnbHX0bY9vKG23dHHueEBie3Onc4Pl[EBieyCnYYLsfUBieG:ydH;0bYMh[2WubIOgZZQhOyC3TTDh[pRmeiB{NDDodpMh[nliQX7u[ZhqdiCYLV\JWGMweHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{Bj[XOnZDDmcI94KGO7dH;t[ZRzgSBqUo\iJF0hOS5|NDD0c{AyNjZ5JTm= MoW3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NUOzOFAoRjJ7OEWzN|QxRC:jPh?=
NCI-H1975 NV7BZnVWTnWwY4Tpc44h[XO|YYm= NXSwR4ZSUW6qaXLpeIlwdiCxZjDFS2ZTKEx6NUjSM3Q4QTCPIHTveYJt\SCvdYThcpQheGixc4Doc5J6dGG2aX;uJIlvKEWJRj3zeIlufWyjdHXkJIh2dWGwIF7DTU1JOTl5NTDj[YxteyCjdDCxJJRwKDFyMDDuUUBjgSCZZYP0[ZJvKGKub4SgcYV1cG:m MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTlyNkGxOEc,Ojl7ME[xNVQ9N2F-
A431 NGKwT5dHfW6ldHnvckBie3OjeR?= NV;YXnI5W2WuZXP0bZZqfHlicnH0bY8tKHKjdHnvJGlEPTBiZn;yJIh2dWGwIFG0N|Eh[2WubIOgc5ZmemW6cILld5Nqdmdid3ns[E11gXCnIFXHSnIhfG9iSVO1NEBnd3JiaIXtZY4hVkOLLVixPVc2KGOnbHzzJIV5eHKnc4PpcochTUeIUjDUO|kxVS:OOEW4VkBufXSjboS= Mn3QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzM{G2N|koRjJ5MUOxOlM6RC:jPh?=
PC9 NHnkVZpCdnSrdIXtc5Ih[WO2aY\peJkh[XO|YYm= MlLtRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFO5JINmdGy|IHjhdoJwemmwZzDFS2ZTKGW6b36gNVkh\GWuZYTpc44h[WO2aY\heIlv\yCvdYThcpQhgGWwb3fyZYZ1\WRiaX6gV2NKTCCvb4Xz[UBie3Onc4Pl[EBieyC2dX3vdkBoem:5dHigbY5pcWKrdHnvckBifCBzMDDt[{9s\y:mYYmsJJBwKHGmIH\vdkA4KGSjeYOgdoVt[XSrdnWgeI8h[2:wdILvcC=> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ5MUm2N{c,OjV{N{G5OlM9N2F-
A431 NV\lSoUySW62aYT1cY9zKGGldHn2bZR6KGG|c3H5 M1j2NmFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0N|Eh[2WubIOgfIVvd2e{YX\0[YQhcW5iU1PJSEBud3W|ZTDhd5Nme3OnZDDhd{B1fW2xcjDndo94fGhiaX7obYJqfGmxbjDheEA2KG2pL3vnM4RigSxicH:gdYQh\m:{IEeg[IF6eyC{ZXzheIl3\SC2bzDjc451em:u MkP0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{N{G5OlMoRjJ3MkexPVY{RC:jPh?=

... 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)
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):
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 N/A
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