Osimertinib (AZD9291)

Catalog No.S7297 Synonyms: Mereletinib

For research use only.

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.

Osimertinib (AZD9291) Chemical Structure

CAS No. 1421373-65-0

Selleck's Osimertinib (AZD9291) has been cited by 301 publications

Purity & Quality Control

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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
PC-9/BRc1 Mof1SpVv[3Srb36gRZN{[Xl? MWi1NEBvVQ>? NIr2RWgzPCCq MWPEUXNQ MnjPbY5lfWOnczDlfJBz\XO|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2= M1zxW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEe3N|I2Lz5{NUS3O|MzPTxxYU6=
PC-9/ERc1 M1jQbGZ2dmO2aX;uJGF{e2G7 NHK0SlY2OCCwTR?= M1S0eVI1KGh? M1T5S2ROW09? MYDpcoR2[2W|IHX4dJJme3Orb36gc4YhfGinIIDyc4Fxd3C2b4TpZ{BDS0xvMjDmZY1qdHlibXXtZoVzKEKLTR?= NXr5bY5sRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0O|c{OjVpPkK1OFc4OzJ3PD;hQi=>
VP-2 MWLGeY5kfGmxbjDBd5NigQ>? NV;iT|A3PTBibl2= MYiyOEBp M1LHe2ROW09? NIf4Z2JqdmS3Y3XzJIV5eHKnc4Ppc44hd2ZidHjlJJBzd2Gyb4D0c5Rq[yCEQ1ytNkBn[W2rbImgcYVu[mW{IFLJUS=> NYOyUG1QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0O|c{OjVpPkK1OFc4OzJ3PD;hQi=>
PC-9/BRc1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFv0S3E2OCCwTR?= MmO0NVAh\A>? MXrEUXNQ NH3zb4VqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= M3PvcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEe3N|I2Lz5{NUS3O|MzPTxxYU6=
PC-9/ERc1 NFLNU|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnG3OVAhdk1? M4OybVExKGR? NGLGRXVFVVOR MVXpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHzvcocufGW{bTCoNVAu\GG7KTDndo94fGhiaX7obYJqfGmxbjDhd5NigXN? NIPoTms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS3O|MzPSd-MkW0O|c{OjV:L3G+
VP-2 NXy1NIlyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLPOVAhdk1? NIDOTWcyOCCm MknmSG1UVw>? M3P1SYlvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gcI9v\y22ZYLtJEgyOC2mYYmpJIdzd3e2aDDpcohq[mm2aX;uJIF{e2G7cx?= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR5N{OyOUc,OjV2N{ezNlU9N2F-
PC9 GR4 NV7xNoRQTnWwY4Tpc44hSXO|YYm= M4XYclAuOTBizszN MmfUO|IhcA>? NVqzNJJIcW6qaXLpeJPDqEWJRmKgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKHOrZ37hcIlv\8Li NWfIXFlwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OFg3OzNpPkK1PVQ5PjN|PD;hQi=>
PC9 NHLDbIxHfW6ldHnvckBCe3OjeR?= NWHqZpVpOC1zMDFOwG0> MnvrO|IhcA>? MlOxbY5pcWKrdIOgW3QhTUeIUjDheEBtd3diY3;uZ4VvfHKjdHnvcpM> M4fZe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUS4OlM{Lz5{NUm0PFY{OzxxYU6=
PC9 GR4 M4O3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;ZO4xUOC1zMDFOwG0> NVqxTW9sPzJiaB?= MVzpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NV3ONmNFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OFg3OzNpPkK1PVQ5PjN|PD;hQi=>
BAF3 MVrGeY5kfGmxbjDhd5NigQ>? NEPv[pA4OiCq Mm\6S2k2OCB;IECuNFAxOyEQvF2= NUPTPGNFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
BAF3 MUXGeY5kfGmxbjDhd5NigQ>? M3LwZlczKGh? Mk\WS2k2OCB;IECuNFAxOyEQvF2= NIHlclA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
BAF3 MWPGeY5kfGmxbjDhd5NigQ>? NYLPeYhVPzJiaB?= M1S0bmdKPTBiPTCwMlAxOSEQvF2= MoPOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
HCC827 NEfITFRHfW6ldHnvckBie3OjeR?= Mn\nO|IhcA>? MVXHTVUxKD1iMD6wNFEh|ryP MmTMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
PC9 MlnQSpVv[3Srb36gZZN{[Xl? MlXKO|IhcA>? MoHnS2k2OCB;IECuNFAzKM7:TR?= NEmxZlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
BAF3 MXjGeY5kfGmxbjDhd5NigQ>? NV7IcWlRPCCq NXG4XWxRTUN3MDC9JFAvODB{IN88US=> NFq1XZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
HCC827 MXjGeY5kfGmxbjDhd5NigQ>? Ml3rN{Bp NWf6cGZwUUN3MDC9JFAvODB{NTFOwG0> M4LFT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NEOzPFI6Lz5{N{SzN|gzQTxxYU6=
H1975 NYLFOmZqTnWwY4Tpc44h[XO|YYm= M1m1XFMhcA>? Moi1TWM2OCB;IECuNFAzPSEQvF2= NHL2OIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{SzN|gzQSd-Mke0N|M5Ojl:L3G+
H3255 MYXGeY5kfGmxbjDhd5NigQ>? M1f2fFMhcA>? MVzJR|UxKD1iMD6wNFQyKM7:TR?= NY[0WIp4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0N|M5OjlpPkK3OFM{QDJ7PD;hQi=>
NCI-H1975 MlfGSpVv[3Srb36gZZN{[Xl? NH\lTpg4OiCq NULwTZcyT0l3MDC9JFAvODB3IN88US=> Mo\KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
PC9 NXXZNGVPSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NUK1TJJEPzJiaB?= NIniVWpKSzVyIE2gNE4xODZ3IN88US=> M{TBTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{G2OlQyLz5{OEexOlY1OTxxYU6=
NCI-H1975 MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MXS3NkBp NIrkZYJKSzVyIE2gNE4xOTB3IN88US=> NFnLdnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEexOlY1OSd-Mki3NVY3PDF:L3G+
Sf21 MXnGeY5kfGmxbjDhd5NigQ>? M1nrNGlEPTBiPTCwMlAyOiEQvF2= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NkK2O{c,Ojd7OU[yOlc9N2F-
PC9-DRH MXvGeY5kfGmxbjDhd5NigQ>? MVKyJIg> NYP6XVhEUUN3MDC9JFAvODF|IN88US=> NGLvS2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke1OlIzOid-Mk[3OVYzOjJ:L3G+
BAF3 NFT0c2FHfW6ldHnvckBie3OjeR?= M{HZVlczKGh? NIHNbGFIUTVyIE2gNE4xOTNizszN MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
HCC827 NUOxfmRSTnWwY4Tpc44h[XO|YYm= M1nOTVk3KGh? Mn7lSWM2OCB;IECuNFE1KM7:TR?= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ{NUK2PUc,Ojh{MkWyOlk9N2F-
HCC827 NF\vTGhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NXK0NGJIQTZiaB?= M4C1NWVEPTBiPTCwMlAyPCEQvF2= MonYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6NUO1O|UoRjJ6OEWzOVc2RC:jPh?=
NCI-H1975 NUHp[oI2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MmLXPVYhcA>? M{fIWWVEPTBiPTCwMlAyPCEQvF2= NHLK[ms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEi1N|U4PSd-Mki4OVM2PzV:L3G+
NCI-H1975 M2C5dGZ2dmO2aX;uJIF{e2G7 MkLpNkBp MVHJR|UxKD1iMD6wNVUh|ryP MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd3NkKyNkc,OjZ5NU[yNlI9N2F-
H1975 MUPGeY5kfGmxbjDhd5NigQ>? MViyJIg> Mn:4TWM2OCB;IECuNFE2KM7:TR?= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl4OEK1N{c,OjZ7NkiyOVM9N2F-
PC9 MXvGeY5kfGmxbjDhd5NigQ>? MkXJNkBp NGDmSHJKSzVyIE2gNE4xOTdizszN MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl4OEK1N{c,OjZ7NkiyOVM9N2F-
NCI-H1975 NEHUUpFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NUnHS5hUPzJiaB?= Mo\RTWM2OCB;IECuNFE6KM7:TR?= M4PtblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NE[2O|c{Lz5{OUS2Olc4OzxxYU6=
NCI-H1975 NFGw[XdHfW6ldHnvckBie3OjeR?= MVe5OkBp MnG4SWM2OCB;IECuNFE6KM7:TR?= M4jYSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkK1NlY6Lz5{OEKyOVI3QTxxYU6=
NCI-H1975 NW\KU3k{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NH\zPZI6PiCq Ml;WSWM2OCB;IECuNFE6KM7:TR?= M{C5V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkCzPVkyLz5{OE[wN|k6OTxxYU6=
NCI-H1975 M2exXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NIX4eJA4OiCq MYTJR|UxKD1iMD6wNVkh|ryP M1zVWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OEWzN|QxLz5{OUi1N|M1ODxxYU6=
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NCI-H1975 M2nMS2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M1;4elczKGh? NFzKelFKSzVyIE2gNE4xOjNizszN NYPkWWxxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1N|Q6OjZpPkK5OVM1QTJ4PD;hQi=>
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NCI-H1975 MlnKR5l1d3SxeHnjbZR6KGG|c3H5 MX[3NkBp MlvRS2k2OCB;IECuNFI1KM7:TR?= NY[4N3RXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyO|E6PjNpPkK1NlcyQTZ|PD;hQi=>
HCC827 NVO5cnRUSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NVf6XIVnPzJiaB?= MnfXTWM2OCB;IECuNFI2PCEQvF2= MmS3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3N{[yO|IoRjJ7NUe2NlczRC:jPh?=
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NCI-H1975 M2jpbmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M{m5VlczKGh? NVXIV21HUUN3MDC9JFAvODNizszN NX3lcXloRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiwN|M2PzlpPkK4NFM{PTd7PD;hQi=>
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NCI-H1975 M{fZOmZ2dmO2aX;uJIF{e2G7 NFTlflYyKGh? M1;hUGlEPTBiPTCwMlA1OSEQvF2= NX61PXZyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1N|Q6OjZpPkK5OVM1QTJ4PD;hQi=>
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NCI-H1975 Mn3VRY51cXS3bX;yJIFkfGm4aYT5JIF{e2G7 MkS5RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgyQTd3IHPlcIx{KHinbn;ndoFnfGWmIHnuJHNVV0ONLV\vfI4ydnVxTnr1JI52\GVibX;1d4Uh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB1fW2xcjDndo94fGhiYYSgNlAhdWdxa3ev[IF6NCCybzDx[EBnd3JiMUSg[IF6eyC{ZXzheIl3\SC2bzD1cpRz\WG2ZXSgZ49vfHKxbB?= NIflfGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEO5OVIyQSd-MkizPVUzOTl:L3G+
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Caco2 NVztSYdWTnWwY4Tpc44h[XO|YYm= Mon3NkBp M361NWFxeGG{ZX70JJBmem2nYXLpcIl1gSCjY4Lvd5Mh[XCrY3HsJJRwKGKjc3;sZZRmemGuIIPp[IUhcW5iaIXtZY4hS2Glb{KgZ4VtdHNiYYSgOUB2VSCrbnP1ZoF1\WRiZn;yJFIhcHK| MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh3M{W3OUc,Ojh6NUO1O|U9N2F-
Caco2 MoK3SpVv[3Srb36gZZN{[Xl? MVyyJIg> NIO3NWhCeHCjcnXueEBx\XKvZXHibYxqfHliYXPyc5N{KGKjc3;sZZRmemGuIITvJIFxcWOjbDDzbYRmKGmwIHj1cYFvKEOjY3:yJINmdGy|IHH0JFUhfU1iaX7jeYJifGWmIH\vdkAzKGi{cx?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh3M{W3OUc,Ojh6NUO1O|U9N2F-
NCI-H1975 MVrGeY5kfGmxbjDhd5NigQ>? NU\CUG1iPCCq NV7TclVSUW6qaXLpeIlwdiCxZjDFS2ZTKEx6NUjSM3Q4QTCPIH31eIFvfCCrbjDoeY1idiCQQ1mtTFE6PzViY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGFsfCCyaH;zdIhwenmuYYTpc44h[XRiVHjyN|A5N1OnckS3N{B{cXSnIHH0JFEhfU1ibXXhd5Vz\WRiYX\0[ZIhPCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NXzRcWxjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
HCC827 NGq0SmVHfW6ldHnvckBie3OjeR?= MUK0JIg> M4D0VWlvcGmkaYTpc44hd2ZiRVfGVkBmgG:wIEG5JIRmdGW2aX;uJI12fGGwdDDpckBpfW2jbjDIR2M5OjdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGFsfCCyaH;zdIhwenmuYYTpc44h[XRiVHjyN|A5N1OnckS3N{B{cXSnIHH0JFEhfU1ibXXhd5Vz\WRiYX\0[ZIhPCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| MkjQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
NCI-H1975 M4S4fGFxd3C2b4Ppd{Bie3OjeR?= M3myWFQ5KGh? MUXJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKE6FST3INVk4PSClZXzsd{Bp[XKkb4LpcochTUeIUjDMPFU5Wi:WN{mwUUBufXSjboSgZZN{\XO|ZXSgZZMh[2G|cHHz[VMh[2ynYY\h[4Uh[XRiMTD1UUBi\nSncjC0PEBpenNiYomgbY1ufW6xYnzveJRqdmd? M{\FU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
HCC827 MV3BdI9xfG:|aYOgZZN{[Xl? MkjqOFghcA>? MnjrTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKQ1O4Nlch[2WubIOgbIFz[m:{aX7nJGVITlJiZYjvckAyQSCmZXzleIlwdiCvdYThcpQh[XO|ZYPz[YQh[XNiY3HzdIF{\S1|IHPs[YF3[WenIHH0JFEhfU1iYX\0[ZIhPDhiaILzJIJ6KGmvbYXuc4Jtd3S2aX7n NVrqeWs6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
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NCI-H1975 MXXBdI9xfG:|aYOgZZN{[Xl? MUG0PEBp Mn;CTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCQQ1mtTFE6PzViY3XscJMhcGG{Yn;ybY5oKEWJRmKgUFg2QFJxVEe5NG0hdXW2YX70JIF{e2W|c3XkJIF{KFCDUmCgZ4xm[X[jZ3WgZZQhOSC3TTDh[pRmeiB2ODDodpMh[nliaX3teY5w[myxdITpcoc> NH\ncpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
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NCI-H1975 M1\kZ2Z2dmO2aX;uJIF{e2G7 MorBV4Vt\WO2aY\peJkhemG2aX:gc4YhUUN3MDDmc5IhcHWvYX6gUmNKNUhzOUe1JINmdGy|IHjhdoJwemmwZzDFS2ZTKEx6NUjSM3Q4QTCPIHTveYJt\SCvdYThcpQhfG9iSVO1NEBnd3JiaIXtZY4hSTR|MTDj[YxteyCqYYLic5Jqdmdid3ns[E11gXCnIFXHSnI> Mme2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2Mk[5PVYoRjJ6NEK2PVk3RC:jPh?=
human hepatocytes NGjOZXNHfW6ldHnvckBie3OjeR?= MnLLTY51emmwc3njJINt\WG{YX7j[UBqdiCqdX3hckBp\XCjdH;jfZRmeyCjc4Pld5Nm\CCyZYKgcYltdGmxbjDj[Yxtew>? MlrQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2Mk[5PVYoRjJ6NEK2PVk3RC:jPh?=
rat hepatocytes NFG3RVVHfW6ldHnvckBie3OjeR?= MYfJcpRzcW6|aXOgZ4xm[XKjbnPlJIlvKHKjdDDo[ZBifG:leYTld{Bie3Onc4Pl[EBx\XJibXnscIlwdiClZXzsdy=> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR{Nkm5Okc,Ojh2Mk[5PVY9N2F-
A549, NCI-H1975 NXviW|hLTnWwY4Tpc44h[XO|YYm= M13iXnNmdGWldHn2bZR6KHKjdHnvJI9nKEmFNUCg[o9zKEWJRj3zeIlufWyjdHXkJJdqdGRidInw[UBGT0[UIHnuJIh2dWGwIFG1OFkh[2WubIOgeI8hUUN3MDDmc5IhTUeIUjDMPFU5Wi:WN{mwUUBld3WkbHWgcZV1[W62IHnuJIh2dWGwIF7DTU1JOTl5NTDj[Yxtew>? M4L2R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{W2NlIzLz5{Nke1OlIzOjxxYU6=
A549, PC9 M4DlVGZ2dmO2aX;uJIF{e2G7 M4jFb3NmdGWldHn2bZR6KHKjdHnvJI9nKEmFNUCg[o9zKEWJRj3zeIlufWyjdHXkJJdqdGRidInw[UBGT0[UIHnuJIh2dWGwIFG1OFkh[2WubIOgeI8hUUN3MDDmc5IhTUeIUjDk[YxmfGmxbjDteZRidnRiaX6gbJVu[W5iUFO5JINmdGy| M3v3XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{W2NlIzLz5{Nke1OlIzOjxxYU6=
HCC827 MX7BdI9xfG:|aYOgZZN{[Xl? NYrtUoZkUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIR2M5OjdiY3XscJMhcGG{Yn;ybY5oKEWJRmKgSVc1PiC2bzDBO|UxKGSnbHX0bY9vKG23dHHueEBie3Onc4Pl[EBieyCnYYLsfUBieG:ydH;0bYMh[2WubIOgZZQhOyC3TTDh[pRmeiB{NDDodpMh[nliQX7u[ZhqdiCYLV\JWGMweHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{Bj[XOnZDDmcI94KGO7dH;t[ZRzgSBqUo\iJF0hOS5|NDD0c{AyNjZ5JTm= M1rhflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OEWzN|QxLz5{OUi1N|M1ODxxYU6=
NCI-H1975 MnrySpVv[3Srb36gZZN{[Xl? MmC3TY5pcWKrdHnvckBw\iCHR1\SJGw5PTiUL2S3PVBOKGSxdXLs[UBufXSjboSgdIhwe3Cqb4L5cIF1cW:wIHnuJGVITi2|dHnteYxifGWmIHj1cYFvKE6FST3INVk4PSClZXzsd{BifCBzIITvJFExOCCwTTDifUBY\XO2ZYLuJIJtd3RibXX0bI9l NXj2PJdRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5NFYyOTRpPkK5PVA3OTF2PD;hQi=>
A431 MX;GeY5kfGmxbjDhd5NigQ>? MlPvV4Vt\WO2aY\peJkhemG2aX:sJJJifGmxIFnDOVAh\m:{IHj1cYFvKEF2M{GgZ4VtdHNib4\ldoV5eHKnc4Ppcochf2muZD30fZBmKEWJRmKgeI8hUUN3MDDmc5IhcHWvYX6gUmNKNUhzOUe1JINmdGy|IHX4dJJme3OrbnegSWdHWiCWN{mwUU9NQDV6UjDteZRidnR? NEfaR2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVY{QSd-MkexN|E3Ozl:L3G+
PC9 Mln2RY51cXS3bX;yJIFkfGm4aYT5JIF{e2G7 NEfzUWVCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|kh[2WubIOgbIFz[m:{aX7nJGVITlJiZYjvckAyQSCmZXzleIlwdiCjY4TpeoF1cW6pIH31eIFvfCC6ZX7v[5Ji\nSnZDDpckBUS0mGIH3veZNmKGG|c3Xzd4VlKGG|IIT1cY9zKGe{b4f0bEBqdmirYnn0bY9vKGG2IEGwJI1oN2upL3ThfUwheG9icXSg[o9zKDdiZHH5d{Bz\WyjdHn2[UB1dyClb370do9t MmLDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{N{G5OlMoRjJ3MkexPVY{RC:jPh?=
A431 MoTkRY51cXS3bX;yJIFkfGm4aYT5JIF{e2G7 M2[5c2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0N|Eh[2WubIOgfIVvd2e{YX\0[YQhcW5iU1PJSEBud3W|ZTDhd5Nme3OnZDDhd{B1fW2xcjDndo94fGhiaX7obYJqfGmxbjDheEA2KG2pL3vnM4RigSxicH:gdYQh\m:{IEeg[IF6eyC{ZXzheIl3\SC2bzDjc451em:u NVKxW49XRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyO|E6PjNpPkK1NlcyQTZ|PD;hQi=>
Assay
Methods Test Index PMID
Western blot p-EGFR / p-AKT / p-ERK ; ABCB1 28416483 27649127
Growth inhibition assay Cell viability 31043587
Immunofluorescence Ki67 / γH2AX / p16 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 (from reference)

Animal Research:

[2]

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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 499.61
Formula

C28 H33 N7 O2

CAS No. 1421373-65-0
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04591002 Suspended Drug: Osimertinib 80 MG Lung Cancer Samsung Medical Center November 18 2022 Phase 2
NCT05401110 Not yet recruiting Drug: Osimertinib|Drug: Carotuximab Non Small Cell Lung Cancer|Lung Cancer Karen Reckamp MD MS|Enviro Therapeutics Inc.|Cedars-Sinai Medical Center August 2022 Phase 1
NCT05166616 Recruiting Procedure: Biopsy|Drug: Osimertinib|Drug: Triptolide Analog Advanced Lung Non-Small Cell Carcinoma|Locally Advanced Lung Non-Small Cell Carcinoma|Stage III Lung Cancer AJCC v8|Stage IIIA Lung Cancer AJCC v8|Stage IIIB Lung Cancer AJCC v8|Stage IIIC Lung Cancer AJCC v8|Stage IV Lung Cancer AJCC v8|Stage IVA Lung Cancer AJCC v8|Stage IVB Lung Cancer AJCC v8|Unresectable Lung Non-Small Cell Carcinoma City of Hope Medical Center|National Cancer Institute (NCI) July 1 2022 Phase 1
NCT05120349 Recruiting Drug: Osimertinib|Drug: Placebo Non-Small Cell Lung Cancer AstraZeneca February 21 2022 Phase 3
NCT05298176 Recruiting Drug: Afatinib Osimertinib Carboplatin and Pemetrexed Non-Small Cell Lung Cancer Amsterdam UMC location VUmc January 4 2022 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

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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: 5%DMSO+40%PEG300+5%Tween 80+50%ddH2O.

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