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 289 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 NF\4e4ZHfW6ldHnvckBCe3OjeR?= M4f0SFUxKG6P NVi2PWlHOjRiaB?= MWXEUXNQ NX6wc3EzcW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0> MoTiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2N{ezNlUoRjJ3NEe3N|I2RC:jPh?=
PC-9/ERc1 MVHGeY5kfGmxbjDBd5NigQ>? MoHlOVAhdk1? M3SzbVI1KGh? NYPHeZZwTE2VTx?= NGrJNotqdmS3Y3XzJIV5eHKnc4Ppc44hd2ZidHjlJJBzd2Gyb4D0c5Rq[yCEQ1ytNkBn[W2rbImgcYVu[mW{IFLJUS=> NYO2SZlzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0O|c{OjVpPkK1OFc4OzJ3PD;hQi=>
VP-2 MUfGeY5kfGmxbjDBd5NigQ>? NHOwbFg2OCCwTR?= NXT1[2RXOjRiaB?= MkW2SG1UVw>? NEfDOolqdmS3Y3XzJIV5eHKnc4Ppc44hd2ZidHjlJJBzd2Gyb4D0c5Rq[yCEQ1ytNkBn[W2rbImgcYVu[mW{IFLJUS=> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR5N{OyOUc,OjV2N{ezNlU9N2F-
PC-9/BRc1 Moq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV21NEBvVQ>? NFK2ZXYyOCCm NX;UVmRiTE2VTx?= M37yNIlvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gcI9v\y22ZYLtJEgyOC2mYYmpJIdzd3e2aDDpcohq[mm2aX;uJIF{e2G7cx?= NWD0VYJCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0O|c{OjVpPkK1OFc4OzJ3PD;hQi=>
PC-9/ERc1 NHq4cGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITvWmc2OCCwTR?= NWW4cGRoOTBiZB?= NV;QO5Z4TE2VTx?= NHfYdJZqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= MkLhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2N{ezNlUoRjJ3NEe3N|I2RC:jPh?=
VP-2 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTQOVAhdk1? M2n3Z|ExKGR? M{j0e2ROW09? NEHVVWlqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= MnrBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2N{ezNlUoRjJ3NEe3N|I2RC:jPh?=
PC9 GR4 NIL5OpVHfW6ldHnvckBCe3OjeR?= MonXNE0yOCEQvF2= NYHhenNsPzJiaB?= MV3pcohq[mm2c9MgSWdHWiCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gd4lodmGuaX7nxsA> NGe3[4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm0PFY{Oyd-MkW5OFg3OzN:L3G+
PC9 MYjGeY5kfGmxbjDBd5NigQ>? NInER|kxNTFyIN88US=> NXi2Ro9CPzJiaB?= MVjpcohq[mm2czDXWEBGT0[UIHH0JIxwfyClb37j[Y51emG2aX;udy=> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl2OE[zN{c,OjV7NEi2N|M9N2F-
PC9 GR4 M1PUeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYCwMVExKM7:TR?= NVrwSZVWPzJiaB?= M2q0SIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MlPaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NEi2N|MoRjJ3OUS4OlM{RC:jPh?=
BAF3 MkfVSpVv[3Srb36gZZN{[Xl? NV;BO4lXPzJiaB?= M1uwO2dKPTBiPTCwMlAxODNizszN MmrxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
BAF3 NWixT2hmTnWwY4Tpc44h[XO|YYm= NIHFdFQ4OiCq NWTCdlNJT0l3MDC9JFAvODByMzFOwG0> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
BAF3 NYSx[XR4TnWwY4Tpc44h[XO|YYm= MV:3NkBp NELyNpdIUTVyIE2gNE4xODFizszN MmPBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
HCC827 NYDETXozTnWwY4Tpc44h[XO|YYm= MW[3NkBp NUHEflIyT0l3MDC9JFAvODBzIN88US=> Ml\TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
PC9 M1;HVGZ2dmO2aX;uJIF{e2G7 NGTPR5E4OiCq MnLZS2k2OCB;IECuNFAzKM7:TR?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
BAF3 M2\wU2Z2dmO2aX;uJIF{e2G7 NYK2bFY2PCCq MUHFR|UxKD1iMD6wNFIh|ryP NWHLb2xFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
HCC827 NYrYSZlWTnWwY4Tpc44h[XO|YYm= MlfWN{Bp NHTKZ4NKSzVyIE2gNE4xODJ3IN88US=> MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzR|M{iyPUc,Ojd2M{O4Nlk9N2F-
H1975 MmHXSpVv[3Srb36gZZN{[Xl? NEjKeYQ{KGh? MlLwTWM2OCB;IECuNFAzPSEQvF2= NGSxZ|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{SzN|gzQSd-Mke0N|M5Ojl:L3G+
H3255 MlezSpVv[3Srb36gZZN{[Xl? MYKzJIg> MUTJR|UxKD1iMD6wNFQyKM7:TR?= MlTNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd2M{O4NlkoRjJ5NEOzPFI6RC:jPh?=
NCI-H1975 M33x[WZ2dmO2aX;uJIF{e2G7 MlrXO|IhcA>? NFvxcVhIUTVyIE2gNE4xODVizszN NGTnd3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
PC9 M2TDWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NXPFNIN3PzJiaB?= NF\kfVBKSzVyIE2gNE4xODZ3IN88US=> NIHNfJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEexOlY1OSd-Mki3NVY3PDF:L3G+
NCI-H1975 NF;QelFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NETEfIE4OiCq NWi3ZldZUUN3MDC9JFAvODFyNTFOwG0> Mn3QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5MU[2OFEoRjJ6N{G2OlQyRC:jPh?=
Sf21 NH\EZ3BHfW6ldHnvckBie3OjeR?= MVzJR|UxKD1iMD6wNVIh|ryP NHHm[IY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OlI3Pyd-Mke5PVYzPjd:L3G+
PC9-DRH NVP3N2cyTnWwY4Tpc44h[XO|YYm= M2jselIhcA>? Mn72TWM2OCB;IECuNFE{KM7:TR?= NU\zSVVTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3OVYzOjJpPkK2O|U3OjJ{PD;hQi=>
BAF3 NXfZXJNKTnWwY4Tpc44h[XO|YYm= NH\Hd244OiCq MofnS2k2OCB;IECuNFE{KM7:TR?= Mk[2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
HCC827 NWL1OFZQTnWwY4Tpc44h[XO|YYm= NFPMR206PiCq NGTTeppGSzVyIE2gNE4xOTRizszN M13a[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkK1NlY6Lz5{OEKyOVI3QTxxYU6=
HCC827 NI\MUHlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NIDrV3A6PiCq NYfnfGZwTUN3MDC9JFAvODF2IN88US=> NGnTOWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEi1N|U4PSd-Mki4OVM2PzV:L3G+
NCI-H1975 MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NVL4dJBHQTZiaB?= MUXFR|UxKD1iMD6wNVQh|ryP M2DqWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEWzOVc2Lz5{OEi1N|U4PTxxYU6=
NCI-H1975 M4XINWZ2dmO2aX;uJIF{e2G7 M4nwOFIhcA>? NHnPc4FKSzVyIE2gNE4xOTVizszN NGn1RXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke1OlIzOid-Mk[3OVYzOjJ:L3G+
H1975 M2XwSmZ2dmO2aX;uJIF{e2G7 MUGyJIg> NUfzZpFWUUN3MDC9JFAvODF3IN88US=> NUOxVFdERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5OlgzPTNpPkK2PVY5OjV|PD;hQi=>
PC9 NGDDUYZHfW6ldHnvckBie3OjeR?= MXqyJIg> MmHqTWM2OCB;IECuNFE4KM7:TR?= M1TnR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OU[4NlU{Lz5{Nkm2PFI2OzxxYU6=
NCI-H1975 M37VfmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NG\nd|Y4OiCq NV34c4FSUUN3MDC9JFAvODF7IN88US=> MmewQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2Nk[3O|MoRjJ7NE[2O|c{RC:jPh?=
NCI-H1975 NGjXcnVHfW6ldHnvckBie3OjeR?= M4WzV|k3KGh? MmmxSWM2OCB;IECuNFE6KM7:TR?= NF;uWW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEKyOVI3QSd-MkiyNlUzPjl:L3G+
NCI-H1975 NUP3R5NRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MkjnPVYhcA>? NVXYUGw4TUN3MDC9JFAvODF7IN88US=> Ml\qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4MEO5PVEoRjJ6NkCzPVkyRC:jPh?=
NCI-H1975 NFTzcHhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MnvmO|IhcA>? NVjhb5hPUUN3MDC9JFAvODF7IN88US=> NWfS[456RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OVM{PDBpPkK5PFU{OzRyPD;hQi=>
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NCI-H1975 NHjOfIJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NXe2NXJMPzJiaB?= Mn\ZTWM2OCB;IECuNFI{KM7:TR?= NFv5b5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWzOFkzPid-Mkm1N|Q6OjZ:L3G+
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NCI-H1975 NVrwWph6S3m2b4TvfIlkcXS7IHHzd4F6 M2XEeFczKGh? MVzHTVUxKD1iMD6wNlQh|ryP M4\DcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkexPVY{Lz5{NUK3NVk3OzxxYU6=
HCC827 NV3MS2ZXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NVLoeZpLPzJiaB?= MX;JR|UxKD1iMD6wNlU1KM7:TR?= MknSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3N{[yO|IoRjJ7NUe2NlczRC:jPh?=
HCC827 NX7ZcYtKSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MUC3NkBp M3fxTmlEPTBiPTCwMlAzPyEQvF2= NV;XNGg1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OlY4PzNpPkK5OFY3Pzd|PD;hQi=>
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NCI-H1975 MVnGeY5kfGmxbjDhd5NigQ>? NHfxU44yKGh? NUnVbIJyUUN3MDC9JFAvODRzIN88US=> MkH6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3M{S5NlYoRjJ7NUO0PVI3RC:jPh?=
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NCI-H1975 NH:1Zm9HfW6ldHnvckBie3OjeR?= MoHHV4Vt\WO2aY\peJkhemG2aX:gc4YhUUN3MDDmc5IhcHWvYX6gUmNKNUhzOUe1JINmdGy|IHjhdoJwemmwZzDFS2ZTKEx6NUjSM3Q4QTCPIHTveYJt\SCvdYThcpQhfG9iSVO1NEBnd3JiaIXtZY4hSTR|MTDj[YxteyCqYYLic5Jqdmdid3ns[E11gXCnIFXHSnI> NVPHb4tiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0NlY6QTZpPkK4OFI3QTl4PD;hQi=>
human hepatocytes NHHHZ4FHfW6ldHnvckBie3OjeR?= M2Dsc2lvfHKrboPpZ{BkdGWjcnHuZ4UhcW5iaIXtZY4hcGWyYYTvZ5l1\XNiYYPz[ZN{\WRicHXyJI1qdGyrb36gZ4VtdHN? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR{Nkm5Okc,Ojh2Mk[5PVY9N2F-
rat hepatocytes NWXoRVhvTnWwY4Tpc44h[XO|YYm= NYfrb2FGUW62cnnud4lkKGOuZXHyZY5k\SCrbjDyZZQhcGWyYYTvZ5l1\XNiYYPz[ZN{\WRicHXyJI1qdGyrb36gZ4VtdHN? NEjJWoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESyOlk6Pid-Mki0NlY6QTZ:L3G+
A549, NCI-H1975 M2fNdmZ2dmO2aX;uJIF{e2G7 M{PLOHNmdGWldHn2bZR6KHKjdHnvJI9nKEmFNUCg[o9zKEWJRj3zeIlufWyjdHXkJJdqdGRidInw[UBGT0[UIHnuJIh2dWGwIFG1OFkh[2WubIOgeI8hUUN3MDDmc5IhTUeIUjDMPFU5Wi:WN{mwUUBld3WkbHWgcZV1[W62IHnuJIh2dWGwIF7DTU1JOTl5NTDj[Yxtew>? M1HpOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{W2NlIzLz5{Nke1OlIzOjxxYU6=
A549, PC9 M376VmZ2dmO2aX;uJIF{e2G7 MmXmV4Vt\WO2aY\peJkhemG2aX:gc4YhUUN3MDDmc5IhTUeILYP0bY12dGG2ZXSge4lt\CC2eYDlJGVITlJiaX6gbJVu[W5iQUW0PUBk\WyuczD0c{BKSzVyIH\vdkBGT0[UIHTlcIV1cW:wIH31eIFvfCCrbjDoeY1idiCSQ{mgZ4VtdHN? NHTIS5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke1OlIzOid-Mk[3OVYzOjJ:L3G+
HCC827 NULuV|YzSXCxcITvd4l{KGG|c3H5 NUHQ[pdbUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIR2M5OjdiY3XscJMhcGG{Yn;ybY5oKEWJRmKgSVc1PiC2bzDBO|UxKGSnbHX0bY9vKG23dHHueEBie3Onc4Pl[EBieyCnYYLsfUBieG:ydH;0bYMh[2WubIOgZZQhOyC3TTDh[pRmeiB{NDDodpMh[nliQX7u[ZhqdiCYLV\JWGMweHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{Bj[XOnZDDmcI94KGO7dH;t[ZRzgSBqUo\iJF0hOS5|NDD0c{AyNjZ5JTm= MmLwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NUOzOFAoRjJ7OEWzN|QxRC:jPh?=
NCI-H1975 NFju[YNHfW6ldHnvckBie3OjeR?= NGrlPGNKdmirYnn0bY9vKG:oIFXHSnIhVDh3OGKvWFc6OE1iZH;1ZoxmKG23dHHueEBxcG:|cHjvdplt[XSrb36gbY4hTUeILYP0bY12dGG2ZXSgbJVu[W5iTlPJMWgyQTd3IHPlcIx{KGG2IEGgeI8hOTByIH7NJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R? M2jnd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUC2NVE1Lz5{OUmwOlEyPDxxYU6=
A431 M2X5ZmZ2dmO2aX;uJIF{e2G7 MonJV4Vt\WO2aY\peJkhemG2aX:sJJJifGmxIFnDOVAh\m:{IHj1cYFvKEF2M{GgZ4VtdHNib4\ldoV5eHKnc4Ppcochf2muZD30fZBmKEWJRmKgeI8hUUN3MDDmc5IhcHWvYX6gUmNKNUhzOUe1JINmdGy|IHX4dJJme3OrbnegSWdHWiCWN{mwUU9NQDV6UjDteZRidnR? NVnrNFc{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexN|E3OzlpPkK3NVMyPjN7PD;hQi=>
PC9 NGLqWJlCdnSrdIXtc5Ih[WO2aY\peJkh[XO|YYm= Mlr2RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFO5JINmdGy|IHjhdoJwemmwZzDFS2ZTKGW6b36gNVkh\GWuZYTpc44h[WO2aY\heIlv\yCvdYThcpQhgGWwb3fyZYZ1\WRiaX6gV2NKTCCvb4Xz[UBie3Onc4Pl[EBieyC2dX3vdkBoem:5dHigbY5pcWKrdHnvckBifCBzMDDt[{9s\y:mYYmsJJBwKHGmIH\vdkA4KGSjeYOgdoVt[XSrdnWgeI8h[2:wdILvcC=> M3\OfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkexPVY{Lz5{NUK3NVk3OzxxYU6=
A431 NFXqR|ZCdnSrdIXtc5Ih[WO2aY\peJkh[XO|YYm= NHjjcpZCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFMyKGOnbHzzJJhmdm:pcnHmeIVlKGmwIGPDTWQhdW:3c3WgZZN{\XO|ZXSgZZMhfHWvb4Kg[5Jwf3SqIHnubIljcXSrb36gZZQhPSCvZz;r[{9l[XluIIDvJJFlKG[xcjC3JIRigXNicnXsZZRqfmVidH:gZ49vfHKxbB?= M4TSUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkexPVY{Lz5{NUK3NVk3OzxxYU6=
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

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

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
NCT02841579 Completed Drug: Osimertinib Non-Small Cell Lung Cancer MedSIR|AstraZeneca August 2016 Phase 2
NCT02771314 Unknown status Drug: AZD9291 Non Small Cell Lung Cancer Hellenic Oncology Research Group August 2 2016 Phase 2
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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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
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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: 1% DMSO+30% PEG 300+dd H2O at up to 30mg/ml.

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