Home Protein Tyrosine Kinase EGFR inhibitor Osimertinib mesylate For research use only.

Osimertinib mesylate

Synonyms: AZD9291 mesylate

Osimertinib mesylate (AZD9291) is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug.

Osimertinib mesylate Chemical Structure

Osimertinib mesylate Chemical Structure

CAS: 1421373-66-1

Selleck's Osimertinib mesylate has been cited by 106 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC9 Cytotoxicity assay 72 hrs Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay, GI50=0.023μM 25271963
NCI-H1975 Cytotoxicity assay 72 hrs Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay, GI50=0.024μM 25271963
Calu3 Cytotoxicity assay 72 hrs Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay, GI50=0.264μM 25271963
NCI-H1975 Function assay 2 hrs Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay, IC50=15μM 25271963
PC9 Function assay 2 hrs Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay, IC50=17μM 25271963
PC9-DRH Function assay 2 hrs Inhibition of EGFR deletion/T790M mutant autophosphorylation in human PC9-DRH cells after 2 hrs by sandwich ELISA, IC50=0.013μM 26756222
NCI-H1975 Function assay 2 hrs Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA, IC50=0.015μM 26756222
HCC827 Function assay 2 hrs Inhibition of EGFR deletion mutant autophosphorylation in human HCC827 cells after 2 hrs by sandwich ELISA, IC50=0.023μM 26756222
H3255 Function assay 2 hrs Inhibition of EGFR L858R mutant autophosphorylation in human H3255 cells after 2 hrs by sandwich ELISA, IC50=0.036μM 26756222
PC9 Function assay 2 hrs Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA, IC50=0.056μM 26756222
A549 Function assay Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA, IC50=0.15μM 26756222
H1975 Function assay 2 hrs Inhibition of EGFR T790M/L858R double mutant phosphorylation in human H1975 cells preincubated for 2 hrs by ELISA, IC50=0.015μM 26968253
PC9 Function assay 2 hrs Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA, IC50=0.017μM 26968253
LoVo Function assay 2 hrs Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA, IC50=0.48μM 26968253
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay, IC50=0.052μM 27131639
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay, IC50=0.893μM 27131639
NCI-H1975 Function assay 1 to 1000 nM 2 hrs Inhibition of EGF-induced EGFR kinase domain L858R/T790M mutant phosphorylation in human NCI-H1975 cells at 1 to 1000 nM pre-incubated for 2 hrs followed by stimulation with EGF for 15 mins by Western blot method 27396610
NCI-H1975 Function assay 1 to 1000 nM 2 hrs Inhibition of EGF-induced EGFR kinase domain L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in ERK phosphorylation at 1 to 1000 nM pre-incubated for 2 hrs followed by stimulation with EGF for 15 mins by Western blot method 27396610
HCC827 Function assay 3 hrs Inhibition of EGFR E746 to A750 deletion mutant phosphorylation in human patient derived HCC827 cells incubated for 3 hrs by ELISA method, IC50=0.0025μM 27433829
H1975 Function assay 3 hrs Inhibition of EGFR L858R/T790M mutant phosphorylation in human patient derived H1975 cells incubated for 3 hrs by ELISA method, IC50=0.0025μM 27433829
H3255 Function assay 3 hrs Inhibition of EGFR L858R mutant phosphorylation in human patient derived H3255 cells incubated for 3 hrs by ELISA method, IC50=0.0041μM 27433829
HaCaT Function assay 3 hrs Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method, IC50=0.0737μM 27433829
Sf21 Function assay Inhibition of N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (696-end residues) expressed in baculovirus infected Sf21 insect cells, IC50=0.012μM 27996267
LoVo Function assay 2 hrs Inhibition of EGF-stimulated wild type EGFR phosphorylation in human LoVo cells incubated for 2 hrs followed by EGF stimulation for 10 mins by ELISA, IC50=0.48μM 27996267
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay, IC50=0.03μM 28033579
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay, IC50=1.604μM 28033579
HCC827 Function assay 96 hrs Inhibition of EGFR delE746_A750 mutant in human HCC827 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay, EC50<0.014μM 28225269
NCI-H1975 Function assay 96 hrs Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay, EC50=0.019μM 28225269
A431 Function assay 96 hrs Inhibition of wild-type EGFR in human A431 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay, EC50=0.667μM 28225269
BAF3 Function assay 72 hrs Inhibition of Tel-fused EGFR L858R mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50<0.0003μM 28282122
BAF3 Function assay 72 hrs Inhibition of full length EGFR T790M/L858R mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50<0.0003μM 28282122
BAF3 Function assay 72 hrs Inhibition of full length EGFR exon 19 deletion mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.001μM 28282122
HCC827 Function assay 72 hrs Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.001μM 28282122
PC9 Function assay 72 hrs Inhibition of EGFR exon 19 deletion mutant in human PC9 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.002μM 28282122
BAF3 Function assay 4 hrs Inhibition of EGFR T790M/L858R mutant (unknown origin) autophosphorylation at Y1068 expressed in mouse BAF3 cells after 4 hrs by Western blot analysis, EC50=0.002μM 28282122
NCI-H1975 Function assay 72 hrs Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.005μM 28282122
BAF3 Function assay 72 hrs Inhibition of Tel-fused EGFR T790M mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.013μM 28282122
H3255 Function assay 72 hrs Inhibition of EGFR L858R mutant in human H3255 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.033μM 28282122
BAF3 Function assay 4 hrs Inhibition of wild-type EGFR (unknown origin) autophosphorylation at Y1068 expressed in mouse BAF3 cells after 4 hrs by Western blot analysis, EC50=0.043μM 28282122
BAF3 Function assay 72 hrs Inhibition of Tel-fused EGFR (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.3μM 28282122
BAF3 Function assay 72 hrs Inhibition of full length EGFR T790M/L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.31μM 28282122
BAF3 Function assay 72 hrs Inhibition of Tel-fused INSR (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.5μM 28282122
BAF3 Function assay 72 hrs Inhibition of Tel-fused EGFR T790M/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.55μM 28282122
BAF3 Function assay 72 hrs Inhibition of Tel-fused IGF1R (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.56μM 28282122
BAF3 Function assay 72 hrs Inhibition of Tel-fused EGFR C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.59μM 28282122
BAF3 Function assay 72 hrs Inhibition of Tel-fused EGFR L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.59μM 28282122
BAF3 Growth inhibition assay 72 hrs Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50=1.2μM 28282122
NCI-H2122 Function assay 72 hrs Inhibition of wild-type EGFR in human NCI-H2122 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=1.2μM 28282122
CHL Growth inhibition assay 72 hrs Growth inhibition of CHL cells after 72 hrs by CellTiter-Glo assay, GI50=2.9μM 28282122
H1355 Function assay 72 hrs Inhibition of wild-type EGFR in human H1355 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=3μM 28282122
A549 Function assay 72 hrs Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=3.5μM 28282122
H1703 Function assay 72 hrs Inhibition of wild-type EGFR in human H1703 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=3.5μM 28282122
CHO Growth inhibition assay 72 hrs Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay, GI50=4.2μM 28282122
NCI-H1975 Function assay 1 uM 4 hrs Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis 28282122
NCI-H1975 Function assay 1 uM 4 hrs Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in P70S6K phosphorylation at Thr389 site at 1 uM measured after 4 hrs by Western blot analysis 28282122
HCC827 Function assay 1 uM 4 hrs Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis 28282122
HCC827 Function assay 1 uM 4 hrs Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in P70S6K phosphorylation at Thr389 site at 1 uM measured after 4 hrs by Western blot analysis 28282122
NCI-H1975 Function assay 1 uM 48 hrs Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as caspase3 cleavage at 1 uM after 48 hrs by immunoblotting 28282122
PC9 Function assay 1 uM 48 hrs Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting 28282122
HCC827 Function assay 1 uM 48 hrs Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting 28282122
H3255 Function assay 1 uM 48 hrs Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting 28282122
NCI-H1975 Function assay 1 uM 48 hrs Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting 28282122
PC9 Function assay 1 uM 48 hrs Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting 28282122
HCC827 Function assay 1 uM 48 hrs Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting 28282122
H3255 Function assay 1 uM 48 hrs Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting 28282122
HCC827 Antiproliferative assay Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant, IC50=0.0616μM 28426996
NCI-H1975 Antiproliferative assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant, IC50=0.067μM 28426996
HEK293 Function assay Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis, IC50=0.57μM 28426996
A431 Antiproliferative assay Antiproliferative activity against human A431 cells harboring wild-type EGFR, IC50=0.6156μM 28426996
Sf9 Function assay 20 mins Inhibition of recombinant human N-terminally GST-tagged EGFR L858R/T790M/C797S triple mutant expressed in baculovirus in Sf9 insect cells preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method, IC50=0.278μM 28482151
BAF3 Function assay 72 hrs Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.006μM 28528303
BAF3 Function assay 72 hrs Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.016μM 28528303
BAF3 Function assay 72 hrs Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.018μM 28528303
BAF3 Function assay 72 hrs Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.02μM 28528303
BAF3 Function assay 72 hrs Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.066μM 28528303
DFCI032 Function assay 72 hrs Inhibition of EGFR in human DFCI032 cells assessed as reduction in cell viability after 72 hrs in presence of ceritinib by MTS assay, EC50=0.19μM 28528303
BAF3 Function assay 72 hrs Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=1.748μM 28528303
DFCI076 Function assay 72 hrs Inhibition of EGFR in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay in presence of ceritinib, EC50=3.21μM 28528303
DFCI032 Function assay 72 hrs Inhibition of EGFR in human DFCI032 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=4.73μM 28528303
DFCI076 Function assay 72 hrs Inhibition of EGFR in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=7.93μM 28528303
DFCI032 Function assay 0.1 to 1 uM Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR phosphorylation at 0.1 to 1 uM by Western blot analysis 28528303
DFCI032 Function assay 0.1 to 1 uM Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR phosphorylation at 0.1 to 1 uM in presence of ceritinib by Western blot analysis 28528303
DFCI032 Function assay 0.1 to 1 uM Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR mediated ERK phosphorylation at 0.1 to 1 uM in presence of ceritinib by Western blot analysis 28528303
NCI-H1975 Antiproliferative assay 96 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay, EC50=0.019μM 28603991
A431 Antiproliferative assay 96 hrs Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay, EC50=0.7μM 28603991
PC9 Antiproliferative assay 72 hrs Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay, IC50=0.0065μM 28716641
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay, IC50=0.0105μM 28716641
NCI-H460 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay, IC50=0.4159μM 28716641
BEAS2B Antiproliferative assay 72 hrs Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay, IC50=14.9μM 28716641
HCC827 Antiproliferative assay 96 hrs Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50<0.014μM 28853575
NCI-H1975 Antiproliferative assay 96 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50<0.014μM 28853575
A431 Antiproliferative assay 96 hrs Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50=0.67μM 28853575
A549 Antiproliferative assay 96 hrs Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50=1.83μM 28853575
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50=0.019μM 29466773
HCC827 Antiproliferative assay 72 hrs Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay, IC50=0.027μM 29466773
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50=0.53μM 29466773
NCI-H1975 Cytotoxicity assay 72 hrs Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50=0.06μM 29486953
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50=0.65μM 29486953
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay, IC50=0.87μM 29486953
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay, IC50=0.023μM 29534926
NCI-H1975 Function assay 1 hr Inhibition of EGFR L858R/T790M mutant phosphorylation in human NCI-H1975 cells after 1 hr by ELISA, IC50=0.041μM 29534926
A431 Function assay 1 hr Inhibition of wild-type EGFR phosphorylation in human A431 cells preincubated for 1 hr followed by EGF stimulation measured after 45 mins by ELISA, IC50=0.141μM 29534926
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay, IC50=0.685μM 29534926
HCC827 Antiproliferative assay 72 hrs Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay, IC50=0.0254μM 29576272
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay, IC50=0.0472μM 29576272
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=0.486μM 29576272
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay, IC50=0.041μM 29730192
A431 Antiproliferative assay 72 hrs Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay, IC50=1.26μM 29730192
NCI-H1975 Antitumor assay 10 mg/kg 21 days Antitumor activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells xenografted in BALB/c athymic nude mouse assessed as tumor growth inhibition at 10 mg/kg, po bid for 21 days 29730192
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50=0.019μM 29853340
HCC827 Antiproliferative assay 72 hrs Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay, IC50=0.027μM 29853340
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=0.53μM 29853340
NCI-H1975 Function assay 1 to 100 nM Inhibition of EGFR L858R/T790M double mutant phosphorylation in EGF-stimulated human NCI-H1975 cells at 1 to 100 nM by Western blot method 29906114
NCI-H1975 Function assay 100 nM Inhibition of EGFR L858R/T790M double mutant in EGF-stimulated human NCI-H1975 cells assessed as reduction in Akt phosphorylation at Ser-473 residue at 100 nM by Western blot method 29906114
NCI-H1975 Function assay 2 hrs Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells preincubated for 2 hrs followed by compound washout measured up to 24 hrs by Western blot method 29906114
NCI-H1975 Function assay 2 hrs Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as reduction in ERK1/2 phosphorylation preincubated for 2 hrs followed by compound washout measured after 12 hrs by Western blot method 29906114
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay, IC50=0.13μM 30429956
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay, IC50=1.24μM 30429956
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay, IC50=4.61μM 30429956
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay, IC50=5.15μM 30429956
BAF3 Function assay 1 to 3 uM 2 hrs Inhibition of EGFR T790M/L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis 30429956
BAF3 Function assay 1 to 3 uM 2 hrs Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis 30429956
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay, GI50=0.0028μM 30442506
HCC827 Antiproliferative assay 72 hrs Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay, IC50=0.011μM 30442506
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay, GI50=0.0401μM 30442506
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay, IC50=0.06μM 30442506
PC9 Antiproliferative assay 72 hrs Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay, IC50=0.16μM 30442506
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay, IC50=0.61μM 30442506
Calu3 Antiproliferative assay 72 hrs Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay, IC50=0.75μM 30442506
Calu6 Antiproliferative assay 72 hrs Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay, IC50=5.86μM 30442506
NCI-H1975 Function assay 4 hrs Inhibition of EGFR T790M/L858R double mutant phosphorylation at Y1068 residue in human NCI-H1975 cells up to 10 uM after 4 hrs by Western blot analysis 30442506
NCI-H1975 Function assay up to 10 uM 4 hrs Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as reduction in ERK phosphorylation at T202/Y204 residues up to 10 uM after 4 hrs by Western blot analysis 30442506
A431 Function assay 4 hrs Inhibition of WT EGFR phosphorylation at Y1068 residue in human A431 cells up to 10 uM after 4 hrs by Western blot analysis 30442506
A431 Function assay up to 10 uM 4 hrs Inhibition of WT EGFR in human A431 cells assessed as reduction in ERK phosphorylation at T202/Y204 residues up to 10 uM after 4 hrs by Western blot analysis 30442506
Sf9 Function assay 60 mins Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay, IC50=0.0208μM 30471829
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay, IC50=0.096μM 30471829
Sf9 Function assay 60 mins Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay, IC50=0.5675μM 30471829
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay, IC50=0.945μM 30471829
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=3.242μM 30471829
Aspc-1 Antiproliferative assay 72 hrs Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay, IC50=3.985μM 30471829
NCI-H1975 Growth inhibition assay 72 hrs Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay, IC50=0.1μM 30472599
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay, IC50=0.073μM 30530173
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=0.615μM 30530173
HepG2 Antiproliferative assay 72 hrs Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50=1.605μM 30530173
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay, IC50=0.03μM 31223440
A431 Antiproliferative assay 72 hrs Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay, IC50=1.44μM 31223440
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay, IC50=3.93μM 31223440
BAF3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay, IC50=5.11μM 31223440
PC9 Antiproliferative assay 72 hrs Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50<0.01μM 31446247
CL68 Antiproliferative assay 72 hrs Antiproliferative activity against human CL68 cells harbouring EGFR delE746-A750/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.01μM 31446247
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.05μM 31446247
CL97 Antiproliferative assay 72 hrs Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.1μM 31446247
A549 Antiproliferative assay 72 hrs Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=5μM 31446247
A431 Cytotoxicity assay 96 hrs Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method, CC50=0.967μM 31560541
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.014μM 31581004
PC9 Antiproliferative assay 72 hrs Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.016μM 31581004
NCI-H292 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=1.084μM 31581004
LO2 Cytotoxicity assay 72 hrs Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=1.602μM 31581004
HEK293A Cytotoxicity assay 72 hrs Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=2.418μM 31581004
HK2 Cytotoxicity assay 72 hrs Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=3.565μM 31581004
HLF Cytotoxicity assay 72 hrs Cytotoxicity against human HLF cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=8.741μM 31581004
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50=0.073μM 31683104
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50=0.462μM 31683104
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50=0.975μM 31683104
HeLa Function assay 0.1 to 5 uM 24 hrs Inhibition of EFGR protein expression in human HeLa cells at 0.1 to 5 uM after 24 hrs by Western blot analysis 31683104
BAF3 Function assay 72 hrs Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.001μM 31689114
BAF3 Function assay 72 hrs Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.081μM 31689114
A431 Antiproliferative assay 96 hrs Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.084μM 31689114
BAF3 Function assay 72 hrs Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.78μM 31689114
BAF3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=1.1μM 31689114
BaF3 Function assay 4 hrs Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay, IC50=3.1μM 31689114
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay, IC50=0.07μM 31718182
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay, IC50=3.1μM 31718182
NCI-H1975 Cytotoxicity assay 4 days Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay, IC50=0.013μM ChEMBL
A549 Cytotoxicity assay 4 days Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay, IC50=0.31μM ChEMBL
Vero Antiviral assay 24 hrs Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr, IC50=3.26μM ChEMBL
Vero Cell viability assay 72hrs Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr, CC50=13.23μM ChEMBL
NCI-H1975 Function assay 16 hrs Inhibition of EGFR T790M/L858R double mutant phosphorylation in human NCI-H1975 cells up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis ChEMBL
NCI-H1975 Function assay 16 hrs Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as AKT phosphorylation up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis ChEMBL
NCI-H1975 Function assay 16 hrs Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as ERK1/2 phosphorylation up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis ChEMBL
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Biological Activity

Description Osimertinib mesylate (AZD9291) is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug.
Targets
EGFR [1]
In vitro
In vitro

Osimertinib-resistant lung adenocarcinoma (LUAD) cells express higher level of METTL7B in comparison to Osimertinib-sensitive cells. Knock-down of METTL7B by GNC-siRNA re-sensitized LUAD cells to osimertinib.[1]
Cell Research Cell lines lung adenocarcinoma (LUAD) cell lines
Concentrations 0.001 -1 µM
Incubation Time 72 h
Method

Cells are plated at a density of 3,000 cells/well in 96 well plates. Osimertinib is added to the medium and treated for 72 h. Cell viability assays are performed by Cell Counting Kit-8.
In Vivo
In vivo

METTL7B is significantly increased in both mRNA and protein level in osimertinib -resistant xenografts as compared with those in osimertinib-sensitive xenografts. In LUAD CDX mouse model, combination treatment with GNC-siMETTL7B (6 mg siRNA per mouse equivalent) significantly suppresses tumor growth as compared with treatment of osimertinib (30 mg/kg) alone.

Chemical lnformation & Solubility

Molecular Weight 595.71 Formula

C29H37N7O5S
CAS No. 1421373-66-1 SDF --
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.CS(=O)(=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 5 mg/mL ( (8.39 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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