Osimertinib mesylate
别名: AZD9291 mesylate 中文名称：甲磺酸奥希替尼
Osimertinib mesylate (AZD9291) 是osimertinib的甲磺酸盐形式，是口服的第三代 epidermal growth factor receptor (EGFR) 酪氨酸激酶(TKI)抑制剂。
Osimertinib mesylate Chemical Structure
CAS: 1421373-66-1
产品质控
批次：
纯度：
99.99%
99.99
Osimertinib mesylate相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 | 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 | 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 |
| 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 |
| 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 | 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | 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 | 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| A549 | Function assay | Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA, IC50=0.15μM | 26756222 | ||
| 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 | ||
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Osimertinib mesylate (AZD9291) 是osimertinib的甲磺酸盐形式，是口服的第三代 epidermal growth factor receptor (EGFR) 酪氨酸激酶(TKI)抑制剂。 | |
|---|---|---|
| 靶点 |
|
化学信息&溶解度
| 分子量 | 595.71 | 分子式 | C29H37N7O5S |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | 3年 -20°C 粉状 | ||
|
体外溶解度 |
DMSO : 5 mg/mL ( (8.39 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
* 必填项
Tags: buy Osimertinib mesylate | Osimertinib mesylate supplier | purchase Osimertinib mesylate | Osimertinib mesylate cost | Osimertinib mesylate manufacturer | order Osimertinib mesylate | Osimertinib mesylate distributor
