Home Protein Tyrosine Kinase EGFR inhibitor Osimertinib (AZD9291) 仅限科研使用

Osimertinib (AZD9291)

别名: Mereletinib 中文名称：

Osimertinib (AZD9291, Mereletinib)是口服不可逆的，突变选择性EGFR抑制剂，在 LoVo细胞中对Exon 19 缺失的 EGFR，L858R/T790M EGFR，和 WT EGFR的IC50分别为12.92，11.44 和 493.8 nM。Phase 3。

Osimertinib (AZD9291) Chemical Structure

Osimertinib (AZD9291) Chemical Structure

CAS: 1421373-65-0

规格 价格 库存 购买数量
10mM (1mL in DMSO) 647.05 现货
5mg 573.71 现货
100mg 2375.99 现货
1g 7944.3 现货
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常与Osimertinib (AZD9291)一起在实验中被使用的化合物

Afatinib

两者都是 EGFR 抑制剂。 他们的联合疗法比单独疗法对几种 EGFR 外显子 20 插入突变产生更有效的抑制作用。

Hasegawa H, et al. Lung Cancer. 2019 Jan;127:146-152.

Gefitinib

两者都是 EGFR 抑制剂。 他们的联合疗法用于治疗携带 T790M 和 C797S 突变的非小细胞肺癌患者。

Arulananda S, et al. J Thorac Oncol. 2017 Nov;12(11):1728-1732.

Erlotinib

两者都是 EGFR 抑制剂。 奥希替尼（Osmiertinib）与厄洛替尼（erlotinib）联合用于治疗对第一代和第二代 TKI 耐药的非小细胞肺癌患者。

Trametinib (GSK1120212)

奥希替尼和曲美替尼与达拉非尼一起可以克服 BRAF V600E 诱导的携带 BRAF V600E、EGFR 19del 和 T790M 突变的患者对奥希替尼耐药。

Huang Y, et al. Journal of Thoracic Oncology 14.10 (2019): e236-e237.

Lazertinib

Lazertinib 与 Amivantamab 联合用于治疗奥希替尼复发、未接受化疗的 EGFR 突变体 (EGFRm) 非小细胞肺癌。 它也被用作反应的潜在生物标志物。

Bauml J, et al. Journal of Clinical Oncology 39, no. 15_suppl (May 20, 2021) 9006-9006.

Osimertinib (AZD9291)相关产品

相关信号通路图

EGFR Signaling Pathways

EGFR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
VP-2 Growth Inhibition Assay 50 nM 10 d inhibits proliferation in long-term (10-day) growth inhibition assays 25477325
PC-9/ERc1 Growth Inhibition Assay 50 nM 10 d inhibits proliferation in long-term (10-day) growth inhibition assays 25477325
PC-9/BRc1 Growth Inhibition Assay 50 nM 10 d inhibits proliferation in long-term (10-day) growth inhibition assays 25477325
VP-2 Function Assay 50 nM 24 h induces expression of the proapoptotic BCL-2 family member BIM 25477325
PC-9/ERc1 Function Assay 50 nM 24 h induces expression of the proapoptotic BCL-2 family member BIM 25477325
PC-9/BRc1 Function Assay 50 nM 24 h induces expression of the proapoptotic BCL-2 family member BIM 25477325
PC9 GR4 Function Assay 0-10 μM 72 h inhibits EGFR phosphorylation and downstream signaling  25948633
PC9 Function Assay 0-10 μM 72 h inhibits WT EGFR at low concentrations 25948633
PC9 GR4 Growth Inhibition Assay 0-10 μM 72 h inhibits cell growth dose dependently 25948633
BAF3 Function assay 72 h GI50 = 0.0003 μM 28282122
BAF3 Function assay 72 h GI50 = 0.0003 μM 28282122
BAF3 Function assay 72 h GI50 = 0.001 μM 28282122
HCC827 Function assay 72 h GI50 = 0.001 μM 28282122
PC9 Function assay 72 h GI50 = 0.002 μM 28282122
BAF3 Function assay 4 h EC50 = 0.002 μM 28282122
HCC827 Function assay 3 h IC50 = 0.0025 μM 27433829
H1975 Function assay 3 h IC50 = 0.0025 μM 27433829
H3255 Function assay 3 h IC50 = 0.0041 μM 27433829
NCI-H1975 Function assay 72 h GI50 = 0.005 μM 28282122
PC9 Antiproliferative activity assay 72 h IC50 = 0.0065 μM 28716641
NCI-H1975 Antiproliferative activity assay 72 h IC50 = 0.0105 μM 28716641
PC9-DRH Function assay 2 h IC50 = 0.013 μM 26756222
BAF3 Function assay 72 h GI50 = 0.013 μM 28282122
HCC827 Function assay 96 h EC50 = 0.014 μM 28225269
HCC827 Antiproliferative activity assay 96 h EC50 = 0.014 μM 28853575
NCI-H1975 Antiproliferative activity assay 96 h EC50 = 0.014 μM 28853575
NCI-H1975 Function assay 2 h IC50 = 0.015 μM 26756222
H1975 Function assay 2 h IC50 = 0.015 μM 26968253
PC9 Function assay 2 h IC50 = 0.017 μM 26968253
NCI-H1975 Antiproliferative activity assay 72 h IC50 = 0.019 μM 29466773
NCI-H1975 Function assay 96 h EC50 = 0.019 μM 28225269
NCI-H1975 Antiproliferative activity assay 96 h EC50 = 0.019 μM 28603991
NCI-H1975 Antiproliferative activity assay 72 h IC50 = 0.019 μM 29853340
HCC827 Function assay 2 h IC50 = 0.023 μM 26756222
NCI-H1975 Antiproliferative activity assay 72 h IC50 = 0.023 μM 29534926
PC9 Cytotoxicity assay 72 h GI50 = 0.023 μM 25271963
NCI-H1975 Cytotoxicity assay 72 h GI50 = 0.024 μM 25271963
HCC827 Antiproliferative activity assay 72 h IC50 = 0.0254 μM 29576272
HCC827 Antiproliferative activity assay 72 h IC50 = 0.027 μM 29466773
HCC827 Antiproliferative activity assay 72 h IC50 = 0.027 μM 29853340
NCI-H1975 Antiproliferative activity assay 72 h IC50 = 0.03 μM 28033579
H3255 Function assay 72 h GI50 = 0.033 μM 28282122
H3255 Function assay 2 h IC50 = 0.036 μM 26756222
NCI-H1975 Antiproliferative activity assay 72 h IC50 = 0.041 μM 29730192
NCI-H1975 Function assay 1 h IC50 = 0.041 μM 29534926
BAF3 Function assay 4 h EC50 = 0.043 μM 28282122
NCI-H1975 Antiproliferative activity assay 72 h IC50 = 0.0472 μM 29576272
NCI-H1975 Antiproliferative activity assay 72 h IC50 = 0.052 μM 27131639
PC9 Function assay 2 h IC50 = 0.056 μM 26756222
NCI-H1975 Cytotoxicity assay 72 h IC50 = 0.06 μM 29486953
HaCaT Function assay 3 h IC50 = 0.0737 μM 27433829
NCI-H1975 Antiproliferative activity assay 72 h IC50 = 0.13 μM 30429956
A431 Function assay 1 h IC50 = 0.141 μM 29534926
Calu3 Cytotoxicity assay 72 h GI50 = 0.264 μM 25271963
Sf9 Function assay 20 mins IC50 = 0.278 μM 28482151
BAF3 Function assay 72 h GI50 = 0.3 μM 28282122
BAF3 Function assay 72 h GI50 = 0.31 μM 28282122
NCI-H460 Antiproliferative activity assay 72 h IC50 = 0.4159 μM 28716641
LoVo Function assay 2 h IC50 = 0.48 μM 26968253
LoVo Function assay 2 h IC50 = 0.48 μM 27996267
A549 Antiproliferative activity assay 72 h IC50 = 0.486 μM 29576272
BAF3 Function assay 72 h GI50 = 0.5 μM 28282122
A549 Antiproliferative activity assay 72 h IC50 = 0.53 μM 29466773
A549 Cytotoxicity assay 72 h IC50 = 0.53 μM 29853340
BAF3 Function assay 72 h GI50 = 0.55 μM 28282122
BAF3 Function assay 72 h GI50 = 0.56 μM 28282122
BAF3 Function assay 72 h GI50 = 0.59 μM 28282122
HT-29 Cytotoxicity assay 72 h IC50 = 0.65 μM 29486953
A431 Function assay 96 h EC50 = 0.667 μM 28225269
A431 Antiproliferative activity assay 96 h EC50 = 0.67 μM 28853575
A431 Antiproliferative activity assay 72 h IC50 = 0.685 μM 29534926
A431 Antiproliferative activity assay 96 h EC50 = 0.7 μM 28603991
A549 Cytotoxicity assay 72 h IC50 = 0.87 μM 29486953
A431 Antiproliferative activity assay 72 h IC50 = 0.893 μM 27131639
BA/F3 Antiproliferative activity assay 72 h IC50 = 1 μM 26258521
BAF3 Growth inhibition assay 72 h GI50 = 1.2 μM 28282122
NCI-H2122 Function assay 72 h GI50 = 1.2 μM 28282122
A431 Antiproliferative activity assay 72 h IC50 = 1.24 μM 30429956
A431 Antiproliferative activity assay 72 h IC50 = 1.26 μM 29730192
A431 Antiproliferative activity assay 72 h IC50 = 1.604 μM 28033579
A549 Antiproliferative activity assay 96 h EC50 = 1.83 μM 28853575
CHL Growth inhibition assay 72 h GI50 = 2.9 μM 28282122
H1355 Function assay 72 h GI50 = 3 μM 28282122
H1703 Function assay 72 h GI50 = 3.5 μM 28282122
A549 Function assay 72 h GI50 = 3.5 μM 28282122
CHO Growth inhibition assay 72 h GI50 = 4.2 μM 28282122
BAF3 Antiproliferative activity assay 72 h IC50 = 4.61 μM 30429956
BAF3 Antiproliferative activity assay 72 h IC50 = 5.15 μM 30429956
BEAS2B Antiproliferative activity assay 72 h IC50 = 14.9 μM 28716641
NCI-H1975 Function assay 2 h IC50 = 15 μM 25271963
PC9 Function assay 2 h IC50 = 17 μM 25271963
LoVo Function assay 2 h IC50 = 480 μM 25271963
HCC827 Antiproliferative activity assay 72 h Antiproliferative activity against human HCC827 cells at 1 uM after 72 hrs by MTT assay relative to control 29576272
BAF3 Function assay 2 h 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 2 h 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
Caco2 Function assay 2 h Efflux ratio of apparent permeability from basolateral side to apical side over apical side to basolateral side over in human Caco2 cells at 5 uM incubated for 2 hrs 28853575
Caco2 Function assay 2 h Apparent permeability across apical to basolateral side in human Caco2 cells at 5 uM incubated for 2 hrs 28853575
Caco2 Function assay 2 h Apparent permeability across basolateral to apical side in human Caco2 cells at 5 uM incubated for 2 hrs 28853575
NCI-H1975 Function assay 4 h 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
HCC827 Function assay 4 h 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
NCI-H1975 Apoptosis assay 48 h 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
HCC827 Apoptosis assay 48 h 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
PC9 Apoptosis assay 48 h 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
H3255 Apoptosis assay 48 h 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 Apoptosis assay 48 h 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 Apoptosis assay 48 h 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 Apoptosis assay 48 h 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 Apoptosis assay 48 h Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting 28282122
Sf21 Function assay IC50 = 0.012 μM 27996267
HCC827 Antiproliferative activity assay IC50 = 0.0616 μM 28426996
NCI-H1975 Antiproliferative activity assay IC50 = 0.067 μM 28426996
A549 Function assay IC50 = 0.15 μM 26756222
HEK293 Function assay IC50 = 0.57 μM 28426996
A431 Antiproliferative activity assay IC50 = 0.6156 μM 28426996
NCI-H1975 Antitumor activity assay Antitumor activity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant xenografted in SCID mouse assessed as tumor growth inhibition at 2.5 mg/kg/day, po qd for 7 days relative to control 25271963
rat hepatocytes Function assay Intrinsic clearance in rat hepatocytes measured per 10'6 cells 25271963
human hepatocytes Function assay Intrinsic clearance in human hepatocytes measured per 10'6 cells 25271963
NCI-H1975 Antitumor activity assay Antitumor activity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant xenografted in SCID mouse assessed as tumor growth inhibition at 5 mg/kg/day, po qd for 7 days relative to control 25271963
NCI-H1975 Function assay Selectivity index, ratio of IC50 for EGFR T790M/L858R double mutant expressing human NCI-H1975 cells to IC50 for wild type EGFR expressing human A431 cells 29730192
NCI-H1975 Antitumor activity assay 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
HCC827 Apoptosis assay Induction of apoptosis in human HCC827 cells harboring EGFR E746-A750 deletion mutant assessed as early apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.34%) 29466773
HCC827 Apoptosis assay Induction of apoptosis in human HCC827 cells harboring EGFR E746-A750 deletion mutant assessed as late apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 27.14%) 29466773
A549 Function assay Selectivity ratio of IC50 for human A549 cells expressing wild-type EGFR/K-Ras mutant to IC50 for human NCI-H1975 cells expressing EGFR L858R/T790M double mutant 29486953
NCI-H1975 Antitumor activity assay Antitumor activity against human NCI-H1975 cells xenografted in STOCK-Foxn1nu/Nju nude mouse assessed as inhibition of tumor growth at 20 mg/kg/day, po qd for 14 days relative to untreated control 28395219
A431 Function assay Selectivity ratio of EC50 for human A431 cells expressing wild type EGFR to EC50 for human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant 28853575
NCI-H1975 Function assay Selectivity ratio of IC50 for human NCI-H1975 cells harboring EGFR L858R/T790M double mutant to IC50 for human A431 cells harboring wild-type EGFR 28426996
human hepatocytes Function assay Intrinsic clearance in human hepatocytes assessed per million cells 28426996
rat hepatocytes Function assay Intrinsic clearance in rat hepatocytes assessed per million cells 28426996
A549, NCI-H1975 Function assay Selectivity ratio of IC50 for EGF-stimulated wild type EGFR in human A549 cells to IC50 for EGFR L858R/T790M double mutant in human NCI-H1975 cells 26756222
A549, PC9 Function assay Selectivity ratio of IC50 for EGF-stimulated wild type EGFR in human A549 cells to IC50 for EGFR deletion mutant in human PC9 cells 26756222
HCC827 Apoptosis assay Induction of apoptosis in human HCC827 cells harboring EGFR E746 to A750 deletion mutant assessed as early apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.34 to 1.67%) 29853340
NCI-H1975 Function assay 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
A431 Function assay Selectivity ratio, ratio IC50 for human A431 cells overexpressing wild-type EGFR to IC50 for human NCI-H1975 cells expressing EGFR T790M/L858R mutant 27131639
PC9 Antitumor activity assay Antitumor activity against human PC9 cells harboring EGFR exon 19 deletion activating mutant xenografted in SCID mouse assessed as tumor growth inhibition at 10 mg/kg/day, po qd for 7 days relative to control 25271963
A431 Antitumor activity assay Antitumor activity against human A431 cells xenografted in SCID mouse assessed as tumor growth inhibition at 5 mg/kg/day, po qd for 7 days relative to control 25271963
点击查看更多细胞系数据

生物活性

产品描述 Osimertinib (AZD9291, Mereletinib)是口服不可逆的，突变选择性EGFR抑制剂，在 LoVo细胞中对Exon 19 缺失的 EGFR，L858R/T790M EGFR，和 WT EGFR的IC50分别为12.92，11.44 和 493.8 nM。Phase 3。
靶点
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
体外研究(In Vitro)
体外研究活性

与体外野生型相比，在突变EGFR 细胞系中AZD9291能更有效的抑制增殖。[2]
实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-EGFR / p-AKT / p-ERK ABCB1 28416483
Growth inhibition assay Cell viability 31043587
Immunofluorescence Ki67 / γH2AX / p16 29212784
体内研究(In Vivo)
体内研究活性

AZD9291（5mg / kg p.o.）引起整个EGFRm+（PC9）和EGFRm+/ T790M（H1975）肿瘤模型肿瘤中显著的肿瘤消退，伴随着对体内EGFR磷酸化和下游关键信号通路，如AKT和ERK的显著抑制。[2]
动物实验 Animal Models PC9和H1975移植瘤小鼠
Dosages ~5 毫克/千克
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06350097 Not yet recruiting
Non-small Cell Lung Cancer
AstraZeneca|Daiichi Sankyo
 May 16 2024 Phase 3
NCT06323148 Not yet recruiting
Lung Cancer|EGFR Gene Mutation|Minimal Residual Disease
Fudan University
 April 1 2024 Phase 3
NCT05748093 Recruiting
Non-small Cell Lung Cancer
Maastricht University Medical Center
 April 1 2024 Phase 4
NCT06206850 Not yet recruiting
Non-squamous NSCLC
Jair Bar M.D. Ph.D.|Sheba Medical Center
 January 2024 Phase 2
NCT06053099 Recruiting
Non Small Cell Lung Cancer|EGFR Activating Mutation|EGFR DEL19|EGFR L858R
Intergroupe Francophone de Cancerologie Thoracique
 January 22 2024 Not Applicable
NCT05954871 Recruiting
Colorectal Cancer|Non-Small Cell Lung Cancer
Genentech Inc.
 January 8 2024 Phase 1

化学信息&溶解度

分子量 499.61 分子式

C28 H33 N7 O2
CAS号 1421373-65-0 SDF Download Osimertinib (AZD9291) 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
储存条件(自收到货起)

体外溶解度
批次：

DMSO : 99 mg/mL ( (198.15 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 99 mg/mL (198.15 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次：

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

摩尔浓度计算器

质量 浓度 体积 分子量

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。

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常见问题及建议解决方法

问题 1:
Can this formulation be used in mice? What are reconstitution instructions for in vivo with mice?

回答：
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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