Osimertinib (AZD9291) - Moligand™, 10mM in DMSO , Epidermal growth factor receptor erbB1 inhibitor, CAS No.1421373-65-0, Epidermal growth factor receptor erbB1 inhibitor

CAS: 1421373-65-0 Cat. No.: O408946 Peso molecular: 499.62 Número EC: 108-168-8

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Mereletinib | 2-​Propenamide, N-​[2-​[[2-​(dimethylamino)​ethyl]​methylamino]​-​4-​methoxy-​5-​[[4-​(1-​methyl-​1H-​indol-​3-​yl)​-​2-​pyrimidinyl]​amino]​phenyl]​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Osimertinib (AZD9291) is an oral, irreversible, and mutant-selectiveEGFRinhibitor withIC50of 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.
In vitro

AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro.

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.
Cell Data

cell lines：HUVECs

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

Mereletinib | 2-​Propenamide, N-​[2-​[[2-​(dimethylamino)​ethyl]​methylamino]​-​4-​methoxy-​5-​[[4-​(1-​methyl-​1H-​indol-​3-​yl)​-​2-​pyrimidinyl]​amino]​phenyl]​-

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Epidermal growth factor receptor erbB1 inhibitor

Propiedades del producto

• ALogP: 3.7

Nombres e identificadores

• Isómeros 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
• CAS alternativo: 1421373-65-0
• Términos de entrada MeSH: AZD-9291;AZD-9291 mesylate;AZD9291;AZD9291 mesylate;mereletinib;mereletinib mesilate;mereletinib mesylate;N-(2-((2-(dimethylamino)ethyl)methylamino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl)amino)phenyl)-2-propenamide;N-(2-((2-(dimethylamino
• Peso molecular: 499.62
• Reaxy-Rn: 23334373
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23334373&ln=

Objetivos asociados (humanos)

ERBB3 Tclin Receptor tyrosine-protein kinase erbB-3 (1 Activities)

Discover Target: ERBB3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ERBB2 Tclin Receptor tyrosine-protein kinase erbB-2 (1 Activities)

Discover Target: ERBB2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EGFR Tclin Epidermal growth factor receptor (92 Activities)

Discover Target: EGFR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CARS Tchem Cysteine--tRNA ligase, cytoplasmic (1 Activities)

Discover Target: CARS

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (1 Activities)

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 51 mg/mL (198.62 mM)

Referencias

1. Xin Zhang, Yuhan Jiang, Na Guo, Yifan Ding, Jingting Feng, Chenyang Miao, Yanni Lv.  (2023)  Application of SNAP-tag-EGFR cell membrane chromatography model in screening antitumor active components of Silybum marianum (L.) Gaertn.  JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,      [PMID:37976988] [10.1016/j.jpba.2023.115816]

2. Taotao Huo, Bin Zhu, Xiaoyu Shan, Jiaqi Song, Ziyi Wang, Jianxu Zhou, Xianpeng Zhang, Yuquan Bai, Chengcheng Liu, Yiyang Zhao, Na Mei, Yazhong Bu, Jia Zhang, Guangying Li.  (2025)  Allicin amplifies disulfidptosis during GOx catalyzing glucose-starvation for cancer therapy via simultaneous antimicrobial and antitumor intervention.  CHEMICAL ENGINEERING JOURNAL,      [PMID:] [10.1016/j.cej.2025.159871]

3. Zihan Zhu, Peigang Zhang, Kexin An, Kaihua Zhao, Xianghui Chen, Yuheng Pei, Martin M. F. Choi, Ning Wang, Wei Bian.  (2023)  pH/hyaluronidase dual responsive nano drug delivery systems for photothermal/chemotherapy combined treatment for non-small cell lung cancer.  NEW JOURNAL OF CHEMISTRY,  47  (46): (21175-21182).  [PMID:] [10.1039/D3NJ03075J]

4. Dianbao Zhang, Yukun Yang, Yixin Kang, Dongjie Xie, Xianfen Zhang, Jiqing Hao.  (2023)  Dysregulated expression of microRNA involved in resistance to osimertinib in EGFR mutant non-small cell lung cancer cells.  Journal of Thoracic Disease,      [PMID:37197540] [10.21037/jtd-23-401]

5. Rui Feng, Yong-Qi Zhen, Dongbo Wu, Lian Sun, Jin-Bu Xu, Xiaohuan Li, Lan Zhang, Feng Gao.  (2024)  Late-stage modification of complex drug: Base-controlled Pd-catalyzed regioselective synthesis and bioactivity of arylated osimertinibs.  Science Advances,  10  (10):   [PMID:38457511] [10.1126/sciadv.adl0026]

6. Zhitao Zhu, Zhengzhong Lv, Yurong Fan, Hongyuan Wen, Yuqi Zhang, Yirui Guo, Miao Li, Xingxiang Ren, Haibin Shi, Guohua Fan.  (2025)  A Neovascularization and EGFR Dual-Targeting Gold Nanotheranostic System for Non-Small Cell Lung Cancer Treatment.  Advanced Healthcare Materials,      [PMID:40500941] [10.1002/adhm.202500854]

7. Qiu Yueping, Liu Yijie, Ding Haiying, Xin Wenxiu, Lu Shuanghui, Hu Yan, Chen Jing, Weng Qinjie, Wang Jiajia, Fang Luo.  (2026)  Osimertinib activates TFEB to trigger hepatocyte cytoplasmic vacuolation-associated cell death.  Cell Communication and Signaling,      [PMID:41612351] [10.1186/s12964-026-02688-4]