Erlotinib (OSI-774) - Moligand™, 10mM in DMSO , Inhibitor of epidermal growth factor receptor;Inhibitor of OATP2B1, CAS No.183321-74-6, Inhibitor of epidermal growth factor receptor;Inhibitor of OATP2B1

CAS: 183321-74-6 Cat. No.: E408359 Molecular Weight: 393.44 EC Number: 689-196-2

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

CP358774, NSC 718781, Tarceva

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

In vitro

Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi human colon cancer cells and MDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi human colon cancer cells. Erlotinib inhibits growth of a panel of NSCLC cell lines including A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 with IC50 ranging from 29 nM to >20 μM. Erlotinib HCl(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells. The effects of Erlotinib HCl in combination with gemcitabine are considered additive in KRAS-mutated pancreatic cancer cells. Ten micromolar of Erlotinib HCl inhibits EGFR phospho-rylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites. Combination with Erlotinib HCl could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition.

In vivo

At doses of 100 mg/kg, Erlotinib HCl completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice. Erlotinib HCl (100 mg/Kg) inhibits H460a and A549 tumor models with 71 and 93% inhibition rate.
Cell Data

cell lines：KU-19-19 cells

Concentrations：30 nM-20 μM

Incubation Time：72 hours

Powder Purity:≥99%

Specifications

Synonyms

CP358774, NSC 718781, Tarceva

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Erlotinib (OSI-774, CP358774, NSC 718781, Tarceva) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of epidermal growth factor receptor;Inhibitor of OATP2B1

Names and Identifiers

• Isomeric SMILES: COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC
• Alternate CAS: 183321-74-6
• MeSH Entry Terms: 11C erlotinib;11C-erlotinib;358,774, CP;358774, CP;CP 358,774;CP 358774;CP-358,774;CP-358774;CP358,774;CP358774;erlotinib;erlotinib HCl;erlotinib hydrochloride;HCl, Erlotinib;Hydrochloride, Erlotinib;N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-
• Molecular Weight: 393.44
• Reaxy-Rn: 8798958
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8798958&ln=

Associated Targets(Human)

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 (84 Activities)

Discover Target: EGFR

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

STK10 Tchem Serine/threonine-protein kinase 10 (2 Activities)

Discover Target: STK10

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

GAK Tchem Cyclin-G-associated kinase (9 Activities)

Discover Target: GAK

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

SLCO2B1 Tchem Solute carrier organic anion transporter family member 2B1 (3 Activities)

Discover Target: SLCO2B1

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

SLK Tchem STE20-like serine/threonine-protein kinase (2 Activities)

Discover Target: SLK

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

PDGFRB Tclin Platelet-derived growth factor receptor beta (1 Activities)

Discover Target: PDGFRB

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

MAP3K19 Tchem Mitogen-activated protein kinase kinase kinase 19 (1 Activities)

Discover Target: MAP3K19

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

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro Water: 58 mg/mL (227.16 mM); DMSO: 9 mg/mL (35.24 mM); Ethanol: Insoluble
• Refractive Index: 1.62
• Melt Point(°C): 167-180°C

References

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2. Xiaofei Zhang, Mengyuan Lv, Yuyang Wang, Nan Zhang, Di Chen.  (2025)  Inner-wall biochar-coated pipette tip microextraction for rapid and sustainable determination of tyrosine kinase inhibitors in plasma.  RSC Advances,  15  (40): (33536-33548).  [PMID:40959299] [10.1039/D5RA05405B]

3. Zhao-Yang Wang, Hai-Long Wu, Yue-Yue Chang, Tong Wang, Wei Chen, Gao-Yan Tong, Ru-Qin Yu.  (2021)  Simultaneous determination of nine tyrosine kinase inhibitors in three complex biological matrices by using high-performance liquid chromatography–diode array detection combined with a second-order calibration method.  JOURNAL OF SEPARATION SCIENCE,  44  (21): (3914-3923).  [PMID:34463059] [10.1002/jssc.202100293]

4. Bao Shihui, Zheng Hailun, Ye Jinyao, Huang Huirong, Zhou Bin, Yao Qing, Lin Guangyong, Zhang Hailin, Kou Longfa, Chen Ruijie.  (2021)  Dual Targeting EGFR and STAT3 With Erlotinib and Alantolactone Co-Loaded PLGA Nanoparticles for Pancreatic Cancer Treatment.  Frontiers in Pharmacology,      [PMID:33815107] [10.3389/fphar.2021.625084]

5. Yue-Yue Chang, Hai-Long Wu, Huan Fang, Tong Wang, Yang-Zi Ouyang, Xiao-Dong Sun, Gao-Yan Tong, Yu-Jie Ding, Ru-Qin Yu.  (2020)  Comparison of three chemometric methods for processing HPLC-DAD data with time shifts: Simultaneous determination of ten molecular targeted anti-tumor drugs in different biological samples.  TALANTA,      [PMID:33379025] [10.1016/j.talanta.2020.121798]

6. Yang Lehe, Lin Shichong, Kang Yanting, Xiang Youqun, Xu Lingyuan, Li Jifa, Dai Xuanxuan, Liang Guang, Huang Xiaoying, Zhao Chengguang.  (2019)  Rhein sensitizes human pancreatic cancer cells to EGFR inhibitors by inhibiting STAT3 pathway.  JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH,  38  (1): (1-13).  [PMID:30674340] [10.1186/s13046-018-1015-9]

7. Jingwei Shao, Guirong Zheng, Hongning Chen, Jian Liu, Aixiao Xu, Fan Chen, Tao Li, Yusheng Lu, Jianguo Xu, Ning Zheng, Lee Jia.  (2017)  Metapristone (RU486 metabolite) suppresses NSCLC by targeting EGFR-mediated PI3K/AKT pathway.  Oncotarget,      [PMID:29108234] [10.18632/oncotarget.18640]

8. Qianqian Wang, Yuanyuan Zheng, Bowen Deng, Di Chen, Liuqun Jia, Nian Shi.  (2024)  Automated kapok fiber-based pipette-tip solid-phase extraction coupled with liquid chromatography-tandem mass spectrometry for rapid and sensitive analysis of tyrosine kinase inhibitors in plasma.  JOURNAL OF CHROMATOGRAPHY A,      [PMID:39378625] [10.1016/j.chroma.2024.465420]

9. Jing Ye, Yuanyuan Zheng, Xiangyu Li, Xingyi Jiang, Di Chen.  (2024)  Melt-blown polypropylene nonwoven as an efficient and eco-economic sorbent for pipette tip micro-solid phase extraction for the determination of tyrosine kinase inhibitors.  ANALYTICA CHIMICA ACTA,      [PMID:39396303] [10.1016/j.aca.2024.343240]

10. Qianqian Wang, Yuwei Liu, Yuanyuan Zheng, Di Chen, Ya Xie, Nian Shi.  (2024)  MonoTip C18 pipette tip solid-phase extraction coupled with liquid chromatography-tandem mass spectrometry enables rapid and automated therapeutic drug monitoring of tyrosine kinase inhibitors.  Arabian Journal of Chemistry,      [PMID:] [10.1016/j.arabjc.2024.105976]

11. Shuangyu Tian, Jinghang Li, Dongdong Wang, Yingchao Han, Honglian Dai, Lesan Yan.  (2024)  Sonodynamic-chemotherapy synergy with chlorin e6-based carrier-free nanoparticles for non-small cell lung cancer.  Journal of Materials Chemistry B,      [PMID:38487900] [10.1039/D4TB00009A]

12. Dong Wang, Mengrong Li, Tingting Dai, Xiangyu Zhang, Di Chen.  (2025)  In-syringe polypropylene fiber-supported liquid-phase microextraction followed by LC-MS/MS for rapid and sensitive determination of tyrosine kinase inhibitors in plasma.  MICROCHEMICAL JOURNAL,      [PMID:] [10.1016/j.microc.2025.114222]

13. Wang Dong, Li Mengrong, Zhang Xiangyu, Chai Shiwei, Chen Di.  (2026)  Ultrasonic-assisted magnetic sorbent–wrapped stick dip extraction enables batch-scale and green LC-MS/MS analysis of tyrosine kinase inhibitors in plasma.  ANALYTICAL AND BIOANALYTICAL CHEMISTRY,      [PMID:41575510] [10.1007/s00216-026-06335-2]

14. Dong Wang, Mengrong Li, Xiangyu Zhang, Xu Miao, Lifeng Han, Di Chen.  (2026)  Standardized ready-to-use natural deep eutectic solvent-impregnated polypropylene fiber units for robust and high-throughput determination of tyrosine kinase inhibitors in biological fluids.  ANALYTICA CHIMICA ACTA,      [PMID:] [10.1016/j.aca.2026.345394]