Lapatinib (GW-572016) - Moligand™, 10mM in DMSO , Inhibitor of epidermal growth factor receptor;Inhibitor of erb-b2 receptor tyrosine kinase 2, CAS No.231277-92-2, Inhibitor of epidermal growth factor receptor;Inhibitor of erb-b2 receptor tyrosine kinase 2

CAS: 231277-92-2 Cat. No.: L408018 Molecular Weight: 581.06 EC Number: 878-720-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

GSK572016, GW2016 | N-(4-(3-fluorobenzyloxy)-3-chlorophenyl)-6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-amine,di4-methylbenzenesulfonate

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Lapatinib (GW-572016, GSK572016, GW2016), used in the form of Lapatinib Ditosylate, is a potentEGFRandErbB2inhibitor withIC50of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib inducesferroptosisandautophagic cell death.
In vitro

Lapatinib weakly inhibits the activity of ErbB4 with IC50 of 367 nM, and displays >300-fold selectivity for EGFR and ErbB2 over other kinases such as c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2, and VEGFR2. Lapatinib significantly inhibits receptor autophosphorylation of EGFR and ErbB2 in a dose-dependent manner with IC50 of 170 nM and 80 nM, respectively in HN5 cells; as well as 210 nM and 60 nM, respectively in BT474 cells. Unlike OSI-774 and Iressa (ZD1839) which preferentially inhibit the growth of the EGFR-overexpressing cells, Lapatinib inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib displays higher inhibitory activity against EGFR- or ErbB2-overexpressing cells with IC50 of 0.09-0.21 μM, compared with cells expressing low levels of EGFR or ErbB2 with IC50 of 3-12 μM, and exhibits ~100-fold selectivity over the normal fibroblast cells. Lapatinib potently inhibits the outgrowth of EGFR-overexpressing HN5 and A-431 cells, as well as ErbB2-overexpressing BT474 and N87 cells, and significantly induces G1 arrest of HN5 cells and apoptosis of BT474 cells, which are associated with inhibition of AKT phosphorylation.

In vivo

Oral administration of Lapatinib (~100 mg/kg) twice daily significantly inhibits the growth of BT474 and HN5 xenografts in a dose-dependent manner.
Cell Data

cell lines：

Concentrations：Dissolved in DMSO, final concentrations ~100 μM

Incubation Time：72 hours

Powder Purity:≥99%

Specifications

Synonyms

GSK572016, GW2016 | N-(4-(3-fluorobenzyloxy)-3-chlorophenyl)-6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-amine, di4-methylbenzenesulfonate

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Lapatinib (GW-572016, GSK572016, GW2016), used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.

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 erb-b2 receptor tyrosine kinase 2

Names and Identifiers

• Isomeric SMILES: CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl
• Alternate CAS: 231277-92-2,913989-15-8,388082-78-8
• NSC Number: 745750
• MeSH Entry Terms: GW 282974X;GW 572016;GW-282974X;GW-572016;GW282974X;GW572016;lapatinib;lapatinib ditosylate;N-(3-chloro-4-(((3-fluorobenzyl)oxy)phenyl)-6-(5-(((2-methylsulfonyl)ethyl)amino)methyl) -2-furyl)-4-quinazolinamine;Tykerb
• Molecular Weight: 581.06
• Reaxy-Rn: 10502247
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10502247&ln=

Associated Targets(Human)

ERBB4 Tclin Receptor tyrosine-protein kinase erbB-4 (2 Activities)

Discover Target: ERBB4

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

ERBB2 Tclin Receptor tyrosine-protein kinase erbB-2 (26 Activities)

Discover Target: ERBB2

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

EGFR Tclin Epidermal growth factor receptor (66 Activities)

Discover Target: EGFR

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)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 51 mg/mL (200.59 mM); Water: Insoluble; Ethanol: Insoluble
• Melt Point(°C): 147 °C

References

1. Lin Su, Dongdong Jin, Yuqiong Wang, Qinglong Wang, Chengfeng Pan, Shuai Jiang, Haojin Yang, Zhengxin Yang, Xin Wang, Neng Xia, Kai Fung Chan, Philip Wai Yan Chiu, Joseph Jao-Yiu Sung, Li Zhang.  (2023)  Modularized microrobot with lock-and-detachable modules for targeted cell delivery in bile duct.  Science Advances,  9  (50):   [PMID:38100592] [10.1126/sciadv.adj0883]

2. 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]

3. Longfa Kou, Xinyu Jiang, Yingying Tang, Xing Xia, Yingtao Li, Aimin Cai, Hailun Zheng, Hailin Zhang, Vadivel Ganapathy, Qing Yao, Ruijie Chen.  (2021)  Resetting amino acid metabolism of cancer cells by ATB0,+-targeted nanoparticles for enhanced anticancer therapy.  Bioactive Materials,      [PMID:34820552] [10.1016/j.bioactmat.2021.07.009]

4. 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]

5. Ke Du, Yuting Liu, Lu Zhang, Lixia Peng, Wenjing Dong, Yajie Jiang, Mingming Niu, Yuanchao Sun, Chuanhong Wu, Yujuan Niu, Yonghe Ding.  (2024)  Lapatinib combined with doxorubicin causes dose-dependent cardiotoxicity partially through activating the p38MAPK signaling pathway in zebrafish embryos.  BIOMEDICINE & PHARMACOTHERAPY,      [PMID:38653111] [10.1016/j.biopha.2024.116637]

6. Ru Li, Yimei Ma, Anqi He, Yamin Pu, Xuanting Wan, Hongbao Sun, Ningyu Wang, Min Luo, Guan Wang, Yong Xia.  (2025)  Fasting enhances the efficacy of Sorafenib in breast cancer via mitophagy mediated ROS-driven p53 pathway.  FREE RADICAL BIOLOGY AND MEDICINE,      [PMID:39864757] [10.1016/j.freeradbiomed.2025.01.047]

7. 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]

8. 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]