Cat. No.: HY-50898

Lapatinib

(Synonyms: GW572016; GW2016)

95 Cited Publications

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Based on 95 publication(s) in Google Scholar

Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.

For research use only. We do not sell to patients.

Purity: 99.83%
CAS No.: 231277-92-2
Formula: C₂₉H₂₆ClFN₄O₄S
Molecular Weight:581.06

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Lapatinib Chemical Structure

CAS No.: 231277-92-2

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (95)
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Biological Activity

Description

IC₅₀ & Target^[1]

EGFR

10.2 nM (IC₅₀, Cell Free Assay)

ErbB2

9.8 nM (IC₅₀, Cell Free Assay)

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
3T3	EC₅₀	13 μM Compound: 1	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 48 hrs by chlorophenol red-beta-D-galactopyranoside based assay Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 48 hrs by chlorophenol red-beta-D-galactopyranoside based assay	[PMID: 28337329]
4T1	IC₅₀	10.37 nM Compound: Lapatinib	Cytotoxicity against mouse triple negative 4T1 cells Cytotoxicity against mouse triple negative 4T1 cells	[PMID: 24890652]
4T1	IC₅₀	7.86 μM Compound: Lapatinib	Cytotoxicity against mouse 4T1 cells cultured as 2D cells assessed as inhibition of cell growth incubated for 48 hrs by alamar blue assay Cytotoxicity against mouse 4T1 cells cultured as 2D cells assessed as inhibition of cell growth incubated for 48 hrs by alamar blue assay	[PMID: 38408027]
A2780	IC₅₀	10.4 μM Compound: Lapatinib	Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay	[PMID: 29684708]
A2780	IC₅₀	10.4 μM Compound: Lapatinib	Antiproliferative activity against human A2780 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 31655429]
A-431	IC₅₀	104 nM Compound: 3	Cytotoxicity against human A431 cells after 72 hrs by SRB assay Cytotoxicity against human A431 cells after 72 hrs by SRB assay	[PMID: 19888761]
A-431	IC₅₀	52 nM Compound: Lapatinib	Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA	[PMID: 20346655]
A-431	IC₅₀	>10000 nM Compound: Lapatinib	Inhibition of IGF1R intracellular phosphorylation in human A431 cells by ELISA Inhibition of IGF1R intracellular phosphorylation in human A431 cells by ELISA	[PMID: 20346655]
A-431	IC₅₀	0.97 μM Compound: 5, GW-572016	Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay	[PMID: 21080629]
A-431	IC₅₀	2.62 μM Compound: Lapatinib	Cytotoxicity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay Cytotoxicity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay	[PMID: 22182581]
A-431	IC₅₀	104 nM Compound: 1	Cytotoxicity against human A431 cells overexpressing HER-1 gene after 72 hrs by SRB assay Cytotoxicity against human A431 cells overexpressing HER-1 gene after 72 hrs by SRB assay	[PMID: 22372864]
A-431	IC₅₀	2.6 μM Compound: 3	Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay	[PMID: 22595177]
A-431	IC₅₀	643.1 nM Compound: Lapatinib	Cytotoxicity against human A431 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human A431 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
A-431	IC₅₀	0.15 μM Compound: 3; GW-572016	Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
A-431	IC₅₀	4.8 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 28711703]
A-431	IC₅₀	4.8 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 29421573]
A-431	IC₅₀	2.66 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells after 72 hrs by MTT assay Antiproliferative activity against human A431 cells after 72 hrs by MTT assay	[PMID: 30508379]
A-431	IC₅₀	4.8 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
A-431	IC₅₀	3.59 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells overexpressing EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human A431 cells overexpressing EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
A-431	IC₅₀	4.8 μM Compound: Lapatinib	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition by MTT assay	[PMID: 32739648]
A549	IC₅₀	8.5 μM Compound: 5, GW-572016	Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay	[PMID: 21080629]
A549	IC₅₀	6.74 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 27187856]
A549	IC₅₀	0.51 μM Compound: 3; GW-572016	Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
A549	IC₅₀	14.9 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells harboring wild type EGFR/K-Ras mutant after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR/K-Ras mutant after 72 hrs by MTT assay	[PMID: 28711703]
A549	IC₅₀	14.9 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells harboring wild type EGFR/K-ras mutant after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR/K-ras mutant after 72 hrs by MTT assay	[PMID: 29421573]
A549	IC₅₀	3.64 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30508379]
A549	IC₅₀	11 μM Compound: Tykerb(R)	Antiproliferative activity against human A549 cells overexpressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells overexpressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31125894]
A549	IC₅₀	14.9 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
A549	IC₅₀	11.3 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs under normoxia condition by SRB assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs under normoxia condition by SRB assay	[PMID: 32739648]
A549	IC₅₀	13.26 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs under hypoxia condition by SRB assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs under hypoxia condition by SRB assay	[PMID: 32739648]
A549	IC₅₀	14.9 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition by MTT assay	[PMID: 32739648]
AU565	IC₅₀	0.064 μM Compound: Lapatinib	Antiproliferative activity against human AU565 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay Antiproliferative activity against human AU565 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay	[PMID: 33314925]
B16-F10	IC₅₀	0.21 μM Compound: Lapatinib	Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay	[PMID: 26652482]
BaF3	IC₅₀	>2000 nM Compound: Lapatinib	Antiproliferative activity against mouse BaF3 cells harboring HER2 YVMA mutant by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring HER2 YVMA mutant by CellTiter-Glo assay	[PMID: 38518121]
Bel-7402	IC₅₀	3.7 μM Compound: Lapatinib	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay	[PMID: 28092860]
BT-474	IC₅₀	25 nM Compound: 3	Antiproliferative activity against human BT474 cell line Antiproliferative activity against human BT474 cell line	[PMID: 16483772]
BT-474	IC₅₀	0.08 μM Compound: 1, GW-572016	Inhibition of BT474 cell growth after 72 hrs Inhibition of BT474 cell growth after 72 hrs	[PMID: 16777410]
BT-474	IC₅₀	25 nM Compound: 3	Antiproliferative activity against human BT474 cells overexpressing ErB2 Antiproliferative activity against human BT474 cells overexpressing ErB2	[PMID: 18653333]
BT-474	IC₅₀	140 nM Compound: Lapatinib	Inhibition of ERBb2 phosphorylation in human BT474 cells by ELISA Inhibition of ERBb2 phosphorylation in human BT474 cells by ELISA	[PMID: 20817523]
BT-474	IC₅₀	0.025 μM Compound: lapatinib	Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method	[PMID: 21887403]
BT-474	IC₅₀	0.1 μM Compound: Lapatinib	Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining	[PMID: 22101132]
BT-474	IC₅₀	63.9 nM Compound: Lapatinib	Cytotoxicity against human BT474 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human BT474 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
BT-474	GI₅₀	0.93 μM Compound: Lapatinib	Cytotoxicity against human BT474 cells expressing HER2 after 72 hrs by Cell Titer Glo assay Cytotoxicity against human BT474 cells expressing HER2 after 72 hrs by Cell Titer Glo assay	[PMID: 26475520]
BT-474	IC₅₀	0.031 μM Compound: Lapatinib	Cytotoxicity against human BT474 cells expressing Her2 assessed as reduction in cell viability after 72 hrs by cell titer-glo luminescence assay Cytotoxicity against human BT474 cells expressing Her2 assessed as reduction in cell viability after 72 hrs by cell titer-glo luminescence assay	[PMID: 27288180]
BT-474	IC₅₀	0.1 μM Compound: 3; GW-572016	Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
BT-474	GI₅₀	0.2 μM Compound: Lapatinib	Cytotoxicity against human BT474 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human BT474 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
BT-474	IC₅₀	0.037 μM Compound: Lapatinib	Antiproliferative activity against human BT474 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human BT474 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
BT-474	IC₅₀	0.064 μM Compound: Lapatinib	Antiproliferative activity against human BT474 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay Antiproliferative activity against human BT474 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay	[PMID: 33314925]
CAL-27	IC₅₀	<32 nM Compound: 5, GW-572016	Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot	[PMID: 21080629]
CAL-27	IC₅₀	0.007 μM Compound: 5, GW-572016	Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay	[PMID: 21080629]
CAL-27	IC₅₀	0.53 μM Compound: 5, Tykerb	Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
Calu-3	IC₅₀	0.23 μM Compound: Lapatinib	Cytotoxicity against human Calu3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human Calu3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
Calu-3	IC₅₀	0.1 μM Compound: Lapatinib	Antiproliferative activity against human Calu3 cells after 72 hrs by MTT assay Antiproliferative activity against human Calu3 cells after 72 hrs by MTT assay	[PMID: 28092860]
Calu-3	IC₅₀	0.216 μM Compound: Lapatinib	Antiproliferative activity against human Calu3 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human Calu3 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
CAMA-1	IC₅₀	>10 μM Compound: Lapatinib, Tykerb	Antiproliferative activity against human progesterone receptor and HER2 deficient CAMA1 cells expressing estrogen receptor after 72 hrs by MTT assay Antiproliferative activity against human progesterone receptor and HER2 deficient CAMA1 cells expressing estrogen receptor after 72 hrs by MTT assay	[PMID: 23927972]
COLO 205	IC₅₀	4.6 μM Compound: Lapatinib	Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay	[PMID: 28092860]
CWR22R	IC₅₀	6.06 μM Compound: 5, Tykerb	Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
DU-145	IC₅₀	2.99 μM Compound: 5, Tykerb	Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
DU-145	GI₅₀	20 μM Compound: Lapatinib	Antiproliferative activity against human DU145 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human DU145 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
EOL1	GI₅₀	0.41 μM Compound: Lapatinib	Cytotoxicity against human EOL-1 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human EOL-1 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
HCC1954	IC₅₀	5.5 μM Compound: Lapatinib	Antiproliferative activity against human HCC1954 cells assessed as reduction in cell proliferation measured after 72 hrs by celltiter-glo assay Antiproliferative activity against human HCC1954 cells assessed as reduction in cell proliferation measured after 72 hrs by celltiter-glo assay	[PMID: 20571069]
HCC1954	IC₅₀	5 μM Compound: Tykerb(R)	Antiproliferative activity against human HCC1954 cells overexpressing HER2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC1954 cells overexpressing HER2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31125894]
HCC70	IC₅₀	3.2 μM Compound: Lapatinib	Antiproliferative activity against human HCC70 cells assessed as reduction in cell proliferation measured after 72 hrs by celltiter-glo assay Antiproliferative activity against human HCC70 cells assessed as reduction in cell proliferation measured after 72 hrs by celltiter-glo assay	[PMID: 20571069]
HCC827	GI₅₀	22.3 μM Compound: Lapatinib	Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
HCC827	IC₅₀	0.6 μM Compound: Lapatinib	Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 del mutant after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 del mutant after 72 hrs by MTT assay	[PMID: 29421573]
HCC827	IC₅₀	0.6 μM Compound: Lapatinib	Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
HCT-116	IC₅₀	42.36 μM Compound: 3	Antiproliferative activity against human HCT116 cells by MTT assay Antiproliferative activity against human HCT116 cells by MTT assay	[PMID: 21570843]
HCT-116	IC₅₀	13.14 μM Compound: 5, Tykerb	Cytotoxicity against human HCT116 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human HCT116 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
HCT-116	IC₅₀	6.2 μM Compound: Lapatinib	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 28092860]
HCT-116	IC₅₀	10.12 μM Compound: Lapatinib	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 29684708]
HCT-116	IC₅₀	5.92 μM Compound: Lapatinib	Cytotoxicity against human HCT116 cells after 24 hrs by SRB assay Cytotoxicity against human HCT116 cells after 24 hrs by SRB assay	[PMID: 30096580]
HCT-116	GI₅₀	20 μM Compound: Lapatinib	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
HCT-116	IC₅₀	5.92 μM Compound: Lapatinib	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by SRB assay	[PMID: 32361329]
HCT-116	IC₅₀	12 nM Compound: Lapatinib	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 33545637]
HEK293	IC₅₀	>10 μM Compound: 5, GW-572016	Inhibition of human recombinant HDAC1 expressed in HEK293 cells Inhibition of human recombinant HDAC1 expressed in HEK293 cells	[PMID: 21080629]
HEK293	IC₅₀	>10 μM Compound: 5, GW-572016	Inhibition of human recombinant HDAC6 expressed in HEK293 cells Inhibition of human recombinant HDAC6 expressed in HEK293 cells	[PMID: 21080629]
HEK-293T	CC₅₀	123.17 μM Compound: Lapatinib	Cytotoxicity against human HEK293T cells for 24 hrs by MTT assay Cytotoxicity against human HEK293T cells for 24 hrs by MTT assay	[PMID: 26652482]
HeLa	IC₅₀	>100 μM Compound: 5, GW-572016	Inhibition of HDAC in human HeLa cell nuclear extracts Inhibition of HDAC in human HeLa cell nuclear extracts	[PMID: 21080629]
HeLa	IC₅₀	5.9 μM Compound: 5, GW-572016	Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay	[PMID: 21080629]
HeLa	IC₅₀	0.12 μM Compound: Lapatinib	Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay	[PMID: 26652482]
Hep 3B2	IC₅₀	5.49 μM Compound: lapatinib	Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay	[PMID: 20143778]
HepG2	IC₅₀	6.27 μM Compound: lapatinib	Antiproliferative activity against human HepG2 cells after hrs by ATP content assay Antiproliferative activity against human HepG2 cells after hrs by ATP content assay	[PMID: 20143778]
HepG2	IC₅₀	0.27 μM Compound: Lapatinib	Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay	[PMID: 26652482]
HepG2	IC₅₀	11.71 μM Compound: Lapatinib	Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay	[PMID: 30096580]
HepG2	IC₅₀	11.71 μM Compound: Lapatinib	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by SRB assay	[PMID: 32361329]
HFF	IC₅₀	9.9 μM Compound: 1, GW-572016	Inhibition of HFF cell growth Inhibition of HFF cell growth	[PMID: 16777410]
HN5	IC₅₀	25 nM Compound: 3	Antiproliferative activity against human HN5 cell line Antiproliferative activity against human HN5 cell line	[PMID: 16483772]
HN5	IC₅₀	0.12 μM Compound: 1, GW-572016	Inhibition of HN5 cell growth after 72 hrs Inhibition of HN5 cell growth after 72 hrs	[PMID: 16777410]
HN5	IC₅₀	0.01 μM Compound: Lapatinib	Inhibition of EGF-induced EGFR phosphorylation at Tyr-residue in human HN5 cells preincubated for 24 hrs followed by EGF-stimulation and measured after 15 mins by Western blot analysis Inhibition of EGF-induced EGFR phosphorylation at Tyr-residue in human HN5 cells preincubated for 24 hrs followed by EGF-stimulation and measured after 15 mins by Western blot analysis	[PMID: 30600149]
HS27	IC₅₀	>10000 nM Compound: 3	Cytotoxicity against human HS27 cells after 72 hrs by SRB assay Cytotoxicity against human HS27 cells after 72 hrs by SRB assay	[PMID: 19888761]
HT-29	IC₅₀	4.62 μM Compound: 5, Tykerb	Cytotoxicity against human HT-29 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human HT-29 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
HT-29	IC₅₀	12.67 μM Compound: Lapatinib	Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 31655429]
HT-29	IC₅₀	6.81 μM Compound: Lapatinib	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs under normoxia condition by SRB assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs under normoxia condition by SRB assay	[PMID: 32739648]
HT-29	IC₅₀	8.85 μM Compound: Lapatinib	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs under hypoxia condition by SRB assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs under hypoxia condition by SRB assay	[PMID: 32739648]
HUVEC	IC₅₀	47.31 μM Compound: Lapatinib	Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]
JeKo-1	GI₅₀	5 μM Compound: Lapatinib	Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
JIMT-1	IC₅₀	>10000 nM Compound: 1	Cytotoxicity against human JIMT1 cells expressing low HER-2 after 72 hrs by SRB assay Cytotoxicity against human JIMT1 cells expressing low HER-2 after 72 hrs by SRB assay	[PMID: 22372864]
K562	GI₅₀	5.7 μM Compound: Lapatinib	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
KB	IC₅₀	0.062 μM Compound: Lapatinib	Inhibition of EGFR in human KB cells assessed as reduction in EGF-stimulated EGFR phosphorylation preincubated for 1 hr followed by EGF stimulation and measured after 6 mins by ELISA Inhibition of EGFR in human KB cells assessed as reduction in EGF-stimulated EGFR phosphorylation preincubated for 1 hr followed by EGF stimulation and measured after 6 mins by ELISA	[PMID: 32139324]
KG-1a	IC₅₀	9.76 μM Compound: Lapatinib	Antiproliferative activity against human KG1a cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human KG1a cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
L929	IC₅₀	2.05 μM Compound: Lapatinib	Cytotoxicity against mouse L929 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against mouse L929 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 30508379]
LNCaP	IC₅₀	3.68 μM Compound: 5, Tykerb	Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MCF7	IC₅₀	6.6 μM Compound: lapatinib	Antiproliferative activity against human MCF7 cells after hrs by ATP content assay Antiproliferative activity against human MCF7 cells after hrs by ATP content assay	[PMID: 20143778]
MCF7	IC₅₀	4.83 μM Compound: 5, Tykerb	Cytotoxicity against human MCF7 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human MCF7 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MCF7	IC₅₀	15.71 μM Compound: lapatinib	Cytotoxicity against human MCF7 cells expressing pcDNA3 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay Cytotoxicity against human MCF7 cells expressing pcDNA3 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay	[PMID: 24355130]
MCF7	IC₅₀	15.79 μM Compound: lapatinib	Cytotoxicity against human MCF7 cells expressing HER2 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay Cytotoxicity against human MCF7 cells expressing HER2 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay	[PMID: 24355130]
MCF7	IC₅₀	19.22 μM Compound: lapatinib	Cytotoxicity against human MCF7 cells expressing HER2delta16 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay Cytotoxicity against human MCF7 cells expressing HER2delta16 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay	[PMID: 24355130]
MCF7	IC₅₀	64.9 nM Compound: Lapatinib	Cytotoxicity against human ER-positive MCF7 cells Cytotoxicity against human ER-positive MCF7 cells	[PMID: 24890652]
MCF7	IC₅₀	0.011 μM Compound: Lapatinib	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 25151582]
MCF7	IC₅₀	8468 nM Compound: Lapatinib	Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
MCF7	IC₅₀	0.47 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay	[PMID: 26652482]
MCF7	GI₅₀	8.1 μM Compound: Lapatinib	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
MCF7	IC₅₀	6.8 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 29684708]
MCF7	IC₅₀	5.02 μM Compound: Lapatinib	Cytotoxicity against human MCF7 cells after 24 hrs by SRB assay Cytotoxicity against human MCF7 cells after 24 hrs by SRB assay	[PMID: 30096580]
MCF7	IC₅₀	4.691 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30792101]
MCF7	IC₅₀	95 μM Compound: Tykerb(R)	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31125894]
MCF7	IC₅₀	6.8 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 31655429]
MCF7	IC₅₀	5.02 μM Compound: Lapatinib	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by SRB assay	[PMID: 32361329]
MCF7	IC₅₀	6.301 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay	[PMID: 33314925]
MCF7	IC₅₀	21 nM Compound: Lapatinib	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 33545637]
MCF7	IC₅₀	12.62 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MCF7	IC₅₀	3.38 μM Compound: 40	Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 3 days by MTT assay Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 3 days by MTT assay	[PMID: 38908102]
MDA-MB-231	IC₅₀	5.4 μM Compound: lapatinib	Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay	[PMID: 20143778]
MDA-MB-231	IC₅₀	7.7 μM Compound: 5, Tykerb	Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MDA-MB-231	IC₅₀	20 nM Compound: Lapatinib	Cytotoxicity against human triple negative MDA-MB-231 cells Cytotoxicity against human triple negative MDA-MB-231 cells	[PMID: 24890652]
MDA-MB-231	IC₅₀	>100 μM Compound: Lapatinib	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
MDA-MB-231	IC₅₀	4.691 μM Compound: Lapatinib	Antiproliferative activity against human MDA231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA231 cells after 72 hrs by MTT assay	[PMID: 30792101]
MDA-MB-231	GI₅₀	20 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MDA-MB-231	IC₅₀	10.6 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	[PMID: 33139111]
MDA-MB-231	IC₅₀	10.373 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay	[PMID: 33314925]
MDA-MB-231	IC₅₀	29.39 μM Compound: Lapatinib	Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	30.78 μM Compound: Lapatinib	Antiproliferative activity against drug-tolerant human MDA-MB-231/lapatinib cells assessed as CD44-positive cells measured after 24 hrs by MTT assay Antiproliferative activity against drug-tolerant human MDA-MB-231/lapatinib cells assessed as CD44-positive cells measured after 24 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	5.86 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-361	IC₅₀	1029 nM Compound: 1	Cytotoxicity against ER activated human MDA-MB-361 cells expressing Her-2, Src and PIK3CA mutant after 72 hrs by SRB assay Cytotoxicity against ER activated human MDA-MB-361 cells expressing Her-2, Src and PIK3CA mutant after 72 hrs by SRB assay	[PMID: 22372864]
MDA-MB-435	IC₅₀	29.7 nM Compound: Lapatinib	Cytotoxicity against human MDA-MB-435 cells Cytotoxicity against human MDA-MB-435 cells	[PMID: 24890652]
MDA-MB-453	IC₅₀	555 nM Compound: 1	Cytotoxicity against PTEN-deficient human MDA-MB-453 cells expressing HER-2, and PIK3CA mutant after 72 hrs by SRB assay Cytotoxicity against PTEN-deficient human MDA-MB-453 cells expressing HER-2, and PIK3CA mutant after 72 hrs by SRB assay	[PMID: 22372864]
MDA-MB-453	IC₅₀	0.19 μM Compound: Lapatinib	Cytotoxicity against human MDA-MB-453 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human MDA-MB-453 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
MDA-MB-453	IC₅₀	>20 μM Compound: Lapatinib	Photocytotoxicity against human MDA-MB-453 cells cultured as 3D spheroids assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Photocytotoxicity against human MDA-MB-453 cells cultured as 3D spheroids assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 37421416]
MDA-MB-468	IC₅₀	4.5 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell proliferation measured after 72 hrs by celltiter-glo assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell proliferation measured after 72 hrs by celltiter-glo assay	[PMID: 20571069]
MDA-MB-468	IC₅₀	23.46 μM Compound: 3	Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay	[PMID: 21570843]
MDA-MB-468	IC₅₀	83.2 nM Compound: Lapatinib	Cytotoxicity against human triple negative MDA-MB-468 cells Cytotoxicity against human triple negative MDA-MB-468 cells	[PMID: 24890652]
MDA-MB-468	IC₅₀	20 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay	[PMID: 28092860]
MEXF276L	IC₅₀	11.37 μM Compound: 5, Tykerb	Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MIA PaCa-2	GI₅₀	10 μM Compound: Lapatinib	Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MKN-45	IC₅₀	11.48 μM Compound: 5, Tykerb	Cytotoxicity against human MKN45 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human MKN45 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MRC5	IC₅₀	>100 μM Compound: Lapatinib	Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
MRC5	IC₅₀	13.66 μM Compound: Lapatinib	Cytotoxicity against human MRC5 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 31655429]
MV4-11	GI₅₀	10 μM Compound: Lapatinib	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
NCI-H1975	IC₅₀	>1000 nM Compound: 3	Cytotoxicity against human NCI-H1975 cells after 24 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells after 24 hrs by MTT assay	[PMID: 19888761]
NCI-H1975	IC₅₀	>1000 nM Compound: 1	Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant after 72 hrs by SRB assay Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant after 72 hrs by SRB assay	[PMID: 22372864]
NCI-H1975	IC₅₀	7.25 μM Compound: 3; GW-572016	Antiproliferative activity against human NCI-H1975 expressing EGFR T790M/L858R mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human NCI-H1975 expressing EGFR T790M/L858R mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
NCI-H1975	IC₅₀	9.08 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay	[PMID: 28711703]
NCI-H1975	IC₅₀	12.68 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 29421573]
NCI-H1975	IC₅₀	9 μM Compound: Tykerb(R)	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31125894]
NCI-H1975	IC₅₀	12.68 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
NCI-H1975	IC₅₀	7.37 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
NCI-H460	IC₅₀	13.46 μM Compound: 5, Tykerb	Cytotoxicity against human H460 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human H460 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
NCI-H460	IC₅₀	>100 μM Compound: Lapatinib	Cytotoxicity against human NCI-H460 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human NCI-H460 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
NCI-H460	IC₅₀	8.4 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay	[PMID: 28092860]
NCI-H522	IC₅₀	6.4 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H522 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H522 cells after 72 hrs by MTT assay	[PMID: 28092860]
NCI-N87	IC₅₀	0.08 μM Compound: 1, GW-572016	Inhibition of N87 cell growth after 72 hrs Inhibition of N87 cell growth after 72 hrs	[PMID: 16777410]
NCI-N87	IC₅₀	100 nM Compound: Lapatinib	Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA	[PMID: 20346655]
NCI-N87	IC₅₀	0.04 μM Compound: Lapatinib	Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell proliferation measured after 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell proliferation measured after 72 hrs by celltiter-glo assay	[PMID: 20571069]
NCI-N87	IC₅₀	0.09 μM Compound: Lapatinib	Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue staining Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue staining	[PMID: 22101132]
NCI-N87	IC₅₀	36 nM Compound: 1	Cytotoxicity against human NCI-N87 cells expressing HER-2 after 72 hrs by SRB assay Cytotoxicity against human NCI-N87 cells expressing HER-2 after 72 hrs by SRB assay	[PMID: 22372864]
NCI-N87	IC₅₀	0.053 μM Compound: Lapatinib	Antiproliferative activity against human NCI-N87 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-N87 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
NIH3T3	IC₅₀	4.3 μM Compound: 3	Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay	[PMID: 22595177]
OVCAR-3	IC₅₀	13.44 μM Compound: 5, Tykerb	Cytotoxicity against human OVCAR3 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human OVCAR3 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
PANC-1	IC₅₀	8.12 μM Compound: 5, Tykerb	Cytotoxicity against human PANC1 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human PANC1 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
PBMC	IC₅₀	28 μM Compound: lapatinib	Cytotoxicity against human PBMC assessed as induction of cell death by cell Titer-Glo assay Cytotoxicity against human PBMC assessed as induction of cell death by cell Titer-Glo assay	[PMID: 29909341]
PC-3M	IC₅₀	4.55 μM Compound: 5, Tykerb	Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
RAW264.7	EC₅₀	11 μM Compound: 1	Antileishmanial activity against luciferase-expressing Leishmania major amastigotes infected in mouse RAW264.7 cells after 96 hrs by luminescence assay Antileishmanial activity against luciferase-expressing Leishmania major amastigotes infected in mouse RAW264.7 cells after 96 hrs by luminescence assay	[PMID: 28337329]
RKO	IC₅₀	5.35 μM Compound: 5, Tykerb	Cytotoxicity against human RKO cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human RKO cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
SAOS-2	IC₅₀	9.38 μM Compound: 5, Tykerb	Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
Sf21	IC₅₀	>10 μM Compound: 5, GW-572016	Inhibition of Flag tagged human recombinant HDAC3 expressed in Sf21 cells coexpressing SMRT DAD domain Inhibition of Flag tagged human recombinant HDAC3 expressed in Sf21 cells coexpressing SMRT DAD domain	[PMID: 21080629]
Sf21	IC₅₀	>10 μM Compound: 5, GW-572016	Inhibition of Flag tagged human recombinant HDAC8 expressed in Sf21 cells Inhibition of Flag tagged human recombinant HDAC8 expressed in Sf21 cells	[PMID: 21080629]
SK-BR-3	IC₅₀	0.017 μM Compound: GW-572016	Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay	[PMID: 19028425]
SK-BR-3	IC₅₀	29 nM Compound: 3	Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay	[PMID: 19888761]
SK-BR-3	IC₅₀	0.04 μM Compound: lapatinib	Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay	[PMID: 20143778]
SK-BR-3	IC₅₀	0.03 μM Compound: Lapatinib	Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell proliferation measured after 72 hrs by celltiter-glo assay Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell proliferation measured after 72 hrs by celltiter-glo assay	[PMID: 20571069]
SK-BR-3	IC₅₀	0.002 μM Compound: 5, GW-572016	Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay	[PMID: 21080629]
SK-BR-3	IC₅₀	4.35 μM Compound: 3	Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay	[PMID: 21570843]
SK-BR-3	IC₅₀	29 nM Compound: 1	Cytotoxicity against human SKBR3 cells overexpressing HER-2 gene after 72 hrs by SRB assay Cytotoxicity against human SKBR3 cells overexpressing HER-2 gene after 72 hrs by SRB assay	[PMID: 22372864]
SK-BR-3	IC₅₀	5.05 μM Compound: Lapatinib, Tykerb	Antiproliferative activity against human estrogen receptor and progesterone receptor deficient SKBR3 cells expressing HER2 after 72 hrs by MTT assay Antiproliferative activity against human estrogen receptor and progesterone receptor deficient SKBR3 cells expressing HER2 after 72 hrs by MTT assay	[PMID: 23927972]
SK-BR-3	IC₅₀	30.1 nM Compound: Lapatinib	Cytotoxicity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
SK-BR-3	IC₅₀	0.49 μM Compound: Lapatinib	Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay	[PMID: 27187856]
SK-BR-3	IC₅₀	0.06 μM Compound: 3; GW-572016	Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
SK-BR-3	IC₅₀	4.4 μM Compound: Lapatinib	Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay	[PMID: 28092860]
SK-BR-3	IC₅₀	9.76 μM Compound: Lapatinib	Antiproliferative activity against human SKBR3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human SKBR3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
SK-HEP1	IC₅₀	5.3 μM Compound: lapatinib	Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay	[PMID: 20143778]
SK-MEL19	GI₅₀	5 μM Compound: Lapatinib	Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SK-OV-3	IC₅₀	>10 μM Compound: Lapatinib	Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell proliferation measured after 72 hrs by celltiter-glo assay Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell proliferation measured after 72 hrs by celltiter-glo assay	[PMID: 20571069]
SK-OV-3	IC₅₀	0.003 μM Compound: 5, GW-572016	Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay	[PMID: 21080629]
SK-OV-3	IC₅₀	2.99 μM Compound: Lapatinib	Cytotoxicity against human SKOV3 cells overexpressing ErbB2 after 72 hrs by MTT assay Cytotoxicity against human SKOV3 cells overexpressing ErbB2 after 72 hrs by MTT assay	[PMID: 22182581]
SK-OV-3	IC₅₀	0.59 μM Compound: Lapatinib	Cytotoxicity against human SKOV3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human SKOV3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
SUM-159-PT	IC₅₀	9.76 μM Compound: Lapatinib	Antiproliferative activity against human SUM159 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human SUM159 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
SW480	IC₅₀	12.58 μM Compound: Lapatinib	Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 28711703]
SW480	IC₅₀	12.58 μM Compound: Lapatinib	Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 29421573]
SW480	IC₅₀	12.58 μM Compound: Lapatinib	Antiproliferative activity against human SW480 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human SW480 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
SW480	IC₅₀	12.58 μM Compound: Lapatinib	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay	[PMID: 32739648]
T-24	IC₅₀	9.65 μM Compound: 5, Tykerb	Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
T47D	IC₅₀	>10 μM Compound: Lapatinib, Tykerb	Antiproliferative activity against human HER2 deficient T47D cells expressing estrogen receptor and progesterone receptor after 72 hrs by MTT assay Antiproliferative activity against human HER2 deficient T47D cells expressing estrogen receptor and progesterone receptor after 72 hrs by MTT assay	[PMID: 23927972]
T47D	GI₅₀	40 μM Compound: Lapatinib	Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
TE-671	IC₅₀	10.95 μM Compound: 5, Tykerb	Cytotoxicity against human TE671 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human TE671 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
U-87MG ATCC	GI₅₀	10 μM Compound: Lapatinib	Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
Vero	IC₅₀	19.34 μM Compound: 40	Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell growth measured after 3 days by MTT assay Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell growth measured after 3 days by MTT assay	[PMID: 38908102]
WI-38	IC₅₀	>10 μM Compound: GW-572016	Cytotoxicity against human WI38 cells after 72 hrs by SRB assay Cytotoxicity against human WI38 cells after 72 hrs by SRB assay	[PMID: 19028425]
WI-38	IC₅₀	45.2 nM Compound: Lapatinib	Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 33545637]

In Vitro

Lapatinib (GW2016; 0.03-10 μM; 6 hours; BT474 and HN5 cells) treatment inhibits receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was inhibited by GW2016 in a dose-dependent manner^[1].
Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) treatment has a selective inhibition of the proliferation of human tumor cell lines^[1].
Lapatinib (GW2016; 1-10 μM; 72 hours; HN5 cells) treatment results in induces G1 arrest^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

BT474 and HN5 cells
Concentration:

0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM, or 10 µM
Incubation Time:

6 hours
Result:

Inhibited receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was also inhibited in a dose-dependent manner.

Cell Proliferation Assay^[1]

Cell Line:

HN5, A-43, BT474, N87, and CaLu-3 cells
Concentration:
Incubation Time:

72 hours
Result:

Inhibited the growth of tumor cells overexpressing EGFR or ErbB-2.

Cell Cycle Analysis^[1]

Cell Line:

HN5 cells
Concentration:

1 µM, or 10 µM
Incubation Time:

72 hours
Result:

Resulted in induction of G1 arrest.

In Vivo

Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) treatment inhibits tumor xenograft growth of the HN5 cells in a dose-responsive manner at 30 and 100 mg/kg, with complete inhibition of tumor growth at the higher dose^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

CD-1 nude female mice (4-6 weeks old) with HN5 cells^[1]
Dosage:

30 mg/kg, 100 mg/kg
Administration:

Oral administration; twice daily; for 21 days
Result:

Inhibited tumor xenograft growth of the HN5 cells in a dose-responsive manner.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 231277-92-2
Appearance Solid
Molecular Weight 581.06
Formula C₂₉H₂₆ClFN₄O₄S
Color Light yellow to yellow
SMILES

O=S(CCNCC1=CC=C(O1)C2=CC=C3C(C(NC4=CC(Cl)=C(OCC5=CC(F)=CC=C5)C=C4)=NC=N3)=C2)(C)=O
Synonyms

GW572016; GW2016
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (95)

All WB

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Journal Impact Factor

Nat Med

Combination inhibition of PI3K and mTORC1 yields durable remissions in mice bearing orthotopic patient-derived xenografts of HER2-positive breast cancer brain metastases. [Abstract]

2016 Jul;22(7):723-6. PMID: 27270588
Nature

CDK4/6 inhibition triggers anti-tumour immunity. [Abstract]

2017 Aug 24;548(7668):471-475. PMID: 28813415

Lapatinib purchased from MedChemExpress. Usage Cited in: Nature. 2017 Aug 24;548(7668):471-475. [Abstract]

Western blot of SKBR3, BT474, MDA-MB-453, and MDA-MB-361 cells treated with DMSO, Lapatinib, or Abemaciclib for 48 h. Western blot of MDA-MB-453 cells pretreated with DMSO or Abemaciclib (500 nM) for 0, 1, or 7 days before exposure to Staurosporine (500 nM) for 4 h.
Cancer Cell

A pan-KRAS inhibitor and its derived degrader elicit multifaceted anti-tumor efficacy in KRAS-driven cancers. [Abstract]

2025 Jul 25:S1535-6108(25)00310-1. PMID: 40780213
Nat Cancer

The MEK-RAF molecular glue IK-595 has potent antitumor activity across RAS/MAPK pathway-altered cancers. [Abstract]

2026 Jan;7(1):116-130. PMID: 41482524
Nat Immunol

Tumor-derived exosomes antagonize innate antiviral immunity. [Abstract]

2018 Mar;19(3):233-245. PMID: 29358709
Nat Commun

CNK2 promotes cancer cell motility by mediating ARF6 activation downstream of AXL signalling. [Abstract]

2023 Jun 15;14(1):3560. PMID: 37322019
Nat Commun

Nucleocytoplasmic transport of active HER2 causes fractional escape from the DCIS-like state. [Abstract]

2023 Apr 13;14(1):2110. PMID: 37055441
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Adv Sci (Weinh)

Osteoblast-Derived ECM1 Promotes Anti-Androgen Resistance in Bone Metastatic Prostate Cancer. [Abstract]

2024 Nov 20:e2407662. PMID: 39563492
Adv Sci (Weinh)

RNF126-Mediated MRE11 Ubiquitination Activates the DNA Damage Response and Confers Resistance of Triple-Negative Breast Cancer to Radiotherapy. [Abstract]

2023 Feb;10(5):e2203884. PMID: 36563124
Nat Chem Biol

Plasma membrane-associated ARAF condensates fuel RAS-related cancer drug resistance. [Abstract]

2025 Aug;21(8):1226-1237. PMID: 39870764
J Exp Clin Cancer Res

Dual inhibition of HERs and PD-1 counteract resistance in KRASG12C-mutant head and neck cancer. [Abstract]

2024 Nov 20;43(1):308. PMID: 39567998
J Exp Clin Cancer Res

ER-α36 mediates cisplatin resistance in breast cancer cells through EGFR/HER-2/ERK signaling pathway. [Abstract]

2018 Jun 25;37(1):123. PMID: 29940998

Lapatinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):123. [Abstract]

MCF-7 cells are treated with or without 5 μg/mL cisplatin (DDP) for 48 h after preincubated with or without Lapatinib at the indicated concentrations for 6 h, respectively. Then the levels of ER-α36, total EGFR and P-EGFR, total HER-2 and P-HER-2, total ERK and P-ERK are evaluated using western blot.
Redox Biol

Reactivation of MAPK-SOX2 pathway confers ferroptosis sensitivity in KRASG12C inhibitor resistant tumors. [Abstract]

2024 Nov 5:78:103419. PMID: 39527862
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 2:102053. PMID: 40187357
Pharmacol Res

Ceritinib inhibits growth and ACTH production of PitNETs: Insights from patient-derived organoids. [Abstract]

2025 Nov:221:107993. PMID: 41083089
Cancer Lett

Sideroflexin-1 promotes progression and sensitivity to lapatinib in triple-negative breast cancer by inhibiting TOLLIP-mediated autophagic degradation of CIP2A. [Abstract]

2024 Jun 5:217008. PMID: 38849012
Cancer Lett

Induction of EnR stress by Melatonin enhances the cytotoxic effect of Lapatinib in HER2-positive breast cancer. [Abstract]

2021 Oct 10:518:82-93. PMID: 34153400
Cancer Lett

Targeting ubiquitin conjugating enzyme UbcH5b by a triterpenoid PC3-15 from Schisandra plants sensitizes triple-negative breast cancer cells to lapatinib. [Abstract]

2021 Apr 28;504:125-136. PMID: 33607208
Cancer Lett

Targeting the EphB4 receptor tyrosine kinase sensitizes HER2-positive breast cancer cells to Lapatinib. [Abstract]

2020 Apr 10;475:53-64. PMID: 32006616
Int J Biol Sci

Promoter Hyper-methylation of ZNF662 Restrains its Tumor Suppressing Function in Triple-Negative Breast Cancer Through Regulating NGF Signaling Axis. [Abstract]

2025 Jun 12;21(9):4081-4097. PMID: 40612670
Cell Death Dis

Both direct and indirect suppression of MCL1 synergizes with BCLXL inhibition in preclinical models of gastric cancer. [Abstract]

2025 Mar 12;16(1):170. PMID: 40075071
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

2021 Jan;42(1):108-114. PMID: 32398685
NPJ Precis Oncol

High-throughput screening identifies NT-1 that synergizes with MRTX1133 against acquired resistant KRASG12D colorectal cancer. [Abstract]

2026 Apr 8;10(1):211. PMID: 41951768
Cell Syst

Receptor-Driven ERK Pulses Reconfigure MAPK Signaling and Enable Persistence of Drug-Adapted BRAF-Mutant Melanoma Cells. [Abstract]

2020 Nov 18;11(5):478-494.e9. PMID: 33113355
Oncogene

MUC1 triggers lineage plasticity of Her2 positive mammary tumors. [Abstract]

2022 May;41(22):3064-3078. PMID: 35461328
Oncogene

PIK3CA(H1047R)- and Her2-initiated mammary tumors escape PI3K dependency by compensatory activation of MEK-ERK signaling. [Abstract]

2016 Jun 9;35(23):2961-70. PMID: 26640141

Lapatinib purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70. [Abstract]

The combined use of MEK162 with HER kinase inhibitor Lapatinib, almost completely abolishes MAPK signaling as evidenced by diminished phospho-Erk levels. Western blot analyses of ERK signaling in tumor transplants from mice treated as indicated. Three hours after their dose on day four of treatment, the mice are sacrificed for analysis. Vinculin is used as a loading control.

Lapatinib purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70. [Abstract]

Western blot analysis of p-AKT(T308), p-AKT(S473) and p-ERK in transplanted NIC⁺PIK3CA^H1047R tumors treated as indicated. Transplants of NIC⁺PIK3CA^H1047R primary mammary tumors are first established in immunodeficient nude mice maintained on Doxycycline. Treatment starts when tumor transplants reach 500 mm³. DOX On, on Doxycycline; DOX Off, Doxycycline withdrawal. Lapatinib, 100mg/kg/day, p.o; GDC-0941, 120mg/kg/ day, p.o. Tumo
Cell Death Discov

Targeting the HECTD3-p62 axis increases the radiosensitivity of triple negative breast cancer cells. [Abstract]

2024 Nov 1;10(1):462. PMID: 39487119
Cell Rep

Structural basis for the reversal of human MRP4-mediated multidrug resistance by lapatinib. [Abstract]

2025 Mar 25;44(4):115466. PMID: 40138312
Br J Cancer

PCK1 regulates neuroendocrine differentiation in a positive feedback loop of LIF/ZBTB46 signalling in castration-resistant prostate cancer. [Abstract]

2022 Mar;126(5):778-790. PMID: 34815524
Clin Transl Med

Pyrotinib combined with CDK4/6 inhibitor in HER2-positive metastatic gastric cancer: A promising strategy from AVATAR mouse to patients. [Abstract]

2020 Aug;10(4):e148. PMID: 32898333
Cell Mol Life Sci

Loss of Kmt2c in vivo leads to EMT, mitochondrial dysfunction and improved response to lapatinib in breast cancer. [Abstract]

2023 Mar 18;80(4):100. PMID: 36933062
Front Immunol

Prognostic signatures of sphingolipids: Understanding the immune landscape and predictive role in immunotherapy response and outcomes of hepatocellular carcinoma. [Abstract]

2023 Mar 17:14:1153423. PMID: 37006285
Eur J Med Chem

Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy. [Abstract]

2019 Aug 15:176:393-409. PMID: 31125894
Mol Cancer Ther

Afatinib Is a New Therapeutic Approach in Chordoma with a Unique Ability to Target EGFR and Brachyury. [Abstract]

2018 Mar;17(3):603-613. PMID: 29237806

Lapatinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Mar;17(3):603-613. [Abstract]

Immunoblot analysis of U-CH1 cells treated with the indicated doses of inhibitors (Afatinib, Erlotinib and Lapatinib) for 2 h (upper panel) or 48 h (lower panel). Protein cell extracts are resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC₅₀s of the different inhibitors are reported.
Cells

Machine Learning-Driven Multi-Omics Analysis Identifies CHP2 as a Key PANoptosis-Related Dual-Function Biomarker in Colorectal Cancer. [Abstract]

2026 Feb 28;15(5):430. PMID: 41827864
Commun Biol

Proteolysis targeting chimera (PROTAC)-driven antibody internalization of oncogenic cell surface receptors. [Abstract]

2024 Dec 31;7(1):1719. PMID: 39741170
Life Sci

Qiliqiangxin alleviates Ang II-induced CMECs apoptosis by downregulating autophagy via the ErbB2-AKT-FoxO3a axis. [Abstract]

2021 May 15:273:119239. PMID: 33652033
Drug Des Devel Ther

Metabolic Stability Assessment of New PARP Inhibitor Talazoparib Using Validated LC-MS/MS Methodology: In silico Metabolic Vulnerability and Toxicity Studies. [Abstract]

2020 Feb 25;14:783-793. PMID: 32158196
Stem Cell Reports

Inhibition of Farnesyltransferase Potentiates NOTCH-Targeted Therapy against Glioblastoma Stem Cells. [Abstract]

2017 Dec 12;9(6):1948-1960. PMID: 29198824
Pharmaceuticals (Basel)

Synthesis and Development of 3-((2,4-Difluorophenyl)Amino)Propanoic Acid Derivatives as an Antiproliferative Medicinal Chemistry Scaffold Targeting Growth Factor Receptors. [Abstract]

2026 Feb 27;19(3):381. PMID: 41901229
Front Pharmacol

Influence of YES1 Kinase and Tyrosine Phosphorylation on the Activity of OCT1. [Abstract]

2021 Mar 8;12:644342. PMID: 33790797
RSC Adv

Validated liquid chromatography tandem mass spectrometry for simultaneous quantification of foretinib and lapatinib, and application to metabolic stability investigation. [Abstract]

2019 Jun 20;9(34):19325-19332. PMID: 35519400
Cell Rep Methods

Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. [Abstract]

2026 Jun 15;6(6):101339. PMID: 42134319
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Mol Pharm

Machine Learning Models Identify New Inhibitors for Human OATP1B1. [Abstract]

2022 Nov 7;19(11):4320-4332. PMID: 36269563
Cancers (Basel)

Liver X Receptor Ligand GAC0001E5 Downregulates Antioxidant Capacity and ERBB2/HER2 Expression in HER2-Positive Breast Cancer Cells. [Abstract]

2024 Apr 25;16(9):1651. PMID: 38730603
Cancers (Basel)

Drug Repurposing Applications to Overcome Male Predominance via Targeting G2/M Checkpoint in Human Esophageal Squamous Cell Carcinoma. [Abstract]

2022 Nov 28;14(23):5854. PMID: 36497337
Biol Proced Online

Trastuzumab-resistant breast cancer cells-derived tumor xenograft models exhibit distinct sensitivity to lapatinib treatment in vivo. [Abstract]

2023 Jun 27;25(1):19. PMID: 37370010
ACS Omega

Lapatinib Acts against Biofilm Formation and the Hemolytic Activity of Staphylococcus aureus. [Abstract]

2022 Mar 3;7(10):9004-9014. PMID: 35309438
Biochim Biophys Acta Mol Basis Dis

Additional statin treatment enhances the efficacy of HER2 blockade and improves prognosis in Rac1-high/HER2-positive breast cancer. [Abstract]

2024 Aug 9:167458. PMID: 39128642
iScience

FUS-dependent microRNA deregulations identify TRIB2 as a druggable target for ALS motor neurons. [Abstract]

2023 Oct 6;26(11):108152. PMID: 37920668
Transl Oncol

A novel treatment strategy of HER2-targeted therapy in combination with Everolimus for HR+/HER2- advanced breast cancer patients with HER2 mutations. [Abstract]

2022 Jul; 21: 101444. PMID: 35523006
Sci Rep

A degrader of HER2 and EGFR abolishes p95HER2 and shows robust antitumor efficacy in HER2-positive breast cancer. [Abstract]

2026 Apr 20;16(1):12890. PMID: 42009845
J Biol Chem

MAP3K4 promotes fetal and placental growth by controlling the receptor tyrosine kinases IGF1R/IR and Akt signaling pathway. [Abstract]

2022 Sep;298(9):102310. PMID: 35921893
ACS Chem Biol

Stable Colloidal Drug Aggregates Catch and Release Active Enzymes. [Abstract]

2016 Apr 15;11(4):992-1000. PMID: 26741163
J Proteome Res

An Integrative Proteome-Based Pharmacologic Characterization and Therapeutic Strategy Exploration of SAHA in Solid Malignancies. [Abstract]

2022 Apr 1;21(4):953-964. PMID: 35172096
Biotechnol Bioeng

An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]

2021 Dec;118(12):4687-4698. PMID: 34478150
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
Front Oncol

Discovery and Pharmacological Evaluation of STEAP4 as a Novel Target for HER2 Overexpressing Breast Cancer. [Abstract]

2021 Mar 26:11:608201. PMID: 33842315
Analyst

Assessment of coulometric array electrochemical detection coupled with HPLC-UV for the absolute quantitation of pharmaceuticals. [Abstract]

2017 Jan 26;142(3):525-536. PMID: 28098264
Cancer Med

Focal Adhesion Kinase Intersects With the BRD4-MYC Axis and YAP1 to Drive Tumor Cell Growth, Phenotypic Plasticity, Stemness, and Metastatic Potential in Colorectal Cancer. [Abstract]

2025 Sep;14(18):e71227. PMID: 40959971
Carcinogenesis

SNCA inhibits epithelial-mesenchymal transition and correlates to favorable prognosis of breast cancer. [Abstract]

2022 Dec 25;43(11):1071-1082. PMID: 36179220
Clin Chim Acta

Investigation of metabolic degradation of new ALK inhibitor: Entrectinib by LC-MS/MS. [Abstract]

2018 Oct:485:298-304. PMID: 30006284
J Chromatogr B Analyt Technol Biomed Life Sci

Simultaneous determination of 11 oral targeted antineoplastic drugs and 2 active metabolites by LC-MS/MS in human plasma and its application to therapeutic drug monitoring in cancer patients. [Abstract]

2024 Apr 15:1237:124100. PMID: 38547701
J Chromatogr B Analyt Technol Biomed Life Sci

UPLC-ESI-MS/MS study of the effect of green tea extract on the oral bioavailability of erlotinib and lapatinib in rats: Potential risk of pharmacokinetic interaction. [Abstract]

2017 Apr 1:1049-1050:30-40. PMID: 28260629
Separations

2023 May 26, 10(6), 330.
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
J Nanopart Res

2022; 24:261
PLoS One

Validated LC-MS/MS assay for quantification of the newly approved tyrosine kinase inhibitor, dacomitinib, and application to investigating its metabolic stability. [Abstract]

2019 Apr 4;14(4):e0214598. PMID: 30947315
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Gene

Pharmacotranscriptomic profiling of resistant triple-negative breast cancer cells treated with lapatinib and berberine shows upregulation of PI3K/Akt signaling under cytotoxic stress. [Abstract]

2022 Mar 30:816:146171. PMID: 35026293
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
Cancer Chemother Pharmacol

Lapatinib in combination with paclitaxel plays synergistic antitumor effects on esophageal squamous cancer. [Abstract]

2018 Sep;82(3):383-394. PMID: 29909520

Lapatinib purchased from MedChemExpress. Usage Cited in: Cancer Chemother Pharmacol. 2018 Sep;82(3):383-394. [Abstract]

The expression level of EGFR and HER2 on normal esophageal epithelium cell and four esophageal squamous cancer cell lines analyzed by western blot.
Biochem Biophys Res Commun

2026 Feb 12:800:153165. PMID: 41548485
Head Neck

Effect of HER2-targeted therapy on PDX and PDX-derived organoids generated from HER2-positive salivary duct carcinoma. [Abstract]

2023 Jul;45(7):1801-1811. PMID: 37184432
Cell Physiol Biochem

Lapatinib Induced Suicidal Death of Human Erythrocytes. [Abstract]

2015;37(6):2275-87. PMID: 26624928
Open Life Sci

Systemic investigation of inetetamab in combination with small molecules to treat HER2-overexpressing breast and gastric cancers. [Abstract]

2023 Jan 10;18(1):20220535. PMID: 36694697
chemRxiv

2026 Apr 6.
bioRxiv

2025 Nov 18.
SSRN

2025 Oct 13.
bioRxiv

2025 Sep 21.
bioRxiv

2025 May 09.
bioRxiv

PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]

2024 Nov 6:2024.11.04.621884. PMID: 39574568
Patent

US20240293405A1.
University of Gothenburg

2023 Jun 27.
Patent

US20220305013A1.
Biomedical Engineering Advances

June 2022, 100040.
bioRxiv

2021 Jan 9.
Oncotarget

MEK is a promising target in the basal subtype of bladder cancer. [Abstract]

2020 Nov 3;11(44):3921-3932. PMID: 33216841
Patent

US20200108066A1
bioRxiv

2019 Sep.
Personalized Medicine Universe

2019 May.
Oncotarget

A c-Jun N-terminal kinase inhibitor, JNK-IN-8, sensitizes triple negative breast cancer cells to lapatinib. [Abstract]

2017 Aug 24;8(62):104894-104912. PMID: 29285221

Lapatinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Aug 24;8(62):104894-104912. [Abstract]

MDA-MB-231 cells are serum-starved overnight and pre-treated with 3 μM Lapatinib or DMSO for 3 hours. After that time, cells are lysed (0hr) or stimulated with EGF for 1, 8, 24, 48, and 72 hours. Western blots of p-EGFR (Tyr1173), EGFR, p-cJun (ser63), cJun, and vinculin are shown with band densitometries beneath.
Tumour Biol

Addition of the p110α inhibitor BYL719 overcomes targeted therapy resistance in cells from Her2-positive-PTEN-loss breast cancer. [Abstract]

2016 Nov;37(11):14831-14839. PMID: 27639383

Lapatinib purchased from MedChemExpress. Usage Cited in: Tumour Biol. 2016 Nov;37(11):14831-14839. [Abstract]

Western blot analysis of PI3K signaling in cell lysates treated with Lapatinib (1 μM) with or without BYL719.

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (215.12 mM; ultrasonic and warming and heat to 06°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7210 mL

8.6050 mL

17.2099 mL

5 mM

0.3442 mL

1.7210 mL

3.4420 mL

10 mM

0.1721 mL

0.8605 mL

1.7210 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
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g
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μL
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
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%
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (396 KB)
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- Deutsch - DE (396 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94 [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7210 mL	8.6050 mL	17.2099 mL	43.0248 mL
	5 mM	0.3442 mL	1.7210 mL	3.4420 mL	8.6050 mL
	10 mM	0.1721 mL	0.8605 mL	1.7210 mL	4.3025 mL
	15 mM	0.1147 mL	0.5737 mL	1.1473 mL	2.8683 mL
	20 mM	0.0860 mL	0.4302 mL	0.8605 mL	2.1512 mL
	25 mM	0.0688 mL	0.3442 mL	0.6884 mL	1.7210 mL
	30 mM	0.0574 mL	0.2868 mL	0.5737 mL	1.4342 mL
	40 mM	0.0430 mL	0.2151 mL	0.4302 mL	1.0756 mL
	50 mM	0.0344 mL	0.1721 mL	0.3442 mL	0.8605 mL
	60 mM	0.0287 mL	0.1434 mL	0.2868 mL	0.7171 mL
	80 mM	0.0215 mL	0.1076 mL	0.2151 mL	0.5378 mL
	100 mM	0.0172 mL	0.0860 mL	0.1721 mL	0.4302 mL

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