GLPBio

Icotinib

Catalog No.: GC17982Purity:>98.00%Synonyms: BPI 2009H
COASDSData Sheet
Icotinib is an epidermal growth factor receptor (EGFR; IC₅₀=5nM) inhibitor that targets mutants such as EGFR (L858R, T790M, L861Q).

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Icotinib
Cas No.: 610798-31-7
10mM (in 1mL DMSO)In Stock
$108.00
1
1mgIn Stock
$56.00
1
5mgIn Stock
$98.00
1
10mgIn Stock
$147.00
1
50mgIn Stock
$406.00
1
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Description

Icotinib is an epidermal growth factor receptor (EGFR; IC₅₀=5nM) inhibitor that targets mutants such as EGFR (L858R, T790M, L861Q)[1-2]. Icotinib blocks tumor cell proliferation signals by inhibiting EGFR tyrosine kinase autophosphorylation and promotes tumor cell death through activation of apoptotic pathways, primarily utilized in non-small cell lung cancer research[3-4].

In vitro, Icotinib (2μM) was administered to PC-9/GR and H1975 non-small cell lung cancer cells for 4 weeks. Icotinib upregulated ATG7 expression via the STAT3/FOXM1 signaling pathway, inducing protective autophagy, thereby inhibiting Icotinib-induced apoptosis and enhancing drug resistance[5]. Treatment of A549 non-small cell lung cancer cells with Icotinib (0.01–10μM) for 24-72 hours, Icotinib exerted concentration-dependent inhibitory effects on cell proliferation, migration, and invasion. Icotinib suppressed the the epithelial-mesenchymal transition (EMT) process[6].

In vivo, Icotinib (50mg/kg) was orally administered to BALB/c nude mice bearing H1975 xenograft tumors (starting at a tumor volume of approximately 100mm³, three times per week for 5 weeks). Icotinib monotherapy only slightly reduced tumor volume, whereas its combination with Chidamide (12.5mg/kg or 25mg/kg) significantly suppressed tumor growth[7]. Icotinib (100mg/kg) was orally administered to BALB/c nude mice bearing PC9 xenograft tumors (starting on day 10 post-implantation, once daily for 18 days). Icotinib alone inhibited tumor growth, and a more pronounced antitumor effect was observed when combined with Thalidomide (200mg/kg)[8].

References:
[1] Tan F, Shen X, Wang D, et al. Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. Lung Cancer. 2012 May;76(2):177-82.
[2] Zhao Q, Cheng J, Chen P, et al. Icotinib: efficacy in different solid tumors and gene mutations. Anticancer Drugs. 2020 Mar;31(3):205-210.
[3] Guan YS, He Q, Li M. Icotinib: activity and clinical application in Chinese patients with lung cancer. Expert Opin Pharmacother. 2014 Apr;15(5):717-28.
[4] Li N, Ou W, Cheng C, et al. Adjuvant icotinib for resected EGFR-mutated stage II-IIIA non-small-cell lung cancer (ICTAN, GASTO1002): a randomized comparison study. Signal Transduct Target Ther. 2025 Aug 28;10(1):273.
[5] Lyu X, Zeng L, Shi J, et al. Essential role for STAT3/FOXM1/ATG7 signaling-dependent autophagy in resistance to Icotinib. J Exp Clin Cancer Res. 2022 Jun 11;41(1):200.
[6] Wang GH, Hu ZY. Icotinib inhibits proliferation and epithelial-mesenchymal transition of non-small cell lung cancer A549 cells. Math Biosci Eng. 2019 Aug 21;16(6):7707-7718.
[7] Zhang N, Liang C, Song W, et al. Antitumor activity of histone deacetylase inhibitor chidamide alone or in combination with epidermal growth factor receptor tyrosine kinase inhibitor icotinib in NSCLC. J Cancer. 2019 Jan 29;10(5):1275-1287.
[8] Sun X, Xu Y, Wang Y, et al. Synergistic Inhibition of Thalidomide and Icotinib on Human Non-Small Cell Lung Carcinomas Through ERK and AKT Signaling. Med Sci Monit. 2018 May 15;24:3193-3203.

Protocol

Cell experiment [1]:

Cell lines

A549 cells (human non-small cell lung cancer cell line)

Preparation Method

A549 cells were maintained in RPMI 1640 medium supplemented with 10% fetal bovine serum (FBS), 100U/mL penicillin, and 100μg/mL streptomycin at 37°C, 5% CO₂. A549 cells were treated with Icotinib at concentrations of 0.01–10μM for 24–72 hours.

Reaction Conditions

0.01–10μM; 24–72 hours

Applications

Icotinib significantly inhibited A549 cell proliferation in a concentration- and time-dependent manner, with the highest inhibition rate observed at 10μM after 72 hours. Icotinib induced apoptosis in A549 cells, as evidenced by increased apoptosis rates at concentrations of 0.01–10μM after 48 hours. Icotinib suppressed epithelial-mesenchymal transition (EMT) by upregulating E-cadherin expression and downregulating N-cadherin, Vimentin, and fibronectin levels. Additionally, Icotinib reduced A549 cell migration and invasion abilities in Transwell assays.
Animal experiment [2]:

Animal models

BALB/c nude mice

Preparation Method

Mice were subcutaneously injected with 5×10⁶ PC9 cells and randomized into treatment groups. Mice received daily oral administration of thalidomide (200mg/kg), Icotinib (100mg/kg), or their combination for 18 days. Tumor volumes were measured periodically, and tissues were harvested for analysis.

Dosage form

100mg/kg; p.o.; Daily for 18 days.

Applications

Icotinib monotherapy suppressed tumor growth in PC9 xenograft models, while combination with thalidomide synergistically enhanced antitumor efficacy, significantly reducing tumor volume and Ki-67 proliferation index, and increasing TUNEL-positive apoptotic cells.

References:
[1] Wang GH, Hu ZY. Icotinib inhibits proliferation and epithelial-mesenchymal transition of non-small cell lung cancer A549 cells. Math Biosci Eng. 2019 Aug 21;16(6):7707-7718.
[2] Sun X, Xu Y, Wang Y, et al. Synergistic Inhibition of Thalidomide and Icotinib on Human Non-Small Cell Lung Carcinomas Through ERK and AKT Signaling. Med Sci Monit. 2018 May 15;24:3193-3203.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
610798-31-7
Synonyms
BPI 2009H
Chemical Name
N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine
SMILES
[H]C1=C2OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC2=C([H])C3=NC([H])=NC(N([H])C4=C([H])C([H])=C([H])C(C#C[H])=C4[H])=C31
Molecular Formula
C22H21N3O4
Molecular Weight
391.42
Solubility
≥ 129.6mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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