Icotinib (Synonyms: BPI 2009H) |
Catalog No.GC17982
One-Click Copy Product Info
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Icotinib is an epidermal growth factor receptor (EGFR; IC₅₀=5nM) inhibitor that targets mutants such as EGFR (L858R, T790M, L861Q).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 610798-31-7
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
A549 cells (human non-small cell lung cancer cell line) |
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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. |
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Reaction Conditions |
0.01–10μM; 24–72 hours |
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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]: | |
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Animal models |
BALB/c nude mice |
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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. |
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Dosage form |
100mg/kg; p.o.; Daily for 18 days. |
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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. |
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References: |
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| Cas No. | 610798-31-7 | SDF | |
| 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 | ||
| Canonical 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 | ||
| Formula | C22H21N3O4 | M.Wt | 391.42 |
| Solubility | ≥ 129.6mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5548 mL | 12.774 mL | 25.548 mL |
| 5 mM | 511 μL | 2.5548 mL | 5.1096 mL |
| 10 mM | 255.5 μL | 1.2774 mL | 2.5548 mL |
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Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)