Icotinib表皮生长因子受体（EGFR；IC50=5nM）抑制剂，可抑制EGFR（L858R，T790M，L861Q）等突变体。
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.
Icotinib表皮生长因子受体（EGFR；IC50=5nM）抑制剂，可抑制EGFR（L858R，T790M，L861Q）等突变体[1-2]。Icotinib可抑制EGFR酪氨酸激酶的自磷酸化来阻断肿瘤细胞增殖信号，同时通过激活凋亡通路以促进肿瘤细胞死亡，主要被用于非小细胞癌的相关研究[3-4]。
在体外，Icotinib（2μM）处理PC-9/GR和H1975非小细胞肺癌细胞4周，Icotinib通过STAT3/FOXM1信号通路上调ATG7表达，诱导保护性自噬，从而抑制Icotinib引发的细胞凋亡并增强耐药性[5]。Icotinib（0.01–10μM）处理A549非小细胞肺癌细胞24-72小时，Icotinib以浓度依赖性方式抑制细胞增殖与迁移侵袭能力，同时阻断上皮-间质转化（EMT）进程[6]。
在体内，Icotinib（50mg/kg）口服给药处理荷瘤（H1975细胞）BALB/c裸鼠（从肿瘤体积约100mm³开始，每周三次，持续5周），Icotinib单药治疗仅导致肿瘤体积轻微减小，而与Chidamide（12.5mg/kg或25mg/kg）联合使用时，则显著抑制肿瘤生长[7]。Icotinib（100mg/kg）口服给药处理荷瘤（PC9细胞）BALB/c裸鼠（从接种细胞后第10天开始，每日一次，持续18天），Icotinib单药治疗可抑制肿瘤生长，与Thalidomide（200mg/kg）联合使用时有更好的抑制肿瘤效果[8]。
| 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: | |
| Cas No. | 610798-31-7 | SDF | |
| 别名 | 埃克替尼; BPI-2009 | ||
| 化学名 | 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 | ||
| 分子式 | C22H21N3O4 | 分子量 | 391.42 |
| 溶解度 | ≥ 129.6mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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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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