Icotinib (BPI-2009H)

For research use only.

Catalog No.S2922

4 publications

Icotinib (BPI-2009H) Chemical Structure

CAS No. 610798-31-7

Icotinib (BPI-2009H) is a potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).

Selleck's Icotinib (BPI-2009H) has been cited by 4 publications

2 Customer Reviews

  • B. Effect of Icotinib treatment on the subcellular localization of ABCG2 in NCI-H460/MX20 cell. ABCG2 staining is shown in green. DAPI (blue) counterstains the nuclei. C. Effect of Icotinib on the ATPase activity of ABCG2: The BeFx-sensitive specific ATPase activity of ABCG2 was determined in the presence of 0-5 μM of Icotinib as described in supplemental methods. The activity in the absence of Icotinib (basal activity) was considered to be 100%, and % -fold stimulation ± S.D. (Y-axis) was plotted as a function of indicated concentrations of Icotinib (X-axis). D. Effect of Icotinib on the photolabeling of ABCG2 with [125I]-IAAP: Crude membranes from ABCG2 expressing MCF7-FLV1000 cells were photo-crosslinked with [125I]-IAAP in the presence and absence of 0-50 μM of Icotinib as described in supplemental methods. [125I]-IAAP incorporated in ABCG2 band was quantified using ImageQuant software and plotted as % [125I]-IAAP incorporated ± S.D. (Y-axis) as a function of varying concentration of Icotinib (X-axis). The upper panel shows a representative autoradiogram from three independent experiments and the arrow represents the ABCG2 band photo-crosslinked with [125I]-IAAP.

    Oncotarget, 2015, 5(12):4529-42.. Icotinib (BPI-2009H) purchased from Selleck.

    Icotinib reduced PD-L1 protein expression in H1975 cells. Cells were either left untreated or treated with Icotinib (1 μM or 0.1 μM) for 24 h. Cells were collected and PD-L1 expression was determined by western blotting. GAPDH was used as an internal control.

    Oncogene, 2017, 36(45):6235-6243. Icotinib (BPI-2009H) purchased from Selleck.

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Choose Selective EGFR Inhibitors

Biological Activity

Description Icotinib (BPI-2009H) is a potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).
EGFR [1]
5 nM
In vitro

Icotinib inhibits EGFR activity in a dose-dependent manner, with an IC50 value of 5 nM and complete inhibition at 62.5 nM. Icotinib selectively solely inhibits the EGFR members including the wild type and mutants with inhibition efficacies of 61-99%. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation in human epidermoid carcinoma A431 cells in a dose-dependent manner. Meanwhile, in our proliferation assay performed on A431, BGC-823, A549, H460, HCT8, KB and Bel-7402 cell lines, we found that the relative sensitivity of cell lines to Icotinib is A431 > BGC-823 > A549 > H460 > KB > HCT8 and Bel-7402. Icotinib exhibits a broad spectrum of antitumor activity and it is especially effective against tumors expressing higher levels of EGFR. [1]

In vivo Icotinib shows an antitumor effect in different types of xenografts. Icotinib inhibits tumor growth at a rate of 51.5%, 31.0% and 67.4% in the A431, A549 and H460 xenografts at a dose of 120 mg/kg, respectively. [1]


Kinase Assay:[1]
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Biochemical kinase assays:

In the in vitro kinase assays, 2.4 ng/μL EGFR protein is mixed with 32 ng/μL Crk in 25 μL kinase reaction buffer containing 1 μM cold ATP and 1 μCi 32P-γ-ATP. The mix is incubated with Icotinib at 0, 0.5, 2.5, 12.5 or 62.5 nM on ice for 10 min followed by incubation at 30 °C for 20 min. After quenching with SDS sample buffer at 100 °C for 4 min, the protein mix is resolved by electrophoresis in a 10% SDS-PAGE gel. The dried gel is then exposed to the PhosphorImager to detect radioactivity. Quantification is performed by ImageQuant software. In this methodology the radioactive signal inversely correlates with kinase activity.
Cell Research:[1]
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  • Cell lines: A431, BGC-823, A549, H460, HCT8, KB and Bel-7402 cells.
  • Concentrations: ~25 μM
  • Incubation Time: 96 h
  • Method: Cells (103 /well) are seeded into 96-well plates in RPMI-1640 medium containing 10% FBS and grown in a 5% CO2 incubator at 37 °C. After 24 h, cells are treated with Icotinib at 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 μM for 96 h. Cell proliferation is calculated by subtracting the mean absorbance value on day 0 from the mean absorbance value on day 4.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: A431, A549, H460 and HCT8 xenografts Nude mice
  • Dosages: 30, 60 and 120 mg/kg/day
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (199.27 mM)
Water Insoluble
Ethanol '7 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% CMC
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 391.42


CAS No. 610798-31-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02883543 Unknown status Drug: icotinib|Drug: Chemotherapy|Radiation: Radiotherapy Non-small Cell Lung Cancer Daping Hospital and the Research Institute of Surgery of the Third Military Medical University June 2016 Phase 3
NCT01843647 Unknown status Drug: Icotinib|Drug: Chemotherapy Non-small-cell Lung Cancer Betta Pharmaceuticals Co. Ltd. April 2013 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID