Icotinib

Catalog No.S2922 Synonyms: BPI-2009H

Icotinib Chemical Structure

Molecular Weight(MW): 391.42

Icotinib 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).

Size Price Stock Quantity  
In DMSO USD 420 In stock
USD 270 In stock
USD 370 In stock
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1 Customer Review

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

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Biological Activity

Description Icotinib 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).
Targets
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]

Protocol

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
  • Formulation: 0.5% CMC-Na
  • 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)
Ethanol 7 mg/mL (17.88 mM)
Water slightly soluble or insoluble
In vivo Add solvents individually and in order:
0.5% CMC
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
Formula

 

C22H21N3O4
CAS No. 610798-31-7
Storage powder
in solvent
Synonyms BPI-2009H

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02961270 Recruiting Non-small Cell Lung Cancer Chinese Academy of Medical Sciences November 2016 Phase 2
NCT02960607 Recruiting Carcinoma, Non-Small-Cell Lung Chinese Academy of Medical Sciences November 2016 Phase 2
NCT02934256 Recruiting Vestibular Schwannoma|Neurofibromatosis Type 2 Li Peng|Betta Pharmaceuticals Co.,Ltd.|Beijing Tiantan Hospital July 2016 Phase 2
NCT02801435 Recruiting Psoriasis Betta Pharmaceuticals Co.,Ltd.|Tigermed Consulting Co., Ltd July 2016 Phase 1
NCT02883543 Active, not recruiting Non-small Cell Lung Cancer Daping Hospital and the Research Institute of Surgery of the Third Military Medical University June 2016 Phase 3
NCT02820116 Recruiting Non-small Cell Lung Cancer(NSCLC) Beijing Haidian Hospital|Peking University Peoples Hospital|307 Hospital of PLA|309th Hospital of Chinese Peoples Liberation Army May 2016 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID