Home Protein Tyrosine Kinase EGFR inhibitor Icotinib (BPI-2009H) For research use only.

Icotinib (BPI-2009H)

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).

Icotinib (BPI-2009H) Chemical Structure

Icotinib (BPI-2009H) Chemical Structure

CAS: 610798-31-7

Selleck's Icotinib (BPI-2009H) has been cited by 8 Publications

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Purity & Quality Control

Batch: Purity: 100%
100

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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).
Targets
EGFR [1]
5 nM
In vitro
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]
Kinase Assay 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 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.
In Vivo
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]
Animal Research Animal Models A431, A549, H460 and HCT8 xenografts Nude mice
Dosages 30, 60 and 120 mg/kg/day
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02883543 Unknown status 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 Non-small-cell Lung Cancer Betta Pharmaceuticals Co. Ltd. April 2013 Phase 2

Chemical lnformation & Solubility

Molecular Weight 391.42 Formula

 

C22H21N3O4
CAS No. 610798-31-7 SDF Download Icotinib (BPI-2009H) SDF
Smiles C#CC1=CC(=CC=C1)NC2=NC=NC3=CC4=C(C=C32)OCCOCCOCCO4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 78 mg/mL ( (199.27 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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