Home Protein Tyrosine Kinase EGFR inhibitor Icotinib (BPI-2009H)

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Icotinib (BPI-2009H) EGFR inhibitor

Cat.No.S2922

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

Chemical Structure

Molecular Weight: 391.42

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Quality Control

Batch: Purity: 99.96%
99.96

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (199.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 391.42 Formula

 

C22H21N3O4
 Storage (From the date of receipt)
CAS No. 610798-31-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C#CC1=CC(=CC=C1)NC2=NC=NC3=CC4=C(C=C32)OCCOCCOCCO4

Mechanism of Action

Targets/IC50/Ki
EGFR
5 nM
In vitro
Icotinib (BPI-2009H) inhibits EGFR activity in a dose-dependent manner, with an IC50 value of 5 nM and complete inhibition at 62.5 nM. It selectively solely inhibits the EGFR members including the wild type and mutants with inhibition efficacies of 61-99%. This compound 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. It exhibits a broad spectrum of antitumor activity and is especially effective against tumors expressing higher levels of EGFR.
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 (BPI-2009H) 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.
In vivo
Icotinib (BPI-2009H) shows an antitumor effect in different types of xenografts. At a dose of 120 mg/kg, it inhibits tumor growth at a rate of 51.5%, 31.0% and 67.4% in the A431, A549 and H460 xenografts, respectively.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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