Icotinib

Catalog No.S2922

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).

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Icotinib Chemical Structure

Icotinib Chemical Structure
Molecular Weight: 391.42

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Icotinib is available in the following compound libraries:

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Product Information

  • Compare EGFR Inhibitors
    Compare EGFR Products
  • Research Area
  • Inhibition Profile

Product Description

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]
IC50 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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 Assay: [1]

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.

Animal Study: [1]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Tan F, et al. Lung Cancer, 2012, 76(2), 177-182.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02801435 Not yet recruiting Psoriasis Betta Pharmaceuticals Co.,Ltd.|Tigermed Consulting Co., Ltd July 2016 Phase 1
NCT02737774 Not yet recruiting Lung Adenocarcinoma Henan Cancer Hospital April 2016 Phase 2
NCT02744664 Not yet recruiting Lung Neoplasms Fuda Cancer Hospital, Guangzhou April 2016 Phase 4
NCT02726568 Recruiting Non-small Cell Lung Cancer|Brain Metastases Betta Pharmaceuticals Co.,Ltd. March 2016 Phase 2
NCT02574091 Recruiting Psoriasis Betta Pharmaceuticals Co.,Ltd.|Quintiles, Inc. October 2015 Phase 1

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Chemical Information

Download Icotinib SDF
Molecular Weight (MW) 391.42
Formula

 

C22H21N3O4
CAS No. 610798-31-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms BPI-2009H
Solubility (25°C) * In vitro DMSO 78 mg/mL (199.27 mM)
Ethanol 7 mg/mL (17.88 mM)
Water <1 mg/mL (<1 mM)
In vivo 0.5% CMC 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name [1,4,7,10]Tetraoxacyclododecino[2,3-g]quinazolin-4-amine, N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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