Icotinib

Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFRL858R, EGFRL858R/T790M, EGFRT790M and EGFRL861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[610798-31-7]

Product Name Alternative

BPI-2009

UNSPSC

12352005

Hazard Statement

H302

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/icotinib.html

Concentration

10mM

Purity

99.96

Solubility

DMSO : ≥ 155 mg/mL

Smiles

C#CC1=CC(NC2=C(C=C(OCCOCCOCCO3)C3=C4)C4=NC=N2)=CC=C1

Molecular Formula

C22H21N3O4

Molecular Weight

391.42

Precautions

H302

References & Citations

[1]Tan F, et al. Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. Lung Cancer. 2012 May;76 (2) :177-82.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C, 3 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

EGFR/ErbB1/HER1

Citation 01

Breast Cancer Res Treat. 2025 Jun;211 (2) :467-478.|Cell Rep Med. 2023 Feb 21;4 (2) :100911.|Clin Chim Acta. 2022 Feb 15:527:1-10.|Eur J Pharmacol. 2019 May 5:850:141-149.|J Pharm Biomed Anal. 2023 May 10:228:115275.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Biochem Pharmacol. 2016 Dec 1:121:67-77.|Mol Syst Biol. 2024 Jan;20 (1) :28-55.|Science. 2017 Dec 1;358 (6367) :eaan4368.