Icotinib (BPI-2009H) - Moligand™, 10mM in DMSO , Epidermal growth factor receptor erbB1 inhibitor, CAS No.610798-31-7, Epidermal growth factor receptor erbB1 inhibitor

CAS: 610798-31-7 Cat. No.: I408103 Molecular Weight: 391.42

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

[1,4,7,10]Tetraoxacyclododecino[2,3-g]quinazolin-4-amine, N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Icotinib (BPI-2009H) is a potent and specificEGFRinhibitor withIC50of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).
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.

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.
Cell Data

cell lines：primary human CLL cells,T cells, NK cells, and epithelial cells

Concentrations：~25 μM

Incubation Time：96 h

Powder Purity:≥99%

Specifications

Synonyms

[1, 4, 7, 10]Tetraoxacyclododecino[2, 3-g]quinazolin-4-amine, N-(3-ethynylphenyl)-7, 8, 10, 11, 13, 14-hexahydro-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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).

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Epidermal growth factor receptor erbB1 inhibitor

Product Properties

• ALogP: 3.1

Names and Identifiers

• Isomeric SMILES: C#CC1=CC(=CC=C1)NC2=NC=NC3=CC4=C(C=C32)OCCOCCOCCO4
• Molecular Weight: 391.42
• Reaxy-Rn: 12989052
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12989052&ln=

Associated Targets(Human)

EGFR Tclin Epidermal growth factor receptor (3 Activities)

Discover Target: EGFR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CARS Tchem Cysteine--tRNA ligase, cytoplasmic (1 Activities)

Discover Target: CARS

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 0.4 mg/mL (1.55 mM); Water: Insoluble; Ethanol: Insoluble

References

1. Xinying Ni, Hong Wang, Wenwen Chen, Xiao Meng, Mengping Zhang, Hua Shao, Fang Zhang, Cuijuan Wang.  (2026)  Field-ready detection of antineoplastic drugs in workplaces using a wearable flexible surface-enhanced Raman spectroscopy platform.  SENSORS AND ACTUATORS B-CHEMICAL,      [PMID:] [10.1016/j.snb.2026.139447]