Icotinib hydrochloride salt form · hydrochloride · Parent Icotinib hydrochloride

Icotinib Hydrochloride is a potent, CNS-penetrant and specific EGFR inhibitor.

For research use only. Not for human or veterinary use.

Target EGFR

Research area Infection Neurological Disease Metabolic Disease Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Icotinib hydrochloride structure

CAS No.: 1204313-51-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 480.00	BP-01851A-250mg	In stock	Get quote
500 mg	USD 880.00	BP-01851A-500mg	In stock	Get quote
1 g	USD 1,380.00	BP-01851A-1g	In stock	Get quote
5 g	Inquire	BP-01851A-5g	Inquire	Inquire

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Description

Icotinib Hydrochloride (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Biological activity

In Vitro Incubation with Iconitib at 0.5 μM results in kinase activity inhibition of 91%, 99%, 96%, 61% and 61%, respectively. Iconitib inhibits the proliferation of A431 and BGC-823 A549, H460 and KB cell lines with IC50s of 1, 4.06, 12.16, 16.08, 40.71 μM. When profiled with 88 kinases, Icotinib only shows meaningful inhibitory activity to EGFR and its mutants. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation (IC50=45 nM) in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation. In Vivo Icotinib exhibits potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug is well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment. Icotinib inhibits tumor growth at a rate of 25.2%, 45.6% and 51.5% in the A431 cell line groups; 3.4%, 25.9% and 31.0% in the A549 cell line groups; 49.4%, 52.6% and 67.4% in the H460 cell line groups, and 30.3%, 36.4% and 46.5% in the HCT8 cell line groups, at 30, 60 and 120 mg/kg/dose, respectively.

Identifiers

SMILES: Cl.C#CC1=CC(NC2=NC=NC3=CC4=C(OCCOCCOCCO4)C=C23)=CC=C1
InChIKey: PNNGXMJMUUJHAV-UHFFFAOYSA-N

Specifications

MW (average): 427.8810
Formula: C₂₂H₂₂ClN₃O₄
CAS No.: 1204313-51-8
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4°C, sealed storage, away from moisture

Solubility

Soluble in DMSO

Documents

References

[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.

[2]. Zhao X, et al. Efficacy of icotinib versus traditional chemotherapy as first-line treatment for preventing brain metastasis from advanced lung adenocarcinoma in patients with epidermal growth factor receptor-sensitive mutation. J Cancer Res Ther. 2016 Jul-Sep;12(3):1127-1131.

Same target

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Same research area

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