Cat. No.: HY-15164A

Icotinib

(Synonyms: BPI-2009)

9 Cited Publications

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Based on 9 publication(s) in Google Scholar

Icotinib (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 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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Pureté: 99.92%
CAS No.: 610798-31-7
Formule: C₂₂H₂₁N₃O₄
Masse moléculaire:391.42

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Icotinib Chemical Structure

CAS No.: 610798-31-7

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

EGFR

5 nM (IC₅₀)

EGFR^L858R

EGFR^L858R/T790M

EGFR^T790M

EGFR^L861Q

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	45 nM Compound: 12k	Inhibition of EGFR-mediated intracellular tyrosine phosphorylation in EGF-stimulated human A431 cells after 2.5 hrs by SDS-PAGE analysis Inhibition of EGFR-mediated intracellular tyrosine phosphorylation in EGF-stimulated human A431 cells after 2.5 hrs by SDS-PAGE analysis	[PMID: 22959248]
KYSE-410	IC₅₀	>19.16 μM Compound: Icotinib	Antiproliferative activity against drug-sensitive human KYSE-410 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against drug-sensitive human KYSE-410 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36893627]
KYSE-450	IC₅₀	>19.16 μM Compound: Icotinib	Antiproliferative activity against drug-sensitive human KYSE-450 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against drug-sensitive human KYSE-450 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36893627]
KYSE-70 cell line	IC₅₀	>19.16 μM Compound: Icotinib	Antiproliferative activity against drug-sensitive human KYSE-70 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against drug-sensitive human KYSE-70 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36893627]
NCI-H1650	IC₅₀	>19.16 μM Compound: Icotinib	Antiproliferative activity against drug-sensitive human NCI-H1650 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against drug-sensitive human NCI-H1650 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36893627]
NCI-H1975	IC₅₀	>19.16 μM Compound: Icotinib	Antiproliferative activity against drug-sensitive human NCI-H1975 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against drug-sensitive human NCI-H1975 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36893627]

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 610798-31-7
Appearance Solid
Masse moléculaire 391.42
Formule C₂₂H₂₁N₃O₄
Color White to off-white
SMILES

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

BPI-2009
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (9)

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Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Cell Rep Med

Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]

2023 Feb 21;4(2):100911. PMID: 36657446
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
Biochem Pharmacol

Allosteric activation of midazolam CYP3A5 hydroxylase activity by icotinib - Enhancement by ketoconazole. [Abstract]

2016 Dec 1:121:67-77. PMID: 27666601
Eur J Pharmacol

20(S)-ginsenoside Rg3 sensitizes human non-small cell lung cancer cells to icotinib through inhibition of autophagy. [Abstract]

2019 May 5:850:141-149. PMID: 30772396

Icotinib purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2019 May 5:850:141-149. [Abstract]

Immunoblotting for LC3 and p62 using lysates from cells treated with 1 μM icotinib in the presence or absence of CQ for 24 h.

Icotinib purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2019 May 5:850:141-149. [Abstract]

LC3 II levels are evaluated by immunoblotting using lysates from cells treated with 1 μM icotinib (parental cells) or 20 μM icotinib (resistant cells) for 24 h.
Clin Chim Acta

Simultaneous quantitative detection of afatinib, erlotinib, gefitinib, icotinib, osimertinib and their metabolites in plasma samples of patients with non-small cell lung cancer using liquid chromatography-tandem mass spectrometry. [Abstract]

2022 Feb 15:527:1-10. PMID: 34999058
J Pharm Biomed Anal

Simultaneous online SPE-HPLC-MS/MS quantification of gefitinib, osimertinib and icotinib in dried plasma spots: Application to therapeutic drug monitoring in patients with non-small cell lung cancer. [Abstract]

2023 May 10:228:115275. PMID: 36871365
Breast Cancer Res Treat

IGF1R activates FOXP3-β-catenin signaling to promote breast cancer development. [Abstract]

2025 Jun;211(2):467-478. PMID: 40055251

Solvant et solubilité

In Vitro:

DMSO : ≥ 155 mg/mL (395.99 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5548 mL

12.7740 mL

25.5480 mL

5 mM

0.5110 mL

2.5548 mL

5.1096 mL

10 mM

0.2555 mL

1.2774 mL

2.5548 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Kinase Assay^[1]

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 μCi³²P-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 detect radioactivity. Quantification is performed by software^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

Cells (1000/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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice: The effect of three doses of Icotinib (30, 60, and 120 mg/kg/dose p.o. qd) on antitumor activity and survival is determined in mice bearing A431, A549, H460 and HCT8 tumor xenografts. Taxol (30 mg/kg/dose i.p. once a week) is employed in these experiments as a positive control group^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5548 mL	12.7740 mL	25.5480 mL	63.8700 mL
	5 mM	0.5110 mL	2.5548 mL	5.1096 mL	12.7740 mL
	10 mM	0.2555 mL	1.2774 mL	2.5548 mL	6.3870 mL
	15 mM	0.1703 mL	0.8516 mL	1.7032 mL	4.2580 mL
	20 mM	0.1277 mL	0.6387 mL	1.2774 mL	3.1935 mL
	25 mM	0.1022 mL	0.5110 mL	1.0219 mL	2.5548 mL
	30 mM	0.0852 mL	0.4258 mL	0.8516 mL	2.1290 mL
	40 mM	0.0639 mL	0.3194 mL	0.6387 mL	1.5968 mL
	50 mM	0.0511 mL	0.2555 mL	0.5110 mL	1.2774 mL
	60 mM	0.0426 mL	0.2129 mL	0.4258 mL	1.0645 mL
	80 mM	0.0319 mL	0.1597 mL	0.3194 mL	0.7984 mL
	100 mM	0.0255 mL	0.1277 mL	0.2555 mL	0.6387 mL

Keywords

Icotinib

9 Cited Publications

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Icotinib

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Publications Citing Use of MedChemExpress (MCE) Icotinib

Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Publications (9)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Icotinib Related Classifications

HY-15164A Related Classifications