Cat. No.: HY-10367

Canertinib

(Synonyms: CI-1033; PD-183805)

9 Cited Publications

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Based on 9 publication(s) in Google Scholar

Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC₅₀s of 7.4 and 9 nM. Canertinib is active against vaccinia virus respiratory infection in mice.

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Pureté: 99.74%
CAS No.: 267243-28-7
Formule: C₂₄H₂₅ClFN₅O₃
Masse moléculaire:485.94

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Canertinib Chemical Structure

CAS No.: 267243-28-7

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

Activité biologique

Description

IC₅₀ & Target^[1]

EGFR

7.4 nM (IC₅₀)

ErbB2

9 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	7.4 nM Compound: 18	Inhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immunoblotting Inhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immunoblotting	[PMID: 10753475]
A-431	IC₅₀	0.083 μg/mL Compound: 3 (CI-1033)	Inhibition of A431 cell proliferation Inhibition of A431 cell proliferation	[PMID: 12270171]
A-431	IC₅₀	0.15 μM Compound: CI-1033	Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTS assay Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTS assay	[PMID: 22339342]
A549	IC₅₀	1.59 μM Compound: CI-1033	Antiproliferative activity against human A549 cells expressing wild type EGFR coexpressing k-Ras mutant after 72 hrs by MTS assay Antiproliferative activity against human A549 cells expressing wild type EGFR coexpressing k-Ras mutant after 72 hrs by MTS assay	[PMID: 22339342]
A549	IC₅₀	6 nM Compound: 6; CI-1033	Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA	[PMID: 26756222]
A549	IC₅₀	7162 nM Compound: Canertinib	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 33773286]
BaF3	IC₅₀	0.029 μM Compound: Cl-1033	Inhibition of Blk expressed in mouse BAF3 cells assessed as cytotoxicity Inhibition of Blk expressed in mouse BAF3 cells assessed as cytotoxicity	[PMID: 18667312]
BaF3	IC₅₀	0.062 μM Compound: Cl-1033	Inhibition of Bmx expressed in mouse BAF3 cells assessed as cytotoxicity Inhibition of Bmx expressed in mouse BAF3 cells assessed as cytotoxicity	[PMID: 18667312]
BaF3	IC₅₀	2 μM Compound: Cl-1033	Inhibition of JAK3 expressed in mouse BAF3 cells assessed as cytotoxicity Inhibition of JAK3 expressed in mouse BAF3 cells assessed as cytotoxicity	[PMID: 18667312]
BaF3	IC₅₀	9.2 nM Compound: Canertinib	Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 33773286]
BJ	IC₅₀	5612 nM Compound: Canertinib	Cytotoxicity against human BJ cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Cytotoxicity against human BJ cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 33773286]
BT-474	EC₅₀	10 nM Compound: CI-1033	Antiproliferative activity against human BT474 cells overexpressing ERBb2 after 3 days by methylene blue staining Antiproliferative activity against human BT474 cells overexpressing ERBb2 after 3 days by methylene blue staining	[PMID: 19028424]
HCC827	IC₅₀	0.001 μM Compound: CI-1033	Antiproliferative activity against human HCC827 cells harboring EGFR del E746-A750 mutant after 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR del E746-A750 mutant after 72 hrs by MTS assay	[PMID: 22339342]
HCC827	IC₅₀	0.3776 nM Compound: Canertinib	Antiproliferative activity against human HCC827 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human HCC827 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 33773286]
HEK-293T	IC₅₀	6 μM Compound: Canertinib	Cytotoxicity against human HEK293T cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Cytotoxicity against human HEK293T cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 33773286]
HN5	EC₅₀	50 nM Compound: CI-1033	Antiproliferative activity against human HN5 cells overexpressing EGFR after 3 days by methylene blue staining Antiproliferative activity against human HN5 cells overexpressing EGFR after 3 days by methylene blue staining	[PMID: 19028424]
L02	IC₅₀	2.3 μM Compound: CI-1033	Antiproliferative activity against human HL7702 cells expressing wilt type EGFR after 72 hrs by MTS assay Antiproliferative activity against human HL7702 cells expressing wilt type EGFR after 72 hrs by MTS assay	[PMID: 22339342]
NCI-H1975	IC₅₀	0.064 μM Compound: CI-1033	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTS assay	[PMID: 22339342]
NCI-H1975	IC₅₀	3 nM Compound: 6; CI-1033	Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA	[PMID: 26756222]
NCI-H1975	IC₅₀	101 nM Compound: 35	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay	[PMID: 28754471]
NCI-H1975	IC₅₀	11.34 nM Compound: Canertinib	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 33773286]
PC-9	IC₅₀	0.8585 nM Compound: Canertinib	Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 33773286]
SK-BR-3	IC₅₀	0.102 μg/mL Compound: 3 (CI-1033)	Inhibition of SKBR-3 cell proliferation Inhibition of SKBR-3 cell proliferation	[PMID: 12270171]
SW-620	IC₅₀	1.45 μg/mL Compound: 3 (CI-1033)	Inhibition of SW-620 cell proliferation Inhibition of SW-620 cell proliferation	[PMID: 12270171]
Vero	CC₅₀	>10 μM Compound: 41; CI-1033	Cytotoxicity against african green monkey Vero cells Cytotoxicity against african green monkey Vero cells	[PMID: 33539089]

In Vitro

Canertinib significantly inhibits growth of cultured melanoma cells, RaH3 and RaH5, in a dose-dependent manner. IC₅₀ is approximately 0.8 μM and by 5μM both cell lines are completely growth-arrested within 72 h of treatment. Incubation of exponentially growing RaH3 and RaH5 with 1 μM canertinib accumulated the cells in the G1-phase of the cell cycle within 24 h of treatment without induction of apoptosis. 1 μM canertinib inhibits ErbB1-3 receptor phosphorylation with a concomitant decrease of Akt-, Erk1/2- and Stat3 activity in both cell lines^[2].
Canertinib also is a potent activator of exosome secretion^[3].

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

In Vivo

Canertinib shows superior in vivo antitumor activity, giving growth delays in A431 xenografts exceeding 50 days following oral administration^[1]. The growth of human malignant melanoma xenografts, RaH3 and RaH5, in nude mice is significantly inhibited by i.p. injections of 40 mg/kg/day canertinib (Fig. 4). The anti-proliferative effect on melanoma xenografts is visible already within 4 days of treatment and further increased throughout the treatment period as observed through the differences in tumor volumes, reaching statistical significance within 18 days of treatment^[2].

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 267243-28-7
Appearance Solid
Masse moléculaire 485.94
Formule C₂₄H₂₅ClFN₅O₃
Color Light yellow to yellow
SMILES

O=C(NC1=C(C=C2C(C(NC3=CC=C(C(Cl)=C3)F)=NC=N2)=C1)OCCCN4CCOCC4)C=C
Synonyms

CI-1033; PD-183805
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (9)

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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
J Med Chem

Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies. [Abstract]

2025 Aug 28;68(16):17917-17932. PMID: 40801664
Hepatol Int

SOX9 promotes hepatocyte proliferation via upregulating TGF-α expression during liver regeneration. [Abstract]

2025 Nov 3. PMID: 41182562
J Biol Chem

Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics. [Abstract]

2012 Mar 23;287(13):9742-52. PMID: 22223645
J Cell Sci

Crucial role of TRPC6 in maintaining the stability of HIF-1α in glioma cells under hypoxia. [Abstract]

2015 Sep 1;128(17):3317-29. PMID: 26187851
Biochemistry

Discovery of an Irreversible and Cell-Active BCL6 Inhibitor Selectively Targeting Cys53 Located at the Protein-Protein Interaction Interface. [Abstract]

2018 Feb 27;57(8):1369-1379. PMID: 29293322
Biochemistry

Universal and Quantitative Method To Evaluate Inhibitor Potency for Cysteinome Proteins Using a Nonspecific Activity-Based Protein Profiling Probe. [Abstract]

2017 Jun 13;56(23):2921-2927. PMID: 28520393
bioRxiv

Structural dynamics of the active HER4 and HER2/HER4 complexes is finely tuned by different growth factors and glycosylation. [Abstract]

2024 Jan 4:2023.10.06.561161. PMID: 38260342
Oncotarget

MEK is a promising target in the basal subtype of bladder cancer. [Abstract]

2020 Nov 3;11(44):3921-3932. PMID: 33216841

Solvant et solubilité

In Vitro:

Ethanol : 12.5 mg/mL (25.72 mM; Need ultrasonic)

DMSO : 4.9 mg/mL (10.08 mM; Need warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.0579 mL

10.2893 mL

20.5787 mL

5 mM

0.4116 mL

2.0579 mL

4.1157 mL

10 mM

0.2058 mL

1.0289 mL

2.0579 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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% EtOH 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.25 mg/mL (2.57 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (12.5 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% EtOH 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.25 mg/mL (2.57 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 1.25 mg/mL (2.57 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 EtOH stock solution (12.5 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]

Enzyme assays for IC₅₀ determinations are performed in 96-well filter plates. The total volume is 0.1 mL containing 20 mM Hepes, pH 7.4, 50 mM sodium vanadate, 40 mM magnesium chloride, 10 µM adenosine triphosphate (ATP) containing 0.5 mCi of [³²P]ATP, 20 mg of polyglutamic acid/tyrosine, 10 ng of EGFR tyrosine kinase, and appropriate dilutions of inhibitor (Canertinib). All components except the ATP are added to the well and the plate is incubated with shaking for 10 min at 25°C. The reaction is started by adding [³²P]ATP, and the plate is incubated at 25°C for 10 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid (TCA). The plate is kept at 4°C for at least 15 min to allow the substrate to precipitate. The wells is then washed five times with 0.2 mL of 10% TCA and ³²P incorporation determined with a plate counter^[1].

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

Cell Assay^[2]

RaH3 and RaH5 cells are treated with increasing concentrations (0-10 μM) of Canertinib for 72 h. The cells are suspended in buffer and counted^[2].

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

Animal Administration^[2]

Mice: Canertinib treatment starts when the tumors show reliable growth. The mice are randomized into control and treatment groups. In the canertinib treated RaH3 group (n=4) and RaH5 group (n=7) each mouse receives i.p. injections of 1.2 mg canertinib (40 mg/kg/day) in 0.1 ml 0.15 M NaCl 5 days a week. The control RaH3 (n=3) and RaH5 (n=7) mice receive i.p. injections of vehicle only according to the same regimen. At the end of the treatment period, the mice are sacrificed by cervical dislocation where after the tumors are removed and weighed^[2].

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 (282 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)
- 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]. Smaill JB, et al. Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. J Med Chem. 2000 Apr 6;43(7):1380-97. [Content Brief]

[2]. Djerf Severinsson EA, et al. The pan-ErbB receptor tyrosine kinase inhibitor canertinib promotes apoptosis of malignant melanoma in vitro and displays anti-tumor activity in vivo. Biochem Biophys Res Commun. 2011 Oct 28;414(3):563-8. [Content Brief]

[3]. McAndrews KM, et, al. Mechanisms associated with biogenesis of exosomes in cancer. Mol Cancer. 2019 Mar 30;18(1):52. [Content Brief]

[4]. Smee DF, et, al. Progress in the discovery of compounds inhibiting orthopoxviruses in animal models. Antivir Chem Chemother. 2008;19(3):115-24. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	2.0579 mL	10.2893 mL	20.5787 mL	51.4467 mL
	5 mM	0.4116 mL	2.0579 mL	4.1157 mL	10.2893 mL
	10 mM	0.2058 mL	1.0289 mL	2.0579 mL	5.1447 mL
Ethanol	15 mM	0.1372 mL	0.6860 mL	1.3719 mL	3.4298 mL
	20 mM	0.1029 mL	0.5145 mL	1.0289 mL	2.5723 mL
	25 mM	0.0823 mL	0.4116 mL	0.8231 mL	2.0579 mL

Keywords

Canertinib

9 Cited Publications

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Canertinib

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

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Human Metabolite Library

Anti-Prostate Cancer Compound Library

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Cancer Stem Cells Compound Library

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Publications Citing Use of MedChemExpress (MCE) Canertinib

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

Canertinib Related Classifications

Cat. No.: HY-10367