Canertinib dihydrochloride (Synonyms: CI-1033 dihydrochloride; PD-183805 dihydrochloride)

Name: Canertinib dihydrochloride
Brand: MedChemExpress
SKU: HY-10367A
Rating: 5.0 (9 reviews)

Cat. No.: HY-10367A Purity: 99.68%: FAQs
Data Sheet SDS COA Handling Instructions

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

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Canertinib dihydrochloride Chemical Structure

CAS No. : 289499-45-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 38	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 85	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Canertinib dihydrochloride:

Canertinib In-stock

9 Publications Citing Use of MCE Canertinib dihydrochloride

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

EGFR

7.4 nM (IC₅₀)

ErbB2

9 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	0.002 μM Compound: 4	Irreversible inhibition of GST-tagged ERBB1 (unknown origin) (Met-668 to Ala-1211 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA Irreversible inhibition of GST-tagged ERBB1 (unknown origin) (Met-668 to Ala-1211 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA	[PMID: 27491023]
Sf9	IC₅₀	0.011 μM Compound: 4	Irreversible inhibition of GST-tagged ERBB2 (unknown origin) (Ile-675 to Val-1256 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA Irreversible inhibition of GST-tagged ERBB2 (unknown origin) (Ile-675 to Val-1256 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA	[PMID: 27491023]
Sf9	IC₅₀	0.027 μM Compound: 4	Irreversible inhibition of GST-tagged ERBB4 (unknown origin) (Gly-259 to Gly-690 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA Irreversible inhibition of GST-tagged ERBB4 (unknown origin) (Gly-259 to Gly-690 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA	[PMID: 27491023]
T-24	IC₅₀	0.016 μM Compound: 4	Irreversible inhibition of ERBB2 (unknown origin) autophosphorylation transfected in EGF-stimulated mouse T24 NIH/3T3 cells with extracellular binding domain of ERBB1 incubated for 2 hrs followed by stimulation with EGF for 10 mins Irreversible inhibition of ERBB2 (unknown origin) autophosphorylation transfected in EGF-stimulated mouse T24 NIH/3T3 cells with extracellular binding domain of ERBB1 incubated for 2 hrs followed by stimulation with EGF for 10 mins	[PMID: 27491023]

In Vitro

Canertinib dihydrochloride (CI-1033 dihydrochloride) 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 dihydrochloride 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 dihydrochloride (CI-1033 dihydrochloride) 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.

Clinical Trial

Molecular Weight

558.86

Formula

C₂₄H₂₇Cl₃FN₅O₃

CAS No.

289499-45-2

Appearance

Solid

Color

Light yellow to green yellow

SMILES

C=CC(NC1=CC2=C(N=CN=C2C=C1OCCCN3CCOCC3)NC4=CC=C(C(Cl)=C4)F)=O.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (111.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 25 mg/mL (44.73 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7894 mL	8.9468 mL	17.8936 mL
5 mM	0.3579 mL	1.7894 mL	3.5787 mL
10 mM	0.1789 mL	0.8947 mL	1.7894 mL

View the Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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: ≥ 2.08 mg/mL (3.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.08 mg/mL (3.72 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 10 mg/mL (17.89 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.68%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (254 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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]. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.7894 mL	8.9468 mL	17.8936 mL	44.7339 mL
	5 mM	0.3579 mL	1.7894 mL	3.5787 mL	8.9468 mL
	10 mM	0.1789 mL	0.8947 mL	1.7894 mL	4.4734 mL
	15 mM	0.1193 mL	0.5965 mL	1.1929 mL	2.9823 mL
	20 mM	0.0895 mL	0.4473 mL	0.8947 mL	2.2367 mL
	25 mM	0.0716 mL	0.3579 mL	0.7157 mL	1.7894 mL
	30 mM	0.0596 mL	0.2982 mL	0.5965 mL	1.4911 mL
	40 mM	0.0447 mL	0.2237 mL	0.4473 mL	1.1183 mL
DMSO	50 mM	0.0358 mL	0.1789 mL	0.3579 mL	0.8947 mL
	60 mM	0.0298 mL	0.1491 mL	0.2982 mL	0.7456 mL
	80 mM	0.0224 mL	0.1118 mL	0.2237 mL	0.5592 mL
	100 mM	0.0179 mL	0.0895 mL	0.1789 mL	0.4473 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Canertinib dihydrochloride Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Canertinib289499-45-2CI-1033PD-183805CI1033CI 1033PD183805PD 183805EGFROrthopoxvirusEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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Canertinib dihydrochloride (Synonyms: CI-1033 dihydrochloride; PD-183805 dihydrochloride)

Customer Review

Other Forms of Canertinib dihydrochloride:

Canertinib dihydrochloride Related Antibodies

9 Publications Citing Use of MCE Canertinib dihydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Canertinib dihydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Canertinib dihydrochloride Related Classifications

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