1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Anti-infection
  2. EGFR Orthopoxvirus
  3. Canertinib dihydrochloride

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

製品番号: HY-10367A 純度: 99.68%
COA 取扱説明書 Technical Support

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

Canertinib (dihydrochloride) 構造式

CAS 番号 : 289499-45-2

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 47 在庫あり
Solution
10 mM * 1 mL in DMSO USD 47 在庫あり
Solid
5 mg $38 在庫あり
10 mg $60 在庫あり
50 mg $85 在庫あり
100 mg $120 在庫あり
500 mg $480 在庫あり
1 g   お問い合わせ  
5 g   お問い合わせ  

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カスタマーレビュー

Based on 9 publication(s) in Google Scholar

Other Forms of Canertinib dihydrochloride:

Top Publications Citing Use of Products

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製品説明

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[1][2][3][4].

IC50 & Target[1]

EGFR

7.4 nM (IC50)

ErbB2

9 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
NIH3T3 IC50
1.7 1
Compound: 9
Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells
Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells
[PMID: 16480284]
Sf9 IC50
0.002 3
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]
A-431 IC50
7.4 1
Compound: 5, CI-1033
Inhibition of EGF-stimulated autophosphorylation of EGFR in A431 cells
Inhibition of EGF-stimulated autophosphorylation of EGFR in A431 cells
[PMID: 11462982]
Sf9 IC50
0.011 3
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]
A-431 IC50
7.4 1
Compound: 5, CI-1033
Inhibition of EGF-stimulated autophosphorylation of EGFR in A431 cells
Inhibition of EGF-stimulated autophosphorylation of EGFR in A431 cells
[PMID: 11462982]
MDA-MB-453 IC50
7.4 1
Compound: 9
Inhibition of HER stimulated human erbB autophosphorylation in MDA-MB-453 cells
Inhibition of HER stimulated human erbB autophosphorylation in MDA-MB-453 cells
[PMID: 16480284]
Sf9 IC50
0.027 3
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]
A-431 IC50
7.4 1
Compound: 5, CI-1033
Inhibition of autophosphorylation of EGFR in A431 cells
Inhibition of autophosphorylation of EGFR in A431 cells
[PMID: 11462982]
T-24 IC50
16 1
Compound: 9
Inhibition of ligand stimulated erbB2 autophosphorylation in T24 NIH cells
Inhibition of ligand stimulated erbB2 autophosphorylation in T24 NIH cells
[PMID: 16480284]
T-24 IC50
0.016 3
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]
Sf9 IC50
0.002 3
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 3
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 3
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 3
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]
MDA-MB-453 IC50
7.4 1
Compound: 9
Inhibition of HER stimulated human erbB autophosphorylation in MDA-MB-453 cells
Inhibition of HER stimulated human erbB autophosphorylation in MDA-MB-453 cells
[PMID: 16480284]
NIH3T3 IC50
1.7 1
Compound: 9
Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells
Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells
[PMID: 16480284]
Sf9 IC50
0.002 3
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 3
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 3
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 3
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]
T-24 IC50
16 1
Compound: 9
Inhibition of ligand stimulated erbB2 autophosphorylation in T24 NIH cells
Inhibition of ligand stimulated erbB2 autophosphorylation in T24 NIH cells
[PMID: 16480284]
体外実験

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.

体内実験

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.

分子量

558.86

分子式

C24H27Cl3FN5O3

CAS 番号
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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

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

溶剤 & 溶解度
体外: 

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 : 16.67 mg/mL (29.83 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

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一般には略語で表示されます:C1V1 = C2V2

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体内:

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.

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:

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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).
純度とドキュメンテーション

純度: 99.68%

参考文献
キナーゼ実験
[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) はこれらの方法の精度を確認していません。 こちらは参照専用です。

細胞実験
[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) はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[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) はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

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.

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
DMSO 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
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.

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

一般には略語で表示されます:C1V1 = C2V2

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× = ×
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製品名:
Canertinib dihydrochloride
製品番号:
HY-10367A
数量:
MCE 日本正規代理店: