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Canertinib

Catalog No. T6136 CAS 267243-28-7

Synonyms: PD-183805, CI-1033

Canertinib (CI-1033) is a pan-erbB tyrosine kinase inhibitor which work against esophageal squamous cell carcinoma in vitro and in vivo. Canertinib treatment significantly affects tumour metabolism, proliferation and hypoxia as determined by PET.

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Canertinib, CAS 267243-28-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 31.00
10 mg	In stock	$ 50.00
25 mg	In stock	$ 64.00
50 mg	In stock	$ 79.00
1 mL * 10 mM (in DMSO)	In stock	$ 33.00

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Purity: 100%

Purity: 99.18%

Purity: 99%

Purity: 98%

Biological Description

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Description	Canertinib (CI-1033) is a pan-erbB tyrosine kinase inhibitor which work against esophageal squamous cell carcinoma in vitro and in vivo. Canertinib treatment significantly affects tumour metabolism, proliferation and hypoxia as determined by PET.
Targets&IC50	EGFR:1.5 nM, ErbB2:9.0 nM
In vitro	CI-1033 shows excellent potency for irreversible inhibition of erbB2 autophosphorylation in MDA-MB 453 cells. CI-1033 also shows high permeability in Caco-2 cells and inhibits secretory transport of vinblastine, which indicates that CI-1033 is a likely inhibitor of the P-gp. [1] CI-1033 alone, significantly suppresses constitutively activated Akt and MAP kinase. In combination with gemcitabine, CI-1033 inhibits Akt and prevents increased levels of MAPK phosphorylation. CI-1033 stimulates p27 expression and p38 phosphorylation in MDA-MB-453 cells. [2] CI-1033 is highly specific to the erbB receptor family and not sensitive to PGFR, FGFR or IR even at 50 μM. CI-1033 shows high levels of inhibition in A431 cells expressing EGFR with IC50 of 7.4 nM. CI-1033 suppresses heregulin-stimulated tyrosine phosphorylation of erbB2, erbB3 and erbB4 with IC50 of 5, 14 and 10 nM, respectively. CI-1033 also inhibits expression of pp62c-fos in response to heregulin. [3] CI-1033 is predicted to modify Cys773 covalently within the ATP binding site of the HER2 kinase and enhances destruction of both mature and immature ErbB-2 molecules. [4] CI-1033 induces a significant decrease in measurable phosphorylation of tyrosine residues 845 and 1068 of EGFR, which are responsible for Src and Ras/MAPK signaling respectively. The corresponding residues of Her-2, tyrosine residues 877 and 1248 are dephosphorylated significantly by CI-1033 at a concentration of 3 μM or higher. CI could block EGFR internalization and increase the rate of apoptosis in primary osteosarcoma cells in a titratable fashion. [5] In addition, CI-1033 inhibits the proliferation of TT, TE2, TE6 and TE10 cells significantly at 0.1 nM. [6]
In vivo	CI-1033 shows impressive activity against A431 xenografts in nude mice at 5 mg/kg of body weight. [1] CI-1033 (20 to 80 mg/kg/d) achieves a high degree of tumor regressions in H125 xenograft models. [3] Oral administration of CI-1033 causes a marked inhibition of growth in TT, TE6 and TE10 xenografts in nude mice, without animal death and <10% weight loss. [6]
Kinase Assay	Tyrosine Kinase Assays: Enzyme assays for determination of IC50 are performed in 96-well filter plates in a total volume of 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 CI-1033. 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 another 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 are then washed five times with 0.2 mL of 10% TCA and 32P incorporation determined with a Wallac β plate counter.
Cell Research	Cells (1 × 104) are seeded in each well of a 24-well plastic culture plate and left overnight in DMEM or RPMI-1640 supplemented with 10% FBS. The next morning, the cells are treated with the indicated concentrations of CI-1033 (0.1-5.0 nM) for varying periods (1, 3, 5 and 7 days). After treatment, the cells are counted using a Coulter counter. The percent of cell proliferation is calculated by this formula: treatment cell number/control cell number × 100 for each time period.(Only for Reference)

Synonyms	PD-183805, CI-1033
Molecular Weight	485.94
Formula	C24H25ClFN5O3
CAS No.	267243-28-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.86 mg/mL (10 mM), Sonification is recommended

References and Literature

1. Smaill JB et al. J Med Chem. 2000; 43(7): 1380-1397. 2. Nelson JM et al. J Biol Chem. 2001; 276(18): 14842-14827. 3. Slichenmyer WJ et al. Semin Oncol. 2001; 28(5 Suppl 16): 80-85. 4. Citri A et al. EMBO J. 2002; 21(10): 2407-2417. 5. Hughes DP et al. Pediatr Blood Cancer. 2006; 46(5): 614-623.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Covalent Inhibitor Library Human Metabolite Library Bioactive Compounds Library Max

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Almonertinib mesylate PD153035 Neratinib maleate PP2 Patritumab NS309 EGFR/ErbB-2/ErbB-4 inhibitor-2 EGFR-IN-85

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Keywords

Canertinib 267243-28-7 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR ErbB-1 inhibit Inhibitor PD-183805 Epidermal growth factor receptor PD 183805 HER1 CI-1033 CI1033 Orthopoxvirus PD183805 CI 1033 inhibitor

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