CanertinibAn irreversible pan-erbB tyrosine kinase inhibitor

Canertinib (CAS 267243-28-7)

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Application: An irreversible pan-erbB tyrosine kinase inhibitor
CAS Number: 267243-28-7
Purity: ≥99%
Molecular Weight: 485.94
Molecular Formula: C24H25ClFN5O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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Canertinib is a potent and selective inhibitor of tyrosine residue phosphorylation of EGFR, blocking signal transgression and ceasing angiogenisis. Canertinib displays an IC50 = 1.5nM. Additionally, Canertinib's action in inhibiting EGFR increases apoptosis in cancerous cell lines in a titratable fashion.


References

Li, D., et al.: Oncogene, 27, 4702 (2008), Brown, A., et al.: Toxicol. Pathol., 36, 410 (2008), Chen, H., et al.: Chem. Biol. Drug Design, 71, 434 (2008),

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (2 mg/ml), methanol, ethanol (9 mg/ml), and water (<1 mg/ml).
Storage :
Store at room temperature
Melting Point :
175-180° C
Boiling Point :
~691° C at 760 mmHg (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.65 (Predicted)
IC50 :
EGFR: IC50 = 1.5 nM; ErbB2: IC50 = 9.0 nM
pK Values :
pKa: 12.09 (Predicted), pKb: 6.99 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
156414
Merck Index :
14: 1744
MDL Number :
MFCD09837878
SMILES :
C=CC(=O)Nc1cc2c(ncnc2cc1OCCCN1CCOCC1)Nc1ccc(F)c(Cl)c1

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Certificate of Analysis

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Canertinib  Product Citations

See how others have used Canertinib. Click on the entry to view the PubMed entry .

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PMID: # 30462579  Paatero, I.|Veikkolainen, V.|Mäenpää, M.|Schmelzer, E.|Belting, HG.|Pelliniemi, LJ.|Elenius, K.| et al. 2019. Mol. Biol. Cell. 30: 209-218.

Citations 1 to 1 of 1 total
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