Pelitinib (CAS 257933-82-7)
Alternate Names:
EKB 569
Application:
Pelitinib is an EGFR inhibitor
CAS Number:
257933-82-7
Purity:
98%
Molecular Weight:
467.92
Molecular Formula:
C24H23ClFN5O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Pelitinib is a tyrosine kinase inhibitor that covalently binds to EGFR, inhibiting receptor phosphorylation and thus inhibiting signal transduction from EGFR. This induces apoptosis and thus leads to suppression of growth in tumor cell lines.
References
Veronese, M., et al.: Br. J. Cancer, 92, 1846 (2005), Hofheinz, R., et al.: Onkologie, 29, 563 (2006), Meyerhardt, J., et al.: J. Clin. Oncol., 24, 1892 (2006), Hanauske, A., et al.: Clin. Cancer Res., 13, 523 (2007).
Physical State
:
Solid
Solubility
:
Soluble in DMSO (13 mg/ml at 25° C), methanol, water (<1 mg/ml at 25° C), and ethanol (<1 mg/ml at 25° C).
Storage
:
Store at -20° C
Melting Point
:
188-190° C
Boiling Point
:
~655.5° C at 760 mmHg (Predicted)
Density
:
~1.3 g/cm3 (Predicted)
Refractive Index
:
n20D 1.65 (Predicted)
IC50
:
EGFR : IC50 = 38.5 nM; proliferation of normal human keratinocytes: IC50 = 61 nM; proliferation of A431 tumor cells: IC50 = 125 nM; proliferation ofMDA-468 tumor cells: IC50 = 260 nM
pK Values
:
pKa: 12.24 (Predicted), pKb: 8.01 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID
:
MDL Number
:
MFCD09837868
SMILES
:
CCOC1=C(NC(=O)\\C=C\\CN(C)C)C=C2C(=C1)N=CC(C#N)=C2NC1=CC(Cl)=C(F)C=C1
Download SDS (MSDS)
Certificate of Analysis
Adobe Acrobat Reader is required to reliably view,
print and comment on PDF documents