Pelitinib (CAS 257933-82-7)

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Alternativa namn: EKB 569

Ansökan Pelitinib is an EGFR inhibitor

Momsregistreringsnummer :: 257933-82-7

Purity: 98%

Molecular Weight: 467.92

Molecular Formula: C₂₄H₂₃ClFN₅O₂

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

* Refer to Certificate of Analysis for lot specific data (including water content).

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SDS & Certificate of Analysis

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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.

Konferenser

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).

LAGRING :

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 :

n²⁰_D 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 :

pK_a: 12.24 (Predicted), pK_b: 8.01 (Predicted)

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

PubChem CID :

6445562

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

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Certificate of Analysis

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