Description
An inhibitor of EGFR (IC50 = 0.0007 µM for the intracellular kinase domain); selective for the EGFR intracellular kinase domain over the serine/threonine kinases PKC-α and Cdc2/cyclin B (IC50s = >100 and 78 µM, respectively), as well as FLK, c-Met, and Tek (IC50 = >1 µM for all), but does inhibit c-Src, c-Abl, VEGFR2/KDR, FLT1, and c-Kit (IC50s = 0.103, 0.028, 0.327, 0.962, and 2.21 µM, respectively); enhances the cytotoxicity of gemcitabine in L3.6pl cells; reduces tumor growth and metastasis and increases survival in an L3.6pl mouse xenograft model at 100 mg/kg per day with additive effects when administered in combination with gemcitabine; reduces tumor growth and inhibits angiogenesis in an SN12-PM6 human renal cell carcinoma mouse orthotopic model
Formal name: 4-[4-[[(1R)-1-phenylethyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-phenol
Synonyms:
Molecular weight: 330.4
CAS: 187724-61-4
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Death||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling
