PD158780

• CAT Number: I002233
• CAS Number: 171179-06-9
• Molecular Formula: C14H12BrN5
• Molecular Weight: 330.2
• Purity: ≥95%
• Synonyms: N4-(3-bromophenyl)-N6-methylpyrido[3,4-d]pyrimidine-4,6-diamine
• Target: EGFR
• Solubility: 10 mM in DMSO
• Storage: Store at -20C
• IC50: 0.08 nM [1]
• InChI: InChI=1S/C14H12BrN5/c1-16-13-6-11-12(7-17-13)18-8-19-14(11)20-10-4-2-3-9(15)5-10/h2-8H,1H3,(H,16,17)(H,18,19,20)
• InChIKey: KFHMLBXBRCITHF-UHFFFAOYSA-N
• SMILES: BrC1=CC=CC(NC2=NC=NC3=C2C=C(NC)N=C3)=C1

PD158780 (Cat.No:I002233) is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR) kinase. It has been studied for its potential in targeting EGFR-dependent cancers, particularly non-small cell lung cancer. PD158780 shows promise in preclinical studies as an anticancer agent and is actively being researched for its therapeutic applications.

Reference

[1]. Rewcastle GW, et al. Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors. J Med Chem. 1998 Feb 26;41(5):742-51.
[2]. Cunnick JM, et al. Role of tyrosine kinase activity of epidermal growth factor receptor in the lysophosphatidic acid-stimulated mitogen-activated protein kinase pathway. J Biol Chem. 1998 Jun 5;273(23):14468-75.
[3]. Fisahn A, et al. Neuregulin-1 modulates hippocampal gamma oscillations: implications for schizophrenia. Cereb Cortex. 2009 Mar;19(3):612-8.