PD 158780 is a potent in vitro inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) (IC50 0.08 nM), and other members of the erbB family, by competitive binding at the ATP site of these signal transduction enzymes.
CAS Number: 171179-06-9
Molecular Weight: 330.18
Chemical Name: 4-N-(3-bromophenyl)-6-N-methylpyrido[3,4-d]pyrimidine-4,6-diamine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
PD158780 inhibits EGF receptor autophosphorylation in A431 human epidermoid carcinoma with IC50 value of 13 nM. PD158780 is highly specific for the EGF receptor in Swiss 3T3 fibroblasts, inhibiting EGF-dependent receptor autophosphorylation and thymidine incorporation at low nanomolar concentrations while requiring micromolar levels for platelet-derived growth factor- and basic fibroblast growth factordependent processes. PD158780 inhibits heregulin-stimulated phosphorylation in the SK-BR-3 and MDAMB-453 breast carcinomas with IC50 values of 49 and 52 nM, respectively, suggesting that the compound is active against other members of the EGF receptor family.
PD158780 is active against clone formation in several breast tumors having different expression patterns of the ErbB family. PD158780 shows good therapeutic effect against the A431 epidermoid carcinoma when administered either intraperitoneally or orally. PD158780 produces measurable, significant effects against a mouse fibroblast transfected with human EGFR. PD158780 produces a significant therapeutic effect against the estrogendependent MCF-7 breast carcinoma at equitoxic dose levels.
- Rewcastle GW, Murray DK, Elliott WL, Fry DW, Howard CT, Nelson JM, Roberts BJ, Vincent PW, Showalter HD, Winters RT, Denny WA. 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. PubMed PMID: 9513602.
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