PD158780

  Cat. No.:  DC7842   Featured
Chemical Structure
171179-06-9
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More than 5000 active chemicals with high quality for research!
Field of application
PD158780 is a very potent inhibitor of EGFR with IC50 of 0.08 nM; pan-specific antagonist of ErbB receptor.
Cas No.: 171179-06-9
Chemical Name: PD 158780, PD-158780
Synonyms: PD 158780, PD-158780
SMILES: C1=NC(NC2=CC=CC(Br)=C2)=C2C=C(NC)N=CC2=N1
Formula: C14H12BrN5
M.Wt: 330.18
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: PD158780 is a potent EGFR family inhibitor with IC50s of 8 pM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, respectively.
In Vivo: 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[1].
In Vitro: 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[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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