Molecular Formula | C17H13BrN4O |
Molar Mass | 369.22 |
Melting Point | 279℃ |
Appearance | powder |
Color | white to beige |
Storage Condition | room temp |
In vitro study | PD 168393 connected to the ATP binding pocket of EGFR TK. PD168393 continued treatment of A431 cells completely inhibited EGF-dependent receptor autophosphorylation. PD168393 acts on MDA-MB-453 cells and inhibits Heregulin-induced tyrosine phosphorylation with an IC50 of 5.7 nM. PD168393 inhibits the activities of insulin, PDGFR, FGFR TKs and PKC. PD168393 acts on HS-27 human fibroblasts and inhibits EGF-regulated tyrosine phosphorylation with an IC50 of 1-6 nM, but has little effect on FGF or PDGF-regulated tyrosine phosphorylation. PD168393 acted on 3T3-Her2 cells and rapidly and effectively inhibited tyrosine phosphorylation induced by Her2, with an IC50 of ~ 100 nM. PD168393 acts on 3T3-Her2 cells and also inhibits the phosphorylation of PLCγ1/Stat1/Dok1/δ-catenin, except for Fyb. |
In vivo study | PD 168393 treatment of nude mice bearing A431 human epithelial carcinoma xenografts inhibited tumor growth by 115% and decreased the phosphotyrosine content of EGFR by 50%. PD 168393 also decreased plasma concentrations. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.708 ml | 13.542 ml | 27.084 ml |
5 mM | 0.542 ml | 2.708 ml | 5.417 ml |
10 mM | 0.271 ml | 1.354 ml | 2.708 ml |
5 mM | 0.054 ml | 0.271 ml | 0.542 ml |
biological activity | PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM and irreversible alkylation of Cys-773, PDGFR, FGFR and PKC activity. PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM and irreversible alkylation of Cys-773; It inhibits the activities of insulin, PDGFR, FGFR and PKC. |
characteristics | was used to design a clinical compound of CI-1033. |
Target | Value |
EGFR () | 0.70 nM |