Molecular Weight(MW): 369.22
PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC.
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|Description||PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC.|
|Features||Preclinical compound used in the design of CI-1033.|
PD 168393 is docked into the ATP binding pocket of EGFR TK. PD168393 completely suppresses EGF-dependent receptor autophosphorylation in A431 cells during continuous exposure, with continous suppression even after 8 hr in compound-free medium. PD168393 inhibits heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC50 of 5.7 nM. PD168393 is inactive against insulin, PDGF and basic FGFR TKs as well as PKC. PD168393 inhibits EGF-mediated tyrosine phosphorylation in HS-27 human fibroblasts with IC50 of 1-6 nM but has little effect on FGF- or PDGF-mediated tyrosine phosphorylation.  PD168393 shows rapid and potent inhibition of Her2-induced tyrosine phosphorylation with IC50 of ~100 nM in 3T3-Her2 cells. D168393 also inhibits phosphorylation of PLCγ1/Stat1/Dok1/δ-catenin in 3T3-Her2 cells, except for Fyb. 
|In vivo||PD 168393 produces tumor growth inhibition of 115% in A431 human epidermoid carcinoma xenograft in nude mice, with 50% reduced phosphotyrosine content of EGFR. PD 168393 also shows a low plasma concentration. |
|In vitro||DMSO||74 mg/mL (200.42 mM)|
|In vivo||30% PEG400+0.5% Tween80+5% propylene glycol||10 mg/mL|
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