PD-184161

• CAT Number: R051791
• CAS Number: 212631-67-9
• Molecular Formula: C17H13BrClF2IN2O2
• Molecular Weight: 557.558
• Purity: ≥95%
• Target: MEK1/2
• Solubility: Soluble in DMSO
• Storage: Store at -20°C
• IUPAC Name: 5-bromo-2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide
• InChI: InChI=1S/C17H13BrClF2IN2O2/c18-11-6-10(17(25)24-26-7-8-1-2-8)16(15(21)14(11)20)23-13-4-3-9(22)5-12(13)19/h3-6,8,23H,1-2,7H2,(H,24,25)
• InChIKey: VJNZMSLGVUSPCF-UHFFFAOYSA-N
• SMILES: C1CC1CONC(=O)C2=CC(=C(C(=C2NC3=C(C=C(C=C3)I)Cl)F)F)Br

PD184161 is an orally-active MEK inhibitor. PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner more effectively than PD098059 or U0126. PD184161 inhibited cell proliferation and induced apoptosis at concentrations of > or = 1.0 microM in a time- and concentration-dependent manner. PD184161 has antitumor effects in HCC in vitro and in vivo that appear to correlate with suppression of MEK activity. PD184161 is unable to suppress MEK activity in HCC xenografts in the long term.

Reference

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