WHI-P180

Description: WHI-P180 (also known as Janex 3) is a multi-kinase inhibitor which inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 uM, respectively. WHI-P180 is an active inhibitor of IgE-mediated mast cell responses in vitro and in vivo. Further preclinical characterization of WHI-P180 may improve the efficacy of WHI-P180 in vivo and provide the basis for design of effective treatment and prevention programs for mast cell mediated allergic reactions. The elimination half-life of WHI-P180 in CD-1 mice (BALB/ c mice) following i.v., i.p., or p.o. administration was less than 10 min. Systemic clearance of WHI-P180 was 6742 mL/h/kg in CD-I mice and 8188 mL/h/kg in BALB/c mice. Notably, WHI-P180, when administered in two consecutive nontoxic i.p. bolus doses of 25 mg/kg, inhibited IgE/antigen-induced vascular hyperpermeability in a well-characterized murine model of passive cutaneous anaphylaxis.

References: Pharm Res. 1999 Jan; 16(1):117-22; Acta Crystallogr C. 2001 Jan; 57(Pt 1):76-8.

Related CAS#:153437-55-9 (HCl salt)