产品描述

WHI-P180是多种激酶的抑制剂，对RET和KDR的IC50值分别为4.5 nM和66 nM。

靶点（IC50 & Targe）

CDK2

EGFR

体内研究

The elimination half-life of WHI-P180 in CD-1 mice (BALB/ c mice) following i.v., i.p., or p.o. administration is less than 10 min. Systemic clearance of WHI-P180 is 6742 mL/h/kg in CD-1 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[2].

参考文献

[1] Rebecca Newton, et al. Eur J Med Chem. 2016, 112: 20-32.

[2] Newton R, et al. Eur J Med Chem. 2016, 112:20-32.