ZD 4190

ZD 4190 is an inhibitor of VEGFR1, VEGFR2, and EGFR (IC₅₀s = 0.7, 0.03, and 0.4 µM, respectively).^1,2 It is selective for these kinases over PDGFRβ, FGFR1, and HER2 (IC₅₀s = 3.4, >100, and >100 µM, respectively) and MEK, cyclin-dependent kinase 2 (Cdk2), insulin-like growth factor 1 receptor (IGF-1R), Akt, and tunica interna endothelial cell kinase 2 (Tie2; IC₅₀s = >10, >10, >20, >20, and >100 µM, respectively). ZD 4190 selectively inhibits VEGF- or EGF-induced proliferation of HUVECs over FGF-induced proliferation of HUVECs (IC₅₀s = 0.05, 0.05, and 1.5 µM, respectively). In vivo, ZD 4190 (100 mg/kg) reduces tumor volume in a Calu-6 non-small cell lung cancer (NSCLC) mouse xenograft model.¹ It inhibits training-induced increases in collateral blood flow and white gastrocnemius muscle capillarity in exercise-trained rats.³

WARNING This product is not for human or veterinary use.

1. Hennequin, L.F., Thomas, A.P., Johnstone, C., et al. Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors. J. Med. Chem. 42(26), 5369-5389 (1999).

2. Hennequin, L.F., Stokes, E.S.E., Thomas, A.P., et al. Novel 4-anilinoquinazolines with C-7 basic side chains: Design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors. J. Med. Chem. 45(6), 1300-1312 (2002).

3. Lloyd, P.G., Prior, B.M., Li, H., et al. VEGF receptor antagonism blocks arteriogenesis, but only partially inhibits angiogenesis, in skeletal muscle of exercise-trained rats. Am. J. Physiol. Heart Circ. Physiol. 288(2), H759-H768 (2005).