Vatalanib Dihydrochloride (N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine Dihydrochlorid

Vatalanib is a potent, selective, orally active inhibitor of the VEGFR tyrosine kinases VEGFR-1 (Flt-1, IC50=77nM) and VEGFR-2 (FLK-1/KDR, IC50=37nM), with slightly higher potency against the latter. At higher concentrations, other tyrosine kinases are also inhibited, including PDGFR-b (IC50=580nM), c-KIT (IC50=730nM), FLT-4 (IC50=660nM) and c-FMS (IC50=1.4uM). On the other hand, vatalanib is not active against the EGFR, c-SRC, v-ABL, and protein kinase Ca (IC50 > 10uM). Solubility: Soluble in DMSO at 10-20mg/ml with warming, very poorly soluble in ethanol, soluble in water at 100 mg/ml, buffers, serum, or other additives may increase or decrease the aqueous solubility. Storage and Stability: May be stored at RT for short-term only. Long-term storage is recommended at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.