Vatalanib, Dihydrochloride Salt **

产品名称：Vatalanib, Dihydrochloride Salt
产品货号：LC  V-8303
产品规格：1 G
Vatalanib is a potent, selective, orally active inhibitor of the VEGFR tyrosine kinases VEGFR-1 (Flt-1, IC50 = 77 nM) and VEGFR-2 (FLK-1/KDR, IC50 = 37 nM), with slightly higher potency against the latter.  At higher concentrations, other tyrosine kinases are also inhibited, including PDGFR-β (IC50 = 580 nM), c-KIT (IC50 = 730 nM), FLT-4 (IC50 = 660 nM) and c-FMS (IC50 = 1.4 µM).  On the other hand, vatalanib is not active against the EGFR, c-SRC, v-ABL, and protein kinase Cα (IC50 > 10 µM).  Wood, J.M., et al.  "PTK787/ZK 222584, a Novel and Potent Inhibitor of Vascular Endothelial Growth Factor Receptor Tyrosine Kinases, Impairs Vascular Endothelial Growth Factor-induced Responses and Tumor Growth after Oral Administration."  Cancer Res. 60:  2178-2189 (2000).
Vatalanib dose-dependently inhibits proliferation of MM cells and patient cells (IC50 = 1-5 µM), which are both sensitive and resistant to conventional therapy.  Vatalanib increases the inhibitory effect of dexamethasone on growth of MM cells and can decrease the protective effect of interleukin 6 (IL-6) against dexamethasone-induced apoptosis.  Vatalanib (1 µM) also inhibits VEGF-induced migration of MM cells across an extracellular matrix.  Importantly, vatalanib also blocks the increased MM cell proliferation and increased IL-6 and VEGF secretion in cultures of MM cells adherent to bone marrow stem cells.  Lin, B., et al.  "The vascular endothelial growth factor receptor tyrosine kinase inhibitor PTK787/ZK222584 inhibits growth and migration of multiple myeloma cells in the bone marrow microenvironment."  Cancer Res. 62:  5019-5026 (2002).
Vatalanib inhibited VEGF-induced phosphorylation (IC50's of 17 nM and 34 nM for HUVECs and CHO cells, respectively), blocked thymidine incorporation induced by VEGF in HUVECs (IC50 = 7.1 nM), prevented VEGF-induced HUVEC migration dose dependently (IC50 = 58 nM), and inhibited tumor cell proliferation with an IC50 of 17 µM and 18 µM for A431 and DU145 cells, respectively and sprout formation in rat aortas (IC50 = 675 nM).  Wood, J.M., et al.  "PTK787/ZK 222584, a Novel and Potent Inhibitor of Vascular Endothelial Growth Factor Receptor Tyrosine Kinases, Impairs Vascular Endothelial Growth Factor-induced Responses and Tumor Growth after Oral Administration."  Cancer Res. 60:  2178-2189 (2000).
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 10-20 mg/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.  Disposal:  A

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