Vatalanib Dihydrochloride (N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine Dihydrochloride, CGP-79787 Dihydrochloride)

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).\n\nSolubility:\nSoluble 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.\n\nStorage and Stability:\nMay be stored at RT for short-term only. Long-term storage is recommended at -20 degrees C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

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SPECIFICATIONS

Catalog Number

V2120-70A

Size

25mg

Form

Supplied as a pale pink powder.

Purity

~99%

References

1. 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). 2. 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). 3. 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).