Background
Vatalanib is a multi-targeted tyrosine kinase inhibitor. Researchers performing in vitro kinase assays show that vatalanib inhibits VEGFR-1, -2, and -3 with IC50 values of approximately 77 nM, 37 nM, and 640 nM, respectively. Vatalanib also inhibited PDGFR and c-kit at sub micromolar concentrations, but had no activity against several other kinases, including c-Met, EGFR, c-Src, and v-Abl up to 10 μM (1). Vatalanib inhibits VEGF-induced autophosphorylation in HUVE and VEGFR-2 transfected CHO cells with an IC50 of 17 nM and 34 nM, respectively, and effectively blocks VEGF-stimulated HUVE cell proliferation (1). Research studies have demonstrated that vatalanib inhibits proliferation of multiple myeloma (MM) cells in a dose-dependant manner and blocks VEGF-induced ERK phosphorylation and cell migration in MM.1S cells (2). Dose-dependent apoptosis in chronic lymphocytic leukemia (CLL) cells by vatalanib and pazopanib has been observed (3).
Molecular Formula
C20H15ClN4•2HCl
Molecular Weight
419.73 g/mol
Purity
>99%
CAS
212141-51-0
Solubility
Soluble in DMSO at 20mg/ml and H2O at 100mg/ml.
Storage
Directions for Use
Vatalanib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1.19 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 0.5-50 μM for 0.5-2 hr prior to treating with a stimulator. It can also be used alone, with varying treatment times lasting up to 72 hr.
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
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