Chemical structure of sunitinib.
Western blot analysis of extracts from NIH/3T3 cells, serum-starved overnight and untreated or treated with hPDGF-BB #8912 (100 ng/ml, 5 min) either with or without Sunitinib pre-treatment (2 hr) at the indicated concentrations, using Phospho-PDGF Receptor β (Tyr1009) (42F9) Rabbit mAb #3124 (upper) or PDGF Receptor β (28E1) Rabbit mAb #3169 (lower).
Sunitinib is supplied as a lyophilized powder. For a 5 mM stock, reconstitute the 10 mg in 3.76 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 0.1-10 µM either as a pretreatment for 0.5-2 hr prior to treating with a stimulator or is used alone with varying treatment times lasting up to 24 hr. Sunitinib is soluble in DMSO at 40 mg/ml; poorly soluble in ethanol and water with maximum solubility in water ~10-50 µM.
Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Sunitinib, also known as SU11248, is a multi-tyrosine kinase inhibitor widely known to target PDGFR, VEGFR, KIT, and FLT3, and therefore has both antitumor and antiangiogenic activities. Cellular phosphorylation assays show that sunitinib effectively inhibits ligand-dependent phosphorylation of these receptor tyrosine kinases in nanomolar concentrations and can also inhibit ligand-dependent cellular proliferation (1-3). Sunitinib displays greater than 10-fold selectively for PDGFRB and VEGFR over numerous other kinases, including EGFR, Cdk2, Met, IGF -1R, Abl, and src (2). Inhibition of CSF-1 (4) and RET (5) by sunitinib has also been observed.
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