Sunitiba Malate is an antineoplastic agent and a potent RTK inhibitor which includes Flk-1 (VEGFR2) as a primary target. It also is a potent, ATP-competitive inhibitor of VEGFR, PDGFR-β and c-Kit (KIT). Sunitiba Malate inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Exhibits antiangiogenic and antitumor activity in multiple xenograft models. Sunitinib Malate is an inhibitor of c-Fms-CSF-1R, Flt-1, Flt-3/Flk-2, Flt-4, PDGFR-α and Ret.
Sun, L., et al.: J. Med. Chem., 46, 1116 (2003), Mendel, D.B., et al.: Clin. Cancer Res., 9, 327 (2003), Sistla, A., et al.: Drug Dev. Ind. Pharm., 30, 19 (2004), Sakamoto, K.M., et al.: Curr. Opin. Invest. Drugs, 5. 1329 (2004),
Soluble in water (>25 mg/ml, pH 1.2-6.8), DMSO (>10 mg/ml), and methanol.
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FergusonFerguson, MJ. et al. (PubMed 26375012) assessed proliferation, -hexosaminidase release (degranulation), and Erk1/2 phosphorylation in Sunitinib Malate, an antineoplastic, multi-kinase inhibitor, treated Nf1+/- mast cells and fibroblasts. Sunitinib Malate suppressed multiple in vitro gain-in-functions of Nf1+/- mast cells and fibroblasts and attenuated Erk1/2 phosphorylation. -SCBT Publication Review
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