SU14813 是一种多靶点受体酪氨酸激酶抑制剂,能够抑制 VEGFR2 (IC50:50 nM),VEGFR1 (IC50:2 nM),PDGFRβ (IC50:4 nM),KIT (IC50:15 nM)。
产品描述
SU14813 is a multi-receptor tyrosine kinase inhibitor with potent antiangiogenesis and antitumor activity (IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT).
体外活性
SU14813, a small molecule identified from the same chemical library used to isolate sunitinib, has broad-spectrum RTK inhibitory activity through binding to and inhibition of VEGFR, PDGFR, KIT, and FLT3.?In cellular assays, SU14813 inhibited ligand-dependent and ligand-independent proliferation, migration, and survival of endothelial cells and/or tumor cells expressing these targets.?SU14813 inhibited VEGFR-2, PDGFR-beta, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent fashion[1].
体内活性
The plasma concentration required for in vivo target inhibition was estimated to be 100 to 200 ng/mL.?Used as monotherapy, SU14813 exhibited broad and potent antitumor activity resulting in regression, growth arrest, or substantially reduced growth of various established xenografts derived from human or rat tumor cell lines.?Treatment in combination with docetaxel significantly enhanced both the inhibition of primary tumor growth and the survival of the tumor-bearing mice compared with administration of either agent alone[1].
Cas No.
627908-92-3
分子式
C23H27FN4O4
分子量
442.491
储存和溶解度
DMSO:44 mg/mL (99.44 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years