Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.
体外研究
Linifanib (0-10000 nM; 72 hours) inhibits in vitro the cell proliferation of 8305C and 8505C cell lines in a concentration-dependent manner.
Linifanib significantly decreased the levels of phospho-CSF-1R after 24 h and 72 h in both 8505C and 8305C cells.
Cell Viability Assay
Cell Line:
8305C and 8505C cells
Concentration:
0-10000 nM
Incubation Time:
72 hours
Result:
Inhibited the 8305C and 8505C cell proliferation with an IC50 of 0.7 nM and 123.7 nM, respectively.
体内研究
The synergistic ATC antitumor activity of linifanib (10 mg/kg; p.o.; daily for 33 days)/Irinotecan combination significantly increases the survival of ATC affected mice and induces some complete responses.
Animal Model:
Six-week-old CD nu/nu male mice (bearing 8505C ATC cells)
Dosage:
10 mg/kg
Administration:
P.o.; daily for 33 days
Result:
The combination of linifanib and irinotecan produced a greater survival result than either monotherapy, and resulted in a significant higher median survival of 100 days.
分子式
C21H18FN5O
分子量
375.40
CAS号
796967-16-3
中文名称
利尼伐尼
运输条件
Room temperature in continental US; may vary elsewhere.