Linifanib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

VEGFR 和 PDGFR 家族成员的有效多 RTK 抑制剂。

A potent multi-RTKs inhibitor of members of VEGFR and PDGFR families with IC50 of 4/3/3/14/4/66/190/170 nM for KDR/FLT1/CSF1R/KIT/FLT3/PDGFRβ/FLT4/Tie2, respectively; much less active (IC50>10 uM) against other nonrelated tyrosine kinases, such as steroid receptor coactivator and EGFR; inhibits RTK phosphorylation (IC50=2, 4, and 7 nM for PDGFRβ, KDR, and CSF-1R, respectively) and VEGF-stimulated proliferation (IC50=0.2 nM for human endothelial cells); exhibits efficacy in human fibrosarcoma and breast, colon, and small cell lung carcinoma xenograft models (ED50=1.5-5 mg/kg, twice daily).Colon Cancer Phase 2 Discontinued(In Vitro):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. (In Vivo):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.

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ABT-869 | AL-39324 | ABT 869 | ABT869 | AL 39324 | AL39324

Angiogenesis

VEGFR

CSF-1R|FLT3|Kit|VEGFR1/FLT1|VEGFR2/KDR

Cancer

Colon Cancer

796967-16-3

375.3989

C21H18FN5O

>98% (HPLC)

10 mM in DMSO

O=C(N)N(C1=CC=C(C2=CC=CC3=C2C(N)=NN3)C=C1)C4=CC(C)=CC=C4F

Urea, N-[4-(3-amino-1H-indazol-4-yl)phenyl]-N'-(2-fluoro-5-methylphenyl)-

(-20℃)

With Ice Pack

≥ 2 years