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Linifanib

CAT: 0013-GTR19161902-01Size: 1 gDry Ice: NoHazardous: No
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CAT#:0013-GTR19161902-01Size:1 g
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Description
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.
CAS Number
796967-16-3
Product Name Alternative
ABT-869 | AL-39324 | ABT 869 | ABT869 | AL 39324 | AL39324
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
O=C (N) N (C1=CC=C (C2=CC=CC3=C2C (N) =NN3) C=C1) C4=CC (C) =CC=C4F
Molecular Formula
C21H18FN5O
Molecular Weight
375.3989
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
Urea, N-[4- (3-amino-1H-indazol-4-yl) phenyl]-N'- (2-fluoro-5-methylphenyl) -

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HY-50751SLinifanib-d4
HY-50751RLinifanib (Standard)
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