Linifanib

SKU: orb1223985

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.

Key Properties

• CAS Number: 796967-16-3
• MW: 375.3989
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₈FN₅O
• SMILES: O=C(N)N(C1=CC=C(C2=CC=CC3=C2C(N)=NN3)C=C1)C4=CC(C)=CC=C4F
• Target: VEGFR
• Solubility: 10 mM in DMSO

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Quick Database Links

Gene Symbol

VEGFR