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Linifanib

Chemical Structure : Linifanib

CAS No.: 796967-16-3

Linifanib (ABT-869;AL-39324;ABT 869;ABT869;AL 39324;AL39324)

Catalog No.: PC-45859Not For Human Use, Lab Use Only.

Linifanib (ABT-869) is 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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Linifanib (ABT-869) is 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.
Linifanib (ABT-869) shows much less active (IC50>10 uM) against other nonrelated tyrosine kinases, such as steroid receptor coactivator and EGFR.
Linifanib (ABT-869) 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).
Linifanib (ABT-869) exhibits efficacy in human fibrosarcoma and breast, colon, and small cell lung carcinoma xenograft models (ED50=1.5-5 mg/kg, twice daily).
Linifanib (ABT-869) also is a small molecule inhibitor of necroptosis by targeting RIPK1 kinase

Physicochemical Properties

M.Wt 375.3989
Formula C21H18FN5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Dai Y, et al. J Med Chem. 2007 Apr 5;50(7):1584-97.

2. Shankar DB, et al. Blood. 2007 Apr 15;109(8):3400-8.

3. Albert DH, et al. Mol Cancer Ther. 2006 Apr;5(4):995-1006.
4. Pierotti CL, et al. Biochem J. 2023 Apr 28:BCJ20230035.

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