Linifanib (ABT-869)Catalog No. A10025

Quick Overview

Linifanib (ABT-869) is a structurally novel, potent inhibitor of RTK, VEGF and PDGF with IC50 of 0.2, 2, 4, and 7 nM for human endothelial cells, PDGFR-β, KDR, and CSF-1R, respectively.
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Linifanib (ABT-869)

Product Information
Catalog Num A10025
M. Wt 375.4
Formula C21H18FN5O
Solubility DMSO
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 796967-16-3
Synonyms ABT869, ABT-869
Chemical Name N-​[4-​(3-​amino-​1H-​indazol-​4-​yl)phenyl]-​N’-​(2-​fluoro-​5-​methylphenyl)-​urea

Biological activity
Linifanib (ABT-869) is a structurally novel, potent inhibitor of RTK, VEGF and PDGF with IC50 of 0.2, 2, 4, and 7 nM for human endothelial cells, PDGFR-β, KDR, and CSF-1R, respectively.
Target Value
CSF-1RIC50: 3nM
FLT3IC50: 4nM
KitIC50: 14nM
PDGFRβIC50: 66nM
Tie-2IC50: 170nM
VEGFR3/FLT4IC50: 190nM
SGKIC50: 940nM
RETIC50: 1.9μM
PKAIC50: 5.9μM
Cdc2IC50: 9.8μM
FGFRIC50: >12.5μM
LynIC50: >20μM
LCKIC50: 38μM
SrcIC50: >50μM
IGFRIC50: >50μM
INSRIC50: >50μM
EGFRIC50: >50μM
HckIC50: >50μM
c-MetIC50: >50μM
FynIC50: >50μM
FGRIC50: >50μM
AktIC50: >50μM
Solubility (25C) * In vitro DMSO 75 mg/mL (199.78 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

1. Zhou J, Khng J, Jasinghe VJ, Bi C, Neo CH, Pan M, Poon LF, Xie Z, Yu H, Yeoh AE, Lu Y, Glaser KB, Albert DH, Davidsen SK, Chen CS: In vivo activity of ABT-869, a multi-target kinase inhibitor, against acute myeloid leukemia with wild-type FLT3 receptor. Leuk Res. 2008 Jul;32(7):1091-100. Epub 2007 Dec 26. [PubMed:18160102 ]

2. Guo J, Marcotte PA, McCall JO, Dai Y, Pease LJ, Michaelides MR, Davidsen SK, Glaser KB: Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors. Mol Cancer Ther. 2006 Apr;5(4):1007-13. [PubMed:16648572 ]

3. Albert DH, Tapang P, Magoc TJ, Pease LJ, Reuter DR, Wei RQ, Li J, Guo J, Bousquet PF, Ghoreishi-Haack NS, Wang B, Bukofzer GT, Wang YC, Stavropoulos JA, Hartandi K, Niquette AL, Soni N, Johnson EF, McCall JO, Bouska JJ, Luo Y, Donawho CK, Dai Y, Marcotte PA, Glaser KB, Michaelides MR, Davidsen SK: Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol Cancer Ther. 2006 Apr;5(4):995-1006. [PubMed:16648571 ]

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