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Linifanib (ABT-869)

Catalog No.: A10025

VEGFR/PDGFR inhibitor

Linifanib (ABT-869)

Linifanib (ABT-869) Chemical Structure

CAS NO. 796967-16-3

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.

Availability: In stock

Package Price Qty
5 mg
$40.00
10 mg
$70.00
50 mg
$200.00
100 mg
$350.00
10mM * 1mL in DMSO
$89.00
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Warning Products are for laboratory research use only. Not for human use. We do not sell to patients.
  • Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961

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.
Targets
Target Value
VEGFR1/FLT1IC50: 3nM
CSF-1RIC50: 3nM
VEGFR2/KDRIC50: 4nM
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
In vitro (25°C) DMSO 73 mg/mL (194.45 mM)
Water Insoluble
Ethanol Insoluble
In vivo 5%DMSO+40%PEG 300+5%Tween80+50%ddH2O 9 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.
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 26.64 mL 133.19 mL 266.38 mL
0.5 mM 5.33 mL 26.64 mL 53.28 mL
1 mM 2.66 mL 13.32 mL 26.64 mL
5 mM 0.53 mL 2.66 mL 5.33 mL

*The above data is based on the productmolecular weight 375.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Catalog Num A10025
Actions Inhibitor
CAS No. 796967-16-3
Formula C21H18FN5O
M. Wt 375.4
Purity >98%
Synonyms ABT869, ABT-869
SMILES CC1=CC(=C(C=C1)F)NC(=O)NC2=CC=C(C=C2)C3=C4C(=CC=C3)NN=C4N
Storage

Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for 36 months.
In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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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