Linifanib (ABT-869)

For research use only.

Catalog No.S1003 Synonyms: AL39324,RG3635

25 publications

Linifanib (ABT-869) Chemical Structure

CAS No. 796967-16-3

Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3.

Selleck's Linifanib (ABT-869) has been cited by 25 publications

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Biological Activity

Description Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3.
(Cell-free assay)
CSF-1R [1]
(Cell-free assay)
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
Kit [1]
(Cell-free assay)
3 nM 3 nM 4 nM 4 nM 14 nM
In vitro

Linifanib shows inhibitory to Kit, PDGFRβ and Flt4 with IC50 of 14 nM, 66 nM and 190 nM in kinases assay. Linifanib also inhibits ligand-induced KDR, PDGFRβ, Kit, and CSF-1R phosphorylation with IC50 of 2 nM, 2 nM, 31 nM and 10 nM at cellular level and this cellular potency could be affected by serum protein. Linifanib suppresses VEGF-stimulated HUAEC proliferation with IC50 of 0.2 nM. While Linifanib has weak activity against tumor cells which are not induced by VEGF or PDGF, except for MV4-11 leukemia cells (with constitutively active form of Flt3) with IC50 of 4 nM. Linifanib could cause a decrease in S and G2-M phases with a corresponding increase in the sub-G0-G1 apoptotic population in MV4-11 cells. [1] Linifanib binds to the ATP-binding site of CSF-1R with Ki of 3 nM. [2] Linifanib (10 nM) exhibits a reduced phosphorylation of Akt at Ser473 and decreased phosphorylation of GSK3βat Ser9 in Ba/F3 FLT3 ITD cell lines. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse 3T3 cells NWPwdXJRTnWwY4Tpc44h[XO|YYm= Mn[yTY5pcWKrdHnvckBw\iCYRVfGMYlv\HWlZXSgbJVu[W5iS1TSJJBpd3OyaH;yfYxifGmxbjDpckBud3W|ZTCzWFMh[2WubIOgZpkhTUyLU1GsJGlEPTB;MD6wNFQh|ryP MoGxNVc{PDN|N{K=
Sf9 insect cells MXvGeY5kfGmxbjDhd5NigQ>? NHj5enoyOjBibXnudy=> NYDw[3h4UW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBIW1RvdHHn[4VlKF[HR1\SNkBmgHC{ZYPz[YQhcW5iU3[5JIlve2WldDDj[YxteyCjZoTldkAyOjBibXnud{BjgSCNaX7hd4UuT2yxIHHzd4F6NCCLQ{WwQVUhdk1? NWG4eIdYOjF5MEi0Olg>
human MOLM13 cells NGnHXZpEgXSxdH;4bYNqfHliYYPzZZk> MWW3NkBp NHi5TnhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOV0yPMUOgZ4VtdHNiaHHyZo9zcW6pIH31eIFvfCCITGSzJIFnfGW{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTB;MD6wN|ch|ryP NISxdFkzOzZzOEewPS=>
human MV4-11 cells NYTaNHVRWHKxbHnm[ZJifGmxbjDhd5NigQ>? MonMO|IhcA>? NXjwbpVFSW62aYDyc4xq\mW{YYTpc44h[WO2aY\peJkh[WejaX7zeEBHVFR|L1nUSEBp[XKkb4LpcochcHWvYX6gUXY1NTFzIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFNibXX0bI9lNCCJSUWwQVAvODRizszN M3W1cVIyPzB6NE[4
human MOLT4 cells NHraNWxRem:uaX\ldoF1cW:wIHHzd4F6 MV63NkBp MUTBcpRqeHKxbHnm[ZJifGmxbjDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2RTGS0JIFnfGW{IEeyJIhzeyCkeTDNWHMhdWW2aH;kMEBIUTVyPU[uO{DPxE1? NITWPIYzOTdyOES2PC=>
RS4:11 cells MV;Qdo9tcW[ncnH0bY9vKGG|c3H5 M3TsOFczKGh? NGHNfXNCdnSrcILvcIln\XKjdHnvckBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGLTOFoyOSClZXzsd{BmgHC{ZYPzbY5oKHerbHSgeJlx\SCITGSzJIFnfGW{IEeyJIhzeyCkeTDNWHMhdWW2aH;kMEBIUTVyPUmuNkDPpG1? NE[0NYIzOTdyOES2PC=>
U937 cells NVHTXIJuWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2XKPFczKGh? NYm2[3BlSW62aYDyc4xq\mW{YYTpc44h[WO2aY\peJkh[WejaX7zeEBpfW2jbjDGUHQ{KGenbnWt[IVncWOrZX70JHU6OzdiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VWyCvZYToc4QtKEeLNUC9NVkh|ryP MXWyNVcxQDR4OB?=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-PDGFRβ / PDGFRβ/ p-AKT / AKT / p-mTOR / mTOR / p-S6K ; 

PubMed: 25327881     

Immunoblotting for phospho- or total PDGFR-ß, Akt, mTOR and S6Kin cells treated with linifanib for 24 h.

Beclin-1 / ATG5 / ATG7 / p62 ; 

PubMed: 25327881     

Immunoblotting for Beclin-1, ATG5, ATG7, and p62 using lysates from cells treated with linifanib for 24 h. 

phospho-FLT3 / FLT3 ; 

PubMed: 21471285     

Ba/F3 FLT3 ITD cells were treated for 15, 30 or 60 minutes with 10nM Linifanib or vehicle control (DMSO). Cell lysates were immunoprecipitated (IP) with anti-FLT3 polyclonal antisera or anti-AKT(Pan) monoclonal antisera and sepharose beads. 

25327881 21471285
LC3 ; 

PubMed: 25327881     

Relative quantity of LC3-II was calculated by ImageJ densitometric analysis and normalized by GAPDH. (C). Cells were treated with DMSO or 2.5 μM linifanib for 24 h before they were labeled with fluorescence and imaged by fluorescence microscope. Green: FITC-labeled LC3; Red: lyso-tracker-labeled lysosome; Blue: DAPI-labeled nucleus.

In vivo Linifanib (0.3 mg/kg) results in complete inhibition of KDR phosphorylation in lung tissue. Linifanib also inhibits the edema response with ED50 of 0.5 mg/kg. Linifanib (7.5 and 15 mg/kg, bid) significantly inhibits both bFGF- and VEGF-induced angiogenesis in the cornea. Linifanib inhibits tumor growth in flank xenograft models including HT1080, H526, MX-1 and DLD-1 with ED75 from 4.5-12 mg/kg. Linifanib also shows efficacy in A431 and MV4-11 xenografts at low dose levels. Linifanib (12.5 mg/kg bid) reveals a decrease of microvasculure density in MDA-231 xenograft. Linifanib shows a Cmax and AUC24 hours with 0.4 μg/mL and 2.7 μg•hour/mL in HT1080 fibrosarcoma model. [1]


Kinase Assay:[1]
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Kinase assays:

Potencies (IC50 values) are determined by assays of active kinase domains cloned and expressed in baculovirus using the FastBacbaculovirus expression system or obtained commercially. For tyrosine kinase assays, a biotinylated peptide substrate containing a single tyrosine is used with 1 mM ATP, anEu-cryptate–labeled anti-phosphotyrosine antibody (PT66), and Strepavidin-APC in a homogeneous time-resolved fluorescence assay. Serine/threonine kinases are assayed using 5 μM ATP, [33P]ATP, and a biotinylated peptide substrate with peptide capture and incorporation of 33P determined using a SA-Flashplate. Linifanib is assayed at multiple concentrations prepared by serial dilution of a DMSO stock solution of Linifanib. The concentration resulting in 50% inhibition of activity is calculated using nonlinear regression analysis of the concentration response data.
Cell Research:[1]
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  • Cell lines: HUAEC, HT-29, HT1080, A431, MDA-435, MDA-231, H526, DLD-1, 9L and MV4-11 cells
  • Concentrations: 0-100 μM
  • Incubation Time: 72 hours
  • Method: Cells are seeded into 96-well plates at 2.5 × 103 per well and incubated with serum-free medium for 24 hours. Linifanib and VEGF (final, 10 ng/mL) are added and incubated for 72 hours in serum-free medium. For carcinoma cell lines, 3 × 103 cells/well are plated overnight in full growth medium. Linifanib is added to the cells in full growth medium and incubated for 72 hours. For leukemia cells, generally 5 × 104 per well are plated in full growth medium, Linifanib is added, and incubated for 72 hours. The effects on proliferation are determined by addition of Alamar Blue (final solution, 10%), incubation for 4 hours at 37 °C in a CO2 incubator and analysis in a fluorescence plate reader (544 nm, excitation: 590 nm, emission
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: H526, DLD-1, MDA-231, MDA-435LM, HCT-116, H526, DLD-1, MDA-231, MDA-435LM, MV4-11 and MX-1 xenografts are established in mice.
  • Dosages: ~ 10 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL (199.78 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG 300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.
10 mg/mL

* Please note that Selleck 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.

Chemical Information

Molecular Weight 375.41


CAS No. 796967-16-3
Storage powder
in solvent
Synonyms AL39324,RG3635
Smiles CC1=CC(=C(C=C1)F)NC(=O)NC2=CC=C(C=C2)C3=C4C(=CC=C3)NN=C4N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01401933 Completed Drug: Linifanib|Drug: Rifampin Advanced Solid Tumors Abbott May 2011 Phase 1
NCT01381341 Completed Drug: linifanib Advanced Solid Tumors Abbott May 2011 Phase 1
NCT01114191 Completed Drug: ABT-869|Drug: ketoconazole Solid Tumors Abbott May 2010 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID