1. Protein Tyrosine Kinase/RTK Autophagy Apoptosis
  2. PDGFR VEGFR FLT3 c-Fms c-Kit Autophagy Apoptosis
  3. Linifanib

Linifanib  (Synonyms: ABT-869; AL-39324)

Art. -Nr.: HY-50751 Reinheit: 99.39%
Handling Instructions Technical Support

Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.

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Linifanib

Linifanib Chemische Struktur

CAS. Nr. : 796967-16-3

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Based on 5 publication(s) in Google Scholar

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Beschreibung

Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis[1][2].

IC50 & Target[1]

Flt-1

3 nM (IC50)

KDR

4 nM (IC50)

PDGFRβ

66 nM (IC50)

FLT3

4 nM (IC50)

CSF-1R

3 nM (IC50)

Kit

14 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
8343 1
Compound: Linifanib
Antiproliferative activity activity human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity activity human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
A549 IC50
8343 1
Compound: Linifanib
Antiproliferative activity activity human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity activity human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
MV4-11 IC50
3.4 1
Compound: Linifanib
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
NIH3T3 IC50
4 1
Compound: 17p, ABT-869
Inhibition of VEGF-induced human KDR phosphorylation in mouse 3T3 cells by ELISA
Inhibition of VEGF-induced human KDR phosphorylation in mouse 3T3 cells by ELISA
[PMID: 17343372]
EA.hy 926 IC50
2.48 3
Compound: ABT-869
Antiangiogenic activity in human EA.hy 926 cells measured after 24 hrs by MTT assay
Antiangiogenic activity in human EA.hy 926 cells measured after 24 hrs by MTT assay
[PMID: 32750566]
EA.hy 926 IC50
2.48 3
Compound: ABT-869
Antiangiogenic activity in human EA.hy 926 cells measured after 24 hrs by MTT assay
Antiangiogenic activity in human EA.hy 926 cells measured after 24 hrs by MTT assay
[PMID: 32750566]
HepG2 IC50
4001 1
Compound: Linifanib
Antiproliferative activity activity human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity activity human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
MOLM-13 IC50
19 1
Compound: Linifanib
Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
EA.hy 926 IC50
2.48 3
Compound: ABT-869
Antiangiogenic activity in human EA.hy 926 cells measured after 24 hrs by MTT assay
Antiangiogenic activity in human EA.hy 926 cells measured after 24 hrs by MTT assay
[PMID: 32750566]
HL-60 IC50
7880 1
Compound: Linifanib
Antiproliferative activity against human HL-60 cells harboring wildtype FLT3 assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity against human HL-60 cells harboring wildtype FLT3 assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
HUVEC IC50
40.11 3
Compound: Linifanib
Antiproliferative activity against HUVEC after 72 hrs by cell titer glo-based fluorescence assay
Antiproliferative activity against HUVEC after 72 hrs by cell titer glo-based fluorescence assay
[PMID: 30121211]
HUVEC IC50
40.11 3
Compound: Linifanib
Antiproliferative activity against HUVEC after 72 hrs by cell titer glo-based fluorescence assay
Antiproliferative activity against HUVEC after 72 hrs by cell titer glo-based fluorescence assay
[PMID: 30121211]
HL-60 IC50
7880 1
Compound: Linifanib
Antiproliferative activity against human HL-60 cells harboring wildtype FLT3 assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity against human HL-60 cells harboring wildtype FLT3 assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
HUVEC IC50
4920 1
Compound: Linifanib
Cytotoxicity against HUVEC cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Cytotoxicity against HUVEC cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
K562 GI50
>20 3
Compound: ABT-869, 4
Antiproliferation activity against human K562 cells expressing wild type BCR/ABL after 72 hrs by MTS method
Antiproliferation activity against human K562 cells expressing wild type BCR/ABL after 72 hrs by MTS method
[PMID: 21708468]
MOLM-13 GI50
37 1
Compound: 3, ABT-869
Antiproliferative activity against human MOLM13 cells expressing FLT3-ITD mutant
Antiproliferative activity against human MOLM13 cells expressing FLT3-ITD mutant
[PMID: 22726931]
K562 GI50
> 20 3
Compound: ABT-869, 4
Antiproliferation activity against human K562 cells expressing wild type BCR/ABL after 72 hrs by MTS method
Antiproliferation activity against human K562 cells expressing wild type BCR/ABL after 72 hrs by MTS method
[PMID: 21708468]
K562 IC50
6963 1
Compound: Linifanib
Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
MCF7 IC50
17.03 3
Compound: Linifanib
Antiproliferative activity against human MCF7 cells after 72 hrs by cell titer glo-based fluorescence assay
Antiproliferative activity against human MCF7 cells after 72 hrs by cell titer glo-based fluorescence assay
[PMID: 30121211]
MOLM-13 GI50
0.037 3
Compound: ABT-869, 4
Antiproliferation activity against human MOLM13 cells expressing FLT3 mutation assessed as cell viability after 72 hrs by MTS method
Antiproliferation activity against human MOLM13 cells expressing FLT3 mutation assessed as cell viability after 72 hrs by MTS method
[PMID: 21708468]
MCF7 IC50
17.03 3
Compound: Linifanib
Antiproliferative activity against human MCF7 cells after 72 hrs by cell titer glo-based fluorescence assay
Antiproliferative activity against human MCF7 cells after 72 hrs by cell titer glo-based fluorescence assay
[PMID: 30121211]
HUVEC IC50
40.11 3
Compound: Linifanib
Antiproliferative activity against HUVEC after 72 hrs by cell titer glo-based fluorescence assay
Antiproliferative activity against HUVEC after 72 hrs by cell titer glo-based fluorescence assay
[PMID: 30121211]
MOLM-13 GI50
0.037 3
Compound: 3, ABT-869
Cytotoxicity against human MOLM13 cells harboring mutant FLT3 after 72 hrs by MTS assay
Cytotoxicity against human MOLM13 cells harboring mutant FLT3 after 72 hrs by MTS assay
[PMID: 23618709]
MOLM-13 GI50
0.037 3
Compound: 3, ABT-869
Cytotoxicity against human MOLM13 cells harboring mutant FLT3 after 72 hrs by MTS assay
Cytotoxicity against human MOLM13 cells harboring mutant FLT3 after 72 hrs by MTS assay
[PMID: 23618709]
HUVEC IC50
4920 1
Compound: Linifanib
Cytotoxicity against HUVEC cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Cytotoxicity against HUVEC cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
MOLM-13 GI50
0.037 3
Compound: ABT-869, 4
Antiproliferation activity against human MOLM13 cells expressing FLT3 mutation assessed as cell viability after 72 hrs by MTS method
Antiproliferation activity against human MOLM13 cells expressing FLT3 mutation assessed as cell viability after 72 hrs by MTS method
[PMID: 21708468]
MOLT-4 GI50
6.7 3
Compound: ABT-869, 4
Antiproliferation activity against human MOLT4 after 72 hrs by MTS method
Antiproliferation activity against human MOLT4 after 72 hrs by MTS method
[PMID: 21708468]
HepG2 IC50
4001 1
Compound: Linifanib
Antiproliferative activity activity human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity activity human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
MV4-11 GI50
0.04 3
Compound: ABT-869, 4
Antiproliferation activity against FLT3/ITD harboring human MV4-11 cells after 72 hrs by MTS method
Antiproliferation activity against FLT3/ITD harboring human MV4-11 cells after 72 hrs by MTS method
[PMID: 21708468]
MOLM-13 IC50
19 1
Compound: Linifanib
Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
MV4-11 IC50
0.69 3
Compound: Linifanib
Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo-based fluorescence assay
Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo-based fluorescence assay
[PMID: 30121211]
MOLT-4 GI50
6.7 3
Compound: ABT-869, 4
Antiproliferation activity against human MOLT4 after 72 hrs by MTS method
Antiproliferation activity against human MOLT4 after 72 hrs by MTS method
[PMID: 21708468]
MV4-11 GI50
0.04 3
Compound: ABT-869, 4
Antiproliferation activity against FLT3/ITD harboring human MV4-11 cells after 72 hrs by MTS method
Antiproliferation activity against FLT3/ITD harboring human MV4-11 cells after 72 hrs by MTS method
[PMID: 21708468]
RS4-11 GI50
9.2 3
Compound: ABT-869, 4
Antiproliferation activity against human RS4:11 cells expressing wild type FLT3 after 72 hrs by MTS method
Antiproliferation activity against human RS4:11 cells expressing wild type FLT3 after 72 hrs by MTS method
[PMID: 21708468]
MV4-11 IC50
0.69 3
Compound: Linifanib
Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo-based fluorescence assay
Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo-based fluorescence assay
[PMID: 30121211]
Sf9 IC50
0.02 3
Compound: ABT-869, 4
Inhibition of GST-tagged FLT3 expressing wild type kinase domain expressed in Sf9 insect cells after 4 hrs by Kinase-Glo assay
Inhibition of GST-tagged FLT3 expressing wild type kinase domain expressed in Sf9 insect cells after 4 hrs by Kinase-Glo assay
[PMID: 21708468]
MV4-11 IC50
3.4 1
Compound: Linifanib
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
Sf9 IC50
0.76 3
Compound: 3, ABT-869
Inhibition of recombinant GST tagged Aurora A kinase (123 to 401) (unknown origin) transfected in insect sf9 cells after 90 mins by wallac counting analysis
Inhibition of recombinant GST tagged Aurora A kinase (123 to 401) (unknown origin) transfected in insect sf9 cells after 90 mins by wallac counting analysis
[PMID: 23618709]
K562 GI50
> 20 3
Compound: ABT-869, 4
Antiproliferation activity against human K562 cells expressing wild type BCR/ABL after 72 hrs by MTS method
Antiproliferation activity against human K562 cells expressing wild type BCR/ABL after 72 hrs by MTS method
[PMID: 21708468]
NIH3T3 IC50
4 1
Compound: 17p, ABT-869
Inhibition of VEGF-induced human KDR phosphorylation in mouse 3T3 cells by ELISA
Inhibition of VEGF-induced human KDR phosphorylation in mouse 3T3 cells by ELISA
[PMID: 17343372]
Sf9 IC50
0.007 3
Compound: 3, ABT-869
Inhibition of recombinant GST tagged VEGFR2 (789 to 1356) (unknown origin) transfected in insect sf9 cells after 120 mins by wallac counting analysis
Inhibition of recombinant GST tagged VEGFR2 (789 to 1356) (unknown origin) transfected in insect sf9 cells after 120 mins by wallac counting analysis
[PMID: 23618709]
K562 IC50
6963 1
Compound: Linifanib
Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
RS4-11 GI50
9.2 3
Compound: ABT-869, 4
Antiproliferation activity against human RS4:11 cells expressing wild type FLT3 after 72 hrs by MTS method
Antiproliferation activity against human RS4:11 cells expressing wild type FLT3 after 72 hrs by MTS method
[PMID: 21708468]
Sf9 IC50
0.76 3
Compound: ABT-869, 4
Inhibition of recombinant GST-tagged Aurora A expressed in Sf9 insect cells after 90 mins by Kinase-Glo assay
Inhibition of recombinant GST-tagged Aurora A expressed in Sf9 insect cells after 90 mins by Kinase-Glo assay
[PMID: 21708468]
MCF7 IC50
17.03 3
Compound: Linifanib
Antiproliferative activity against human MCF7 cells after 72 hrs by cell titer glo-based fluorescence assay
Antiproliferative activity against human MCF7 cells after 72 hrs by cell titer glo-based fluorescence assay
[PMID: 30121211]
Sf9 IC50
0.005 3
Compound: ABT-869, 4
Inhibition of recombinant GST-tagged VEGFR2 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay
Inhibition of recombinant GST-tagged VEGFR2 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay
[PMID: 21708468]
Sf9 IC50
0.037 3
Compound: ABT-869, 4
Inhibition of recombinant GST-tagged VEGFR1 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay
Inhibition of recombinant GST-tagged VEGFR1 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay
[PMID: 21708468]
Sf9 IC50
0.005 3
Compound: ABT-869, 4
Inhibition of recombinant GST-tagged VEGFR2 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay
Inhibition of recombinant GST-tagged VEGFR2 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay
[PMID: 21708468]
MOLM-13 GI50
0.037 3
Compound: 3, ABT-869
Cytotoxicity against human MOLM13 cells harboring mutant FLT3 after 72 hrs by MTS assay
Cytotoxicity against human MOLM13 cells harboring mutant FLT3 after 72 hrs by MTS assay
[PMID: 23618709]
Sf9 IC50
0.007 3
Compound: 3, ABT-869
Inhibition of recombinant GST tagged VEGFR2 (789 to 1356) (unknown origin) transfected in insect sf9 cells after 120 mins by wallac counting analysis
Inhibition of recombinant GST tagged VEGFR2 (789 to 1356) (unknown origin) transfected in insect sf9 cells after 120 mins by wallac counting analysis
[PMID: 23618709]
MOLM-13 GI50
0.037 3
Compound: ABT-869, 4
Antiproliferation activity against human MOLM13 cells expressing FLT3 mutation assessed as cell viability after 72 hrs by MTS method
Antiproliferation activity against human MOLM13 cells expressing FLT3 mutation assessed as cell viability after 72 hrs by MTS method
[PMID: 21708468]
Sf9 IC50
0.02 3
Compound: 3, ABT-869
Inhibition of wild type GST tagged FLT3 kinase (567 to 993) (unknown origin) transfected in insect sf9 cells after 4 hrs by wallac counting analysis
Inhibition of wild type GST tagged FLT3 kinase (567 to 993) (unknown origin) transfected in insect sf9 cells after 4 hrs by wallac counting analysis
[PMID: 23618709]
Sf9 IC50
0.02 3
Compound: 3, ABT-869
Inhibition of wild type GST tagged FLT3 kinase (567 to 993) (unknown origin) transfected in insect sf9 cells after 4 hrs by wallac counting analysis
Inhibition of wild type GST tagged FLT3 kinase (567 to 993) (unknown origin) transfected in insect sf9 cells after 4 hrs by wallac counting analysis
[PMID: 23618709]
MOLM-13 GI50
37 1
Compound: 3, ABT-869
Antiproliferative activity against human MOLM13 cells expressing FLT3-ITD mutant
Antiproliferative activity against human MOLM13 cells expressing FLT3-ITD mutant
[PMID: 22726931]
Sf9 IC50
0.02 3
Compound: ABT-869, 4
Inhibition of GST-tagged FLT3 expressing wild type kinase domain expressed in Sf9 insect cells after 4 hrs by Kinase-Glo assay
Inhibition of GST-tagged FLT3 expressing wild type kinase domain expressed in Sf9 insect cells after 4 hrs by Kinase-Glo assay
[PMID: 21708468]
HepG2 IC50
4001 1
Compound: Linifanib
Antiproliferative activity activity human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity activity human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
MOLM-13 IC50
19 1
Compound: Linifanib
Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
HUVEC IC50
4920 1
Compound: Linifanib
Cytotoxicity against HUVEC cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Cytotoxicity against HUVEC cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
Sf9 IC50
0.037 3
Compound: ABT-869, 4
Inhibition of recombinant GST-tagged VEGFR1 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay
Inhibition of recombinant GST-tagged VEGFR1 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay
[PMID: 21708468]
MOLT-4 GI50
6.7 3
Compound: ABT-869, 4
Antiproliferation activity against human MOLT4 after 72 hrs by MTS method
Antiproliferation activity against human MOLT4 after 72 hrs by MTS method
[PMID: 21708468]
K562 IC50
6963 1
Compound: Linifanib
Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
Sf9 IC50
0.76 3
Compound: 3, ABT-869
Inhibition of recombinant GST tagged Aurora A kinase (123 to 401) (unknown origin) transfected in insect sf9 cells after 90 mins by wallac counting analysis
Inhibition of recombinant GST tagged Aurora A kinase (123 to 401) (unknown origin) transfected in insect sf9 cells after 90 mins by wallac counting analysis
[PMID: 23618709]
HL-60 IC50
7880 1
Compound: Linifanib
Antiproliferative activity against human HL-60 cells harboring wildtype FLT3 assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity against human HL-60 cells harboring wildtype FLT3 assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
Sf9 IC50
0.76 3
Compound: ABT-869, 4
Inhibition of recombinant GST-tagged Aurora A expressed in Sf9 insect cells after 90 mins by Kinase-Glo assay
Inhibition of recombinant GST-tagged Aurora A expressed in Sf9 insect cells after 90 mins by Kinase-Glo assay
[PMID: 21708468]
U-937 GI50
19 3
Compound: ABT-869, 4
Antiproliferation activity against human FLT3 gene-deficient U937 cells after 72 hrs by MTS method
Antiproliferation activity against human FLT3 gene-deficient U937 cells after 72 hrs by MTS method
[PMID: 21708468]
A549 IC50
8343 1
Compound: Linifanib
Antiproliferative activity activity human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity activity human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
U-937 GI50
19 3
Compound: ABT-869, 4
Antiproliferation activity against human FLT3 gene-deficient U937 cells after 72 hrs by MTS method
Antiproliferation activity against human FLT3 gene-deficient U937 cells after 72 hrs by MTS method
[PMID: 21708468]
MV4-11 GI50
0.04 3
Compound: ABT-869, 4
Antiproliferation activity against FLT3/ITD harboring human MV4-11 cells after 72 hrs by MTS method
Antiproliferation activity against FLT3/ITD harboring human MV4-11 cells after 72 hrs by MTS method
[PMID: 21708468]
MV4-11 IC50
0.69 3
Compound: Linifanib
Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo-based fluorescence assay
Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo-based fluorescence assay
[PMID: 30121211]
MV4-11 IC50
3.4 1
Compound: Linifanib
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 35863236]
NFS-60 GI50
4.4 3
Compound: ABT-869
Growth inhibition of mouse NFS-60 cells incubated for 72 hrs by Cell titer-glo assay
Growth inhibition of mouse NFS-60 cells incubated for 72 hrs by Cell titer-glo assay
[PMID: 36335744]
NFS-60 IC50
30 1
Compound: ABT-869
Cytotoxicity against mouse NFS-60 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titer-glo assay
Cytotoxicity against mouse NFS-60 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titer-glo assay
[PMID: 36335744]
NIH3T3 IC50
4 1
Compound: 17p, ABT-869
Inhibition of VEGF-induced human KDR phosphorylation in mouse 3T3 cells by ELISA
Inhibition of VEGF-induced human KDR phosphorylation in mouse 3T3 cells by ELISA
[PMID: 17343372]
RAW264.7 IC50
8.6 3
Compound: ABT-869
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 36335744]
RPMI-8226 IC50
5889.4 1
Compound: Chemical probe : ABT-869
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
[PMID: 26254279]
RS4-11 GI50
9.2 3
Compound: ABT-869, 4
Antiproliferation activity against human RS4:11 cells expressing wild type FLT3 after 72 hrs by MTS method
Antiproliferation activity against human RS4:11 cells expressing wild type FLT3 after 72 hrs by MTS method
[PMID: 21708468]
Sf9 IC50
0.005 3
Compound: ABT-869, 4
Inhibition of recombinant GST-tagged VEGFR2 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay
Inhibition of recombinant GST-tagged VEGFR2 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay
[PMID: 21708468]
Sf9 IC50
0.007 3
Compound: 3, ABT-869
Inhibition of recombinant GST tagged VEGFR2 (789 to 1356) (unknown origin) transfected in insect sf9 cells after 120 mins by wallac counting analysis
Inhibition of recombinant GST tagged VEGFR2 (789 to 1356) (unknown origin) transfected in insect sf9 cells after 120 mins by wallac counting analysis
[PMID: 23618709]
Sf9 IC50
0.02 3
Compound: 3, ABT-869
Inhibition of wild type GST tagged FLT3 kinase (567 to 993) (unknown origin) transfected in insect sf9 cells after 4 hrs by wallac counting analysis
Inhibition of wild type GST tagged FLT3 kinase (567 to 993) (unknown origin) transfected in insect sf9 cells after 4 hrs by wallac counting analysis
[PMID: 23618709]
Sf9 IC50
0.02 3
Compound: ABT-869, 4
Inhibition of GST-tagged FLT3 expressing wild type kinase domain expressed in Sf9 insect cells after 4 hrs by Kinase-Glo assay
Inhibition of GST-tagged FLT3 expressing wild type kinase domain expressed in Sf9 insect cells after 4 hrs by Kinase-Glo assay
[PMID: 21708468]
Sf9 IC50
0.037 3
Compound: ABT-869, 4
Inhibition of recombinant GST-tagged VEGFR1 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay
Inhibition of recombinant GST-tagged VEGFR1 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay
[PMID: 21708468]
Sf9 IC50
0.76 3
Compound: 3, ABT-869
Inhibition of recombinant GST tagged Aurora A kinase (123 to 401) (unknown origin) transfected in insect sf9 cells after 90 mins by wallac counting analysis
Inhibition of recombinant GST tagged Aurora A kinase (123 to 401) (unknown origin) transfected in insect sf9 cells after 90 mins by wallac counting analysis
[PMID: 23618709]
Sf9 IC50
0.76 3
Compound: ABT-869, 4
Inhibition of recombinant GST-tagged Aurora A expressed in Sf9 insect cells after 90 mins by Kinase-Glo assay
Inhibition of recombinant GST-tagged Aurora A expressed in Sf9 insect cells after 90 mins by Kinase-Glo assay
[PMID: 21708468]
U-937 GI50
19 3
Compound: ABT-869, 4
Antiproliferation activity against human FLT3 gene-deficient U937 cells after 72 hrs by MTS method
Antiproliferation activity against human FLT3 gene-deficient U937 cells after 72 hrs by MTS method
[PMID: 21708468]
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[3].
Linifanib significantly decreased the levels of phospho-CSF-1R after 24 h and 72 h in both 8505C and 8305C cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: 8305C and 8505C cells
Concentration: 0-10000 nM
Incubation Time: 72 hours
Result: Inhibited the 8305C and 8505C cell proliferation with an IC50 of 0.7 nM and 123.7 nM, respectively.
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[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-week-old CD nu/nu male mice (bearing 8505C ATC cells)[3]
Dosage: 10 mg/kg
Administration: P.o.; daily for 33 days
Result: The combination of linifanib and irinotecan produced a greater survival result than either monotherapy, and resulted in a significant higher median survival of 100 days.
Klinische Studie
Molekulargewicht

375.40

Formel

C21H18FN5O

CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(C2=C3C(N)=NNC3=CC=C2)C=C1)NC4=C(C=CC(C)=C4)F

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 10.5 mg/mL (27.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6638 mL 13.3191 mL 26.6383 mL
5 mM 0.5328 mL 2.6638 mL 5.3277 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.32 mg/mL (3.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.32 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.32 mg/mL (3.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.32 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation

Purity: 99.39%

Verweise

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6638 mL 13.3191 mL 26.6383 mL 66.5956 mL
5 mM 0.5328 mL 2.6638 mL 5.3277 mL 13.3191 mL
10 mM 0.2664 mL 1.3319 mL 2.6638 mL 6.6596 mL
15 mM 0.1776 mL 0.8879 mL 1.7759 mL 4.4397 mL
20 mM 0.1332 mL 0.6660 mL 1.3319 mL 3.3298 mL
25 mM 0.1066 mL 0.5328 mL 1.0655 mL 2.6638 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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