1. Protein Tyrosine Kinase/RTK
  2. VEGFR PDGFR
  3. Linifanib

Linifanib  (Synonyms: 利尼伐尼; ABT-869; AL-39324)

目录号: HY-50751G
产品使用指南 技术支持

Linifanib (ABT-869) (GMP) 是 GMP 级别的 Linifanib (HY-50751)。GMP 级别的小分子可用做细胞疗法中的辅助试剂。Linifanib 是一种高效、口服的 VEGFRPDGFR 家族多靶点抑制剂,对 KDR、FLT1、PDGFRβ、FLT3 的 IC50 分别为 4、3、66、4 nM。Linifanib (GMP) 可促进由体细胞到 iPSC 的生成和重编程。

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Linifanib

Linifanib Chemical Structure

CAS No. : 796967-16-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Linifanib (ABT-869) (GMP) is Linifanib (HY-50751) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Linifanib 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 (GMP) promotes the generation and reprogramming of iPSCs from somatic cells[1].

IC50 & Target

IC50: 4 nM (KDR), 4 nM (FLT1), 66 nM (PDGFRβ), 3 nM (CSF-1R), 4 nM (FLT3), 14 nM (Kit)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
8343 nM
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]
EA.hy 926 IC50
2.48 μM
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 nM
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 μM
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
4920 nM
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]
HepG2 IC50
4001 nM
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]
K562 GI50
> 20 μM
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 nM
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 μM
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 μM
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 μM
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]
MOLM-13 GI50
37 nM
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]
MOLM-13 IC50
19 nM
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]
MOLT-4 GI50
6.7 μM
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 μM
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 μM
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 nM
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 μM
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 nM
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 nM
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 μM
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 nM
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 μM
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 μM
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 μM
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 μM
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 μM
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 μM
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 μM
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 μM
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 μM
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]
体外研究
(In Vitro)

Linifanib (GMP) (1 μM) 诱导人胚胎成纤维细胞 (HEF) 生成 hCiPS 细胞[1]
Linifanib (GMP) (1 μM) 诱导 hADSCs 或 hASFs 产生 hCiPS 细胞[1]

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

Clinical Trial
分子量

375.40

Formula

C21H18FN5O

CAS 号
中文名称

利尼伐尼 (GMP)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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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