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)

Cat. No.: HY-50751 Purity: 99.72%
Handling Instructions

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.

For research use only. We do not sell to patients.

Linifanib Chemical Structure

Linifanib Chemical Structure

CAS No. : 796967-16-3

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10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
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50 mg USD 250 In-stock
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100 mg USD 350 In-stock
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200 mg USD 650 In-stock
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Description

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)

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].

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].

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.
Clinical Trial
Molecular Weight

375.40

Formula

C₂₁H₁₈FN₅O

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 13.16 mg/mL (35.06 mM; Need ultrasonic)

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
10 mM 0.2664 mL 1.3319 mL 2.6638 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.72%

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Keywords:

LinifanibABT-869 AL-39324ABT869ABT 869AL39324AL 39324AL-39324PDGFRVEGFRFLT3c-Fmsc-KitAutophagyApoptosisPlatelet-derived growth factor receptorVascular endothelial growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3CSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RSCFRCD117cellproliferationantitumormicroRNAcytotoxicityInhibitorinhibitorinhibit

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