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)

製品番号: HY-50751 純度: 98.89%
COA 取扱説明書

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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Linifanib 構造式

Linifanib 構造式

CAS 番号 : 796967-16-3

容量 価格(税別) 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 61 在庫あり
Solution
10 mM * 1 mL in DMSO USD 61 在庫あり
Solid
5 mg USD 55 在庫あり
10 mg USD 99 在庫あり
50 mg USD 275 在庫あり
100 mg USD 385 在庫あり
200 mg USD 715 在庫あり
500 mg USD 1320 在庫あり
1 g   お問い合わせ  
5 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Other Forms of Linifanib:

Top Publications Citing Use of Products

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VEGFR アイソフォーム固有の製品をすべて表示:

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  • 純度とドキュメンテーション

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製品説明

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)

体外実験

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.
体内実験

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.
臨床実験
分子量

375.40

分子式

C21H18FN5O

CAS 番号
Appearance

Solid

Color

White to gray

SMILES

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.
体内:
  • 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 available by MedChemExpress (MCE).
純度とドキュメンテーション

純度: 99.28%

参考文献
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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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製品名:
Linifanib
製品番号:
HY-50751
数量:
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