1. Protein Tyrosine Kinase/RTK
    Apoptosis
    Autophagy
  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: 99.60%
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 (ABT-869) shows prominent antitumor activity. Linifanib (ABT-869) has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases.

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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 (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 55 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 50 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 90 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 250 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 350 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 650 在庫あり
Estimated Time of Arrival: December 31
500 mg USD 1200 在庫あり
Estimated Time of Arrival: December 31
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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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 (ABT-869) shows prominent antitumor activity. Linifanib (ABT-869) has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases[1][2].

IC50 & Target

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 exhibits IC50 values that range from 4 nM (KDR) to 190 nM (FLT4) for members of the VEGF and PDGF receptor families. Linifanib is also active against TIE2 and, to a lesser extent, RET, but is much less active (IC50>10 μM) against other nonrelated tyrosine kinases, such as steroid receptor coactivator and epidermal growth factor receptor. Phosphorylation of KDR induced by VEGF is inhibited by Linifanib with an IC50 of 4 nM in 3T3 murine fibroblasts engineered to express human KDR. A similar potency for inhibition of receptor autophosphorylation is seen with Linifanib when HUAECs are used as the target cell. Linifanib inhibits VEGF-stimulated phosphorylation of KDR completely at 10 nM and by 70% at 3 nM (IC50=2 nM)[1].

体内実験

Linifanib is effective orally in the mechanism-based murine models of VEGF-induced uterine edema (ED50=0.5 mg/kg) and corneal angiogenesis (>50% inhibition, 15 mg/kg). ABT-869 exhibits efficacy in human fibrosarcoma and breast, colon, and small cell lung carcinoma xenograft models (ED50=1.5-5 mg/kg, twice daily) and is also effective (>50% inhibition) in orthotopic breast and glioma models. Reduction in tumor size and tumor regression is observed in epidermoid carcinoma and leukemia xenograft models, respectively[1].

臨床実験
分子量

375.40

分子式

C₂₁H₁₈FN₅O

CAS 番号

796967-16-3

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 : ≥ 72 mg/mL (191.80 mM)

*"≥" means soluble, but saturation unknown.

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.
参考文献
キナーゼ実験
[1]

For tyrosine kinase assays, a biotinylated peptide substrate containing a single tyrosine is used with 1 mM ATP, an Eu-cryptate-labeled anti-phosphotyrosine antibody (PT66), and Strepavidin-APC in a homogeneous timeresolved 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 the compound. The concentration resulting in 50% inhibition of activity is calculated using nonlinear regression analysis of the concentration response data[1].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

細胞実験
[1]

HUAEC are plated into 96-well plates at 2,500 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, 2,500 per 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 50,000 per well are plated in full growth medium, drug 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 37jC in a CO2 incubator, and analysis in a fluorescence plate reader[1].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[1]

Mice: Tumor-bearing animals are divided into groups (n=10), and administration of vehicle (2% ethanol, 5% Tween 80, 20% PEG400, 73% saline) or inhibitor (Linifanib) at the indicted dose is initiated. Tumor growth in the flank is assessed by measuring tumor size with calipers and calculating size. Tumor volume for the orthotopic glioma model is determined using magnetic resonance imaging[1].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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Keywords:

LinifanibABT-869AL-39324ABT869ABT 869AL39324AL 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-1RCSF1RSCFRCD117Inhibitorinhibitorinhibit

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