Linifanib (ABT-869)

製品コードS1003 別名:AL39324,RG3635

Linifanib (ABT-869)化学構造

分子量(MW):375.41

Linifanib (ABT-869)は一種の新たで、有効なATP競争性的なVEGFR/PDGFR阻害剤で、KDR、CSF-1R、Flt-1/3とPDGFRβに作用する時のIC50値が4 nM、3 nM、3 nM/4 nMと66 nMにそれぞれ別れることですが、突然変容キナーゼ依頼性細胞(FLT3)に作用する効果が一番強いです。臨床3期。

サイズ 価格(税別)  
JPY 29880.00
JPY 19920.00
JPY 34860.00
JPY 94620.00

カスタマーフィードバック(3)

  • Effect of the anti-vascular agents Linifanib (100 nM) in the VMO(vascularized micro-organ). VMOs were exposed to the drug at day 5 and cultured for an additional 96 h.

    Sci Rep, 2016, 6:31589.. Linifanib (ABT-869) purchased from Selleck.

    (B and C) KMCH-1 cells were plated alone (monoculture) or together with PDGF-BB-secreting LX-2 cells (co-culture) in a transwell insert co-culture system (KMCH-1 cells in the bottom wells and LX-2 cells in the inserts; 1:1 ratio) for 2 days. Cells were treated as indicated with vehicle, rhTRAIL (10 ng/ml for 6 h on day 2), rhTRAIL plus imatinib [rhTRAIL:10 ng/ml for 6 h on day 2; Imatinib: 5 μmol/L for 24 h (day2)], or rhTRAIL plus linifanib [rhTRAIL: 10 ng/ml for 6 h on day 2; Linifanib:0.5 μmol/L for 24 h (day2)]. After rhTRAIL treatment for 6 h,KMCH-1 cells were analysed for apoptotic nuclear morphology by DAPI-staining (B) and for DNA fragmentation by transferasemediated dUTP nick end labelling assay (C) with quantification of apoptotic nuclei by fluorescence microscopy.

    Liver Int 2011 32, 400-409. Linifanib (ABT-869) purchased from Selleck.

  • T47D breast cancer cells were pretreated with indicated concentrations of ABT-869

     

     

    Dr. Zhang of Tianjin Medical University. Linifanib (ABT-869) purchased from Selleck.

製品安全説明書

VEGFR阻害剤の選択性比較

生物活性

製品説明 Linifanib (ABT-869)は一種の新たで、有効なATP競争性的なVEGFR/PDGFR阻害剤で、KDR、CSF-1R、Flt-1/3とPDGFRβに作用する時のIC50値が4 nM、3 nM、3 nM/4 nMと66 nMにそれぞれ別れることですが、突然変容キナーゼ依頼性細胞(FLT3)に作用する効果が一番強いです。臨床3期。
ターゲット
VEGFR1/FLT1 [1]
(Cell-free assay)
CSF-1R [1]
(Cell-free assay)
VEGFR2/KDR [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
Kit [1]
(Cell-free assay)
3 nM 3 nM 4 nM 4 nM 14 nM
体外試験

Linifanib shows inhibitory to Kit, PDGFRβ and Flt4 with IC50 of 14 nM, 66 nM and 190 nM in kinases assay. Linifanib also inhibits ligand-induced KDR, PDGFRβ, Kit, and CSF-1R phosphorylation with IC50 of 2 nM, 2 nM, 31 nM and 10 nM at cellular level and this cellular potency could be affected by serum protein. Linifanib suppresses VEGF-stimulated HUAEC proliferation with IC50 of 0.2 nM. While Linifanib has weak activity against tumor cells which are not induced by VEGF or PDGF, except for MV4-11 leukemia cells (with constitutively active form of Flt3) with IC50 of 4 nM. Linifanib could cause a decrease in S and G2-M phases with a corresponding increase in the sub-G0-G1 apoptotic population in MV4-11 cells. [1] Linifanib binds to the ATP-binding site of CSF-1R with Ki of 3 nM. [2] Linifanib (10 nM) exhibits a reduced phosphorylation of Akt at Ser473 and decreased phosphorylation of GSK3βat Ser9 in Ba/F3 FLT3 ITD cell lines. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse 3T3 cells M2DQNWZ2dmO2aX;uJIF{e2G7 MlXNTY5pcWKrdHnvckBw\iCYRVfGMYlv\HWlZXSgbJVu[W5iS1TSJJBpd3OyaH;yfYxifGmxbjDpckBud3W|ZTCzWFMh[2WubIOgZpkhTUyLU1GsJGlEPTB;MD6wNFQh|ryP M{PiZVE4OzR|M{ey
Sf9 insect cells M33p[GZ2dmO2aX;uJIF{e2G7 M3HVUVEzOCCvaX7z NGL5eVRKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JGdUXC22YXfn[YQhXkWJRmKyJIV5eHKnc4Pl[EBqdiCVZkmgbY5{\WO2IHPlcIx{KGGodHXyJFEzOCCvaX7zJIJ6KEurbnHz[U1IdG9iYYPzZZktKEmFNUC9OUBvVQ>? M1L0dVIyPzB6NE[4
human MOLM13 cells NE\oW21EgXSxdH;4bYNqfHliYYPzZZk> MkC2O|IhcA>? M3ftfGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1QVE1zMzDj[YxteyCqYYLic5JqdmdibYX0ZY51KE[OVEOgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OD1yLkCzO{DPxE1? NGHsT5czOzZzOEewPS=>
human MV4-11 cells NVH0VYZ[WHKxbHnm[ZJifGmxbjDhd5NigQ>? NWnzXHY5PzJiaB?= NFTFS|ZCdnSrcILvcIln\XKjdHnvckBi[3Srdnn0fUBi\2GrboP0JGZNXDNxSWTEJIhiemKxcnnu[{BpfW2jbjDNWlQuOTFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VWyCvZYToc4QtKEeLNUC9NE4xPCEQvF2= MUeyNVcxQDR4OB?=
human MOLT4 cells MUPQdo9tcW[ncnH0bY9vKGG|c3H5 NITuUoM4OiCq NEf1PY5CdnSrcILvcIln\XKjdHnvckBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUHQ1KGGodHXyJFczKGi{czDifUBOXFNibXX0bI9lNCCJSUWwQVYvPyEQvF2= M2PqWlIyPzB6NE[4
RS4:11 cells M3jOXnBzd2yrZnXyZZRqd25iYYPzZZk> NIXwNGI4OiCq NIe0[5VCdnSrcILvcIln\XKjdHnvckBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGLTOFoyOSClZXzsd{BmgHC{ZYPzbY5oKHerbHSgeJlx\SCITGSzJIFnfGW{IEeyJIhzeyCkeTDNWHMhdWW2aH;kMEBIUTVyPUmuNkDPpG1? M2WzNlIyPzB6NE[4
U937 cells NV7DPYtoWHKxbHnm[ZJifGmxbjDhd5NigQ>? MnPEO|IhcA>? NHvVUpdCdnSrcILvcIln\XKjdHnvckBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF\MWFMh\2WwZT3k[YZq[2mnboSgWVk{PyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRUKG2ndHjv[EwhT0l3ME2xPUDPxE1? NXTNZoN6OjF5MEi0Olg>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 Linifanib (0.3 mg/kg) results in complete inhibition of KDR phosphorylation in lung tissue. Linifanib also inhibits the edema response with ED50 of 0.5 mg/kg. Linifanib (7.5 and 15 mg/kg, bid) significantly inhibits both bFGF- and VEGF-induced angiogenesis in the cornea. Linifanib inhibits tumor growth in flank xenograft models including HT1080, H526, MX-1 and DLD-1 with ED75 from 4.5-12 mg/kg. Linifanib also shows efficacy in A431 and MV4-11 xenografts at low dose levels. Linifanib (12.5 mg/kg bid) reveals a decrease of microvasculure density in MDA-231 xenograft. Linifanib shows a Cmax and AUC24 hours with 0.4 μg/mL and 2.7 μg•hour/mL in HT1080 fibrosarcoma model. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

Kinase assays:

Potencies (IC50 values) are determined by assays of active kinase domains cloned and expressed in baculovirus using the FastBacbaculovirus expression system or obtained commercially. For tyrosine kinase assays, a biotinylated peptide substrate containing a single tyrosine is used with 1 mM ATP, anEu-cryptate–labeled anti-phosphotyrosine antibody (PT66), and Strepavidin-APC in a homogeneous time-resolved 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 Linifanib. The concentration resulting in 50% inhibition of activity is calculated using nonlinear regression analysis of the concentration response data.
細胞試験: [1]
+ 展開
  • 細胞株: HUAEC, HT-29, HT1080, A431, MDA-435, MDA-231, H526, DLD-1, 9L and MV4-11 cells
  • 濃度: 0-100 μM
  • 反応時間: 72 hours
  • 実験の流れ: Cells are seeded into 96-well plates at 2.5 × 103 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, 3 × 103 cells/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 5 × 104 per well are plated in full growth medium, Linifanib is 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 37 °C in a CO2 incubator and analysis in a fluorescence plate reader (544 nm, excitation: 590 nm, emission
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: H526, DLD-1, MDA-231, MDA-435LM, HCT-116, H526, DLD-1, MDA-231, MDA-435LM, MV4-11 and MX-1 xenografts are established in mice.
  • 製剤: 2% ethanol, 5% Tween 80, 20% PEG400, 73% saline
  • 投薬量: ~ 10 mg/kg
  • 投与方法: Oral administration
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 75 mg/mL (199.78 mM)
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 375.41
化学式

C21H18FN5O

CAS No. 796967-16-3
保管
別名 AL39324,RG3635

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01506934 Terminated Advanced or Metastatic Solid Tumors Abbott October 2011 Phase 1
NCT01286974 Terminated Advanced Solid Tumors Abbott August 2011 Phase 1
NCT01413893 Completed Advanced Solid Tumors Abbott June 2011 Phase 1
NCT01365910 Terminated Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer Vanderbilt-Ingram Cancer Center June 2011 Phase 2
NCT01381341 Completed Advanced Solid Tumors Abbott May 2011 Phase 1
NCT01401933 Completed Advanced Solid Tumors Abbott May 2011 Phase 1

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID