Nintedanib (BIBF 1120)

製品コードS1010 別名:Intedanib

Nintedanib (BIBF 1120)化学構造

分子量(MW):539.62

Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.

サイズ 価格(税別)  
JPY 39840.00
JPY 19920.00
JPY 34860.00
JPY 111220.00

カスタマーフィードバック(8)

  • PBLs from CLL5 were treated with vehicles (0.1% ethanol and 0.005% DMSO), 106 M dexamethasone, 50 nM BIBF 1120, or both for 24 h. Cells were also treated with 0.1% ethanol or 106 M dexamethasone in the presence of either nonphosphorylated (control) EGQYEEIP or phosphorylated EGQY*EEIP H2O soluble peptides (200 nM) for 24 h.

     

     

    Cell Death Differ 2010 17, 1381-1391. Nintedanib (BIBF 1120) purchased from Selleck.

    Effect of BIBF 1120 on the accumulation of doxorubicin (Dox) and rhodamine 123. The accumulations of doxorubicin a, b and rhodamine 123 c, d were measured by flow cytometric analysis as described in "Materials and Methods". The results are presented as fold change in fluorescence intensity relative to control MDR cells. Columns, means of triplicate determinations; bars, SDs. **P<0.01 versus control group

    Cell Oncol 2011 34, 33–44. Nintedanib (BIBF 1120) purchased from Selleck.

  • Effect of BIBF 1120 on the expression of ABCB1 in MDR cells. Hep G2/adr and MCF-7/adr cells were treated with BIBF 1120 at various concentrations for 48 h. a The mRNA level of ABCB1 was determined by RT-PCR as described in "Materials and Methods"; b Equal amounts of total cell lysates were loaded and detected by Western blot. A representative result is shown from at least three independent experiments

    Cell Oncol 2011 34, 33–44. Nintedanib (BIBF 1120) purchased from Selleck.

    Effect of BIBF 1120 on blockade of AKT and ERK1/2 phosphorylation. Hep G2/adr and MCF-7/adr cells were treated with drugs for 24 h. Equal amount of protein was loaded for Western blot as described in "Materials and Methods". All these experiments were repeated at leas thrice, and a representative experiment is shown in each pane

    Cell Oncol 2011 34, 33–44. Nintedanib (BIBF 1120) purchased from Selleck.

  • BIBF 1120 inhibition of verapamil-stimulated ABCB1 ATPase activity. ABCB1 ATPase assays were performed according to the instruction of Pgp-Glo™ Assay Systems. Each point represents the mean±SDs for triplated independent determinations

    Cell Oncol 2011 34, 33–44. Nintedanib (BIBF 1120) purchased from Selleck.

    Nintedanib decreases constitutive expression of extracellular matrix proteins fibronectin and collagen 1a1 in idiopathic pulmonary fibrosis (IPF) fibroblasts. (A and B) IPF fibroblasts were treated with increasing doses of nintedanib (0.5, 1, or 2 μM) (A) or nintedanib (2 μM) for increasing durations (24, 48, or 72 h) (B). Expression of fibronectin and collagen 1a1 was evaluated by Western immunoblotting.

    Am J Respir Cell Mol Biol, 2016, 54(1):51-9. Nintedanib (BIBF 1120) purchased from Selleck.

  • Immunofluorescence Assay. PDCD4, GRA3, and overlapping are represented in red, green, and yellow, respectively. Group I TKIs sunitinib and AZD9291 show similar results to that of the negative control with PDCD4 and GRA3 well localized inside the nuclei. Mild disruption of PDCD4 in the nuclei is observed with Group II TKIs gefitinib, erlotinib, and AG1478. Group III TKIs neratinib, afatinib, and pelitinib show comparable changes to that of pyrimethamine 5 μM, with complete disruption of PDCD4 and GRA3, without any localization. The assays were repeated 3 times, and each experiment was performed in triplicate. A representative result is shown (x1,000).

    Korean J Parasitol, 2017, 55(5): 491-503. Nintedanib (BIBF 1120) purchased from Selleck.

    Ba/F3 cell lines expressing the recombinant TEL/kinase domain fusion protein for FGFR1-4 .Cells were grown in RPMI 1640 containing 10% FBS and 500 ng/mL puromycin. The parental Ba/F3 cell line transduced with an empty vector was grown in 10 ng/mL IL-3 (R & D systems). Cell viability was assessed at 72 hours using the Cell Titer 96 Aqueous One Solution (Promega). Data were plotted as percent viability relative to vehicle-treated cells and are shown as mean (±SD) from 3 experiments.

     

     

    AACR 2011 Nintedanib (BIBF 1120) 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 Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.
ターゲット
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
LCK [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
VEGFR1 [1]
(Cell-free assay)
13 nM 13 nM 16 nM 26 nM 34 nM
体外試験

BIBF1120 inhibits PDGFR kinase activity of PDGFR alpha and PDGFR beta types with IC50 values of 59 nM and 65 nM, respectively. In addition, BIBF1120 suppresses the FGFR subtypes with IC50 of 60 nM, 37 nM and 108 nM for FGFR1, FGFR2, and FGFR3, respectively. BIBF1120 binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. The indolinone scaffold forms two hydrogen bonds with the backbone nitrogen of Cys919 and the backbone carbonyl oxygen of Glu917 in the hinge region. BIBF 1120 inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. BIBF1120 at concentrations as low as 100 nM blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. In cultures of human vascular smooth muscle cells (HUASMC), BIBF1120 prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM. [1]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKOV3 M4Lne2Z2dmO2aX;uJGF{e2G7 MUe1JOK2VQ>? NYHPbmxEOjRiaB?= MmC2SG1UVw>? NEn0bHlqdmS3Y3XzJIEhe2mpbnnmbYNidnRiaX7jdoVie2ViaX6geIhmKHC{b33veIVzKGGldHn2bZRq\XNib3[gSU1k[WRuwrDDSGgyNCCjbnVCpGNFUDN? Mn3SNlYxPjF5NEe=
A549 NFvRXFhHfW6ldHnvckBCe3OjeR?= MoXBNk82KM7:TR?= M4HjZ|I1KGh? MXfEUXNQ NF\GXHpp[XNiYTDn[Y5memGuIFXNWEBz\X[ncoPhcEBm\m[nY4VCpC=> MUCyOlA3OTd2Nx?=
T24 MWrGeY5kfGmxbjDBd5NigQ>? MViyM|Uh|ryP M13EflI1KGh? NV;qO2ljTE2VTx?= NFHT[5Jp[XNiYTDn[Y5memGuIFXNWEBz\X[ncoPhcEBm\m[nY4VCpC=> MXyyOlA3OTd2Nx?=
Mia-Paca2 NWDLUIlQTnWwY4Tpc44hSXO|YYm= MWiyM|Uh|ryP NVnXUXF[OjRiaB?= MW\EUXNQ MYHoZZMh[SCpZX7ldoFtKEWPVDDy[ZZmenOjbDDl[oZm[3UEoB?= NFLoVXkzPjB4MUe0Oy=>
A549 NX3aNVltTnWwY4Tpc44hSXO|YYm= Mlu0NE4xOeLCk{ZCpO69VQ>? Mn7ONlQhcA>? MoTySG1UVw>? NITUfZJqdmS3Y3XzJHNHXFCGwrDtVm5CKGW6cILld5Nqd25iZH;z[UBl\XCnbnTlcpRtgQ>? MnjtNlU5PDNyMEW=
A549 NYLKXolbTnWwY4Tpc44hSXO|YYm= NF3wUJgxNjBz4pETOeKh|ryP NF\NbVg4OiCq NFzBdoJFVVOR MWPlcohidmOnczDTVE1FKHC{b4TlbY4h\XiycnXzd4lwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meiCjdDDjc45k\W62cnH0bY9veyCxZjD1dEB1dyB3wrFOwG3DqA>? MWSyOVg1OzByNR?=
A549 NV20S2dCTnWwY4Tpc44hSXO|YYm= NXTUNVVtPcLizszN NHe2PXgxNTFiaB?= M1vORWROW09? NUXRWmE2cW6lcnXhd4V{KEGSLUGgZYN1cX[jdHnvckAh[W[2ZYKgN|AhdWmw M1;kPVI2QDR|MEC1
Hep3B MULD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlHONE0zOCEQvF2= NWHBfmQzPDkEoHi= NEfMTm5l\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NVPYeFdsOjR4NUezPVg>
HepG2 M2TwbmNmdGxiVnnhZoltcXS7IFHzd4F6 NXniU5g1OC1{MDFOwG0> NV\GXnV4PDkEoHi= M2XydIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M1T1[VI1PjV5M{m4
PLC5 NHvsU2ZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVf0b3pWOC1{MDFOwG0> MmrWOFjDqGh? NVf6cGQ4\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= NXj4OWJmOjR4NUezPVg>
HuH7 Mn;6R4VtdCCYaXHibYxqfHliQYPzZZk> NGXGPYcxNTJyIN88US=> NYnMVmVDPDkEoHi= MVXk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MWSyOFY2PzN7OB?=
SK-Hep1 NVTpNpJoS2WubDDWbYFjcWyrdImgRZN{[Xl? M1XoVVAuOjBizszN M2\yZlQ5yqCq MV3k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M1qzUVI1PjV5M{m4
Hep3B NXHYO|BbSXCxcITvd4l{KEG|c3H5 NH7D[mMxNTJyIN88US=> NYP3TpVtPDkEoHi= MVzpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGSxc3Wg[IVx\W6mZX70cJk> MYqyOFY2PzN7OB?=
HepG2 NYrwfFh{SXCxcITvd4l{KEG|c3H5 NUO4NGFyOC1{MDFOwG0> MnW3OFjDqGh? NWLpRY04cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MVOyOFY2PzN7OB?=
PLC5 NYW0fVNlSXCxcITvd4l{KEG|c3H5 NVHidlZGOC1{MDFOwG0> M2fKV|Q5yqCq NXL4VXRJcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NUn6T4hOOjR4NUezPVg>
HuH7 NVHWXmRMSXCxcITvd4l{KEG|c3H5 NGDsbVIxNTJyIN88US=> MYC0POKhcA>? M1q2bYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiZH;z[UBl\XCnbnTlcpRtgQ>? NV76U3FYOjR4NUezPVg>
SK-Hep1 MlHERZBweHSxc3nzJGF{e2G7 MXGwMVIxKM7:TR?= M{Xx[FQ5yqCq MV7pcoR2[2W|IHPlcIwh[XCxcITvd4l{KGSxc3Wg[IVx\W6mZX70cJk> M{L4bVI1PjV5M{m4
H1703 MnfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInkXZVKSzVyPUCuNFUh|ryP NH3lcIMzOzd{OUSwNy=>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 In all tumor models tested thus far, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model, BIBF1120 is highly active at well-tolerated doses (25-100 mg/kg daily p.o.). This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and profound growth inhibition. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[3]
+ 展開

VEGFR2 Kinase Assay:

The cytoplasmic tyrosine kinase domain of VEGFR2 (residues 797-1355 according to sequence deposited in databank SWISS-PROT P35968) is cloned into pFastBac fused to GST and extracted. Enzyme activity is assayed in the presence or absence of serial dilutions of BIBF1120 performed in 25% DMSO. Each microtiter plate contains internal controls such as blank, maximum reaction, and historical reference compound. All incubations are conducted at room temperature on a rotation shaker. 10 μL of each BIBF1120 dilution is added to 10 μL of diluted kinase (0.8 μg/mL VEGFR2, 10 mM Tris pH 7.5, 2 mM EDTA, and 2 mg/mL BSA) and preincubated for 1 hour. The reaction is started by addition of 30 μL of substrate mix containing 62.4 mM Tris pH 7.5, 2.7 mM DTT, 5.3 mM MnCl2, 13.3 mM Mg-acetate, 0.42 mM ATP, 0.83 mg/mL Poly-Glu-Tyr(4:1), and 1.7 μg/mL Poly-Glu-Tyr(4:1)-biotin and incubated for 1 hour. The reaction is stopped by addition of 50 μL of 250 mM EDTA, 20 mM HEPES, pH 7.4. 90 μL of the reaction mix is transferred to a streptavidin plate and incubated for 1-2 hours. After three washes with PBS the EU-labeled antibody, PY20 is added (recommended dilution 1:2000 of 0.5 mg/mL labeled antibody in DELFIA assay buffer). Excessive detection antibody is removed by three washes of DELFIA washing buffer. Then 10 minutes before measurement on the multilabel reader, each well is incubated with 100 μL of DELFIA enhancement solution.
細胞試験: [1]
+ 展開
  • 細胞株: HUVEC, HUASMC, and BRP cell lines
  • 濃度: 50 nM
  • 反応時間: 2 hours
  • 実験の流れ: The cell lines HUVEC, HUASMC, and BRP are used for the assay. BIBF1120 is added to the cultures two hours before the addition of ligands. Cell lysates are generated. Western blotting is done using standard SDS-PAGE methods, loading 50 to 75 μg of protein per lane. Detection is facilitated by enhanced chemiluminescence. Total and phosphorylated mitogen-activated protein kinase (MAPK) is analyzed using monoclonal antibodies M3807 and M8159. Total Akt is detected using the corresponding polyclonal antibody and phosphorylated Akt (Ser473) is analyzed by using its monoclonal antibody. Monoclonal antibody is also used to detect cleaved caspase-3 while KDR (VEGFR2) protein is detected using a corresponding antibody.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 xenografts in Athymic NMRI-nu/nu female mice
  • 製剤: In a 0.5 % Natrosol solution
  • 投薬量: 100 mg/kg
  • 投与方法: p.o.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 6 mg/mL (11.11 mM)
Ethanol 3 mg/mL (5.55 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+40% PEG 300+2% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
0.25mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程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 539.62
化学式

C31H33N5O4

CAS No. 656247-17-5
保管
in solvent
別名 Intedanib

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    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

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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 ( 入力 出力 )

  • 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

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03710824 Not yet recruiting Idiopathic Pulmonary Fibrosis Boehringer Ingelheim December 14 2018 --
NCT03675581 Recruiting Scleroderma Systemic Boehringer Ingelheim November 8 2018 Phase 1
NCT03717012 Not yet recruiting Idiopathic Pulmonary Fibrosis Boehringer Ingelheim November 15 2018 Phase 4
NCT03562416 Not yet recruiting Idiopathic Pulmonary Fibrosis|Lung Transplant; Complications Temple University|Boehringer Ingelheim October 2018 Phase 2
NCT03283007 Not yet recruiting Lung-transplant Recipients Assistance Publique - Hôpitaux de Paris October 2018 Phase 3
NCT03513484 Not yet recruiting Acute Myeloid Leukemia With t(9;11)(p22.3;q23.3); MLLT3-KMT2A|Fibroblast Growth Factor Basic Form Measurement|FLT3 Internal Tandem Duplication|Recurrent Adult Acute Myeloid Leukemia|Refractory Acute Myeloid Leukemia Northwestern University|Robert H. Lurie Cancer Center|Boehringer Ingelheim|National Cancer Institute (NCI) September 30 2018 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

VEGFRシグナル伝達経路

VEGFR Inhibitors with Unique Features

相関VEGFR製品

Tags: Nintedanib (BIBF 1120)を買う | Nintedanib (BIBF 1120) ic50 | Nintedanib (BIBF 1120)供給者 | Nintedanib (BIBF 1120)を購入する | Nintedanib (BIBF 1120)費用 | Nintedanib (BIBF 1120)生産者 | オーダーNintedanib (BIBF 1120) | Nintedanib (BIBF 1120)化学構造 | Nintedanib (BIBF 1120)分子量 | Nintedanib (BIBF 1120)代理店
×

平素は、格別のご愛顧を賜り厚く御礼申し上げます。
誠に勝手ながら、弊社では下記の期間を年末年始による休業とさせていただきます。
【休業期間】
2018年12月29日(土)から2019年1月6日(日)
休業期間中にいただきましたお問合せ等につきましては、2019年1月7日(月)以降の対応とさせていただきます。また、年内の出荷業務は2018年12月26日(水)までとさせていただきます。
ご不便をお掛けいたしますが、ご了承のほど何卒よろしくお願いいたします。

×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID