Nintedanib (BIBF 1120)
製品コードS1010 別名：Intedanib
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.
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カスタマーフィードバック(8)
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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.
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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.
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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.
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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. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| 細胞データ |
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| 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] |
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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. |
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| 細胞試験： [1] |
+ 展開
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| 動物試験：[1] |
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溶解度 (25°C)
| 体外 | DMSO | 6 mg/mL (11.11 mM) |
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| 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 |
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| 化学式 | C31H33N5O4 |
| CAS No. | 656247-17-5 |
| 保管 | 粉 |
| in solvent | |
| 別名 | Intedanib |
便利ツール
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
*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
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 )
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。
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：
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
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 |
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