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Protein Tyrosine Kinase
VEGFR inhibitor
-
FGFR inhibitor
-
PDGFR inhibitor
-
Src inhibitor
Nintedanib
僅限科研使用
Nintedanib
別名: BIBF 1120, Intedanib 中文名稱：尼達(dá)尼布
Nintedanib尼達(dá)尼布是一種有效的三重血管激酶抑制劑，作用于VEGFR1/2/3， FGFR1/2/3和PDGFRα/β，在無細(xì)胞試驗(yàn)中IC50分別為34 nM/13 nM/13 nM， 69 nM/37 nM/108 nM和59 nM/65 nM。Phase 3。
Nintedanib Chemical Structure
CAS: 656247-17-5
產(chǎn)品質(zhì)控
批次：
純度：
99.98%
99.98
Nintedanib相關(guān)產(chǎn)品
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息 |
|---|---|---|---|---|---|
| PLC5 | Cell Viability Assay | 0-20 μM | 48?h | decreases cell viability dose dependently | 24657398 |
| HepG2 | Cell Viability Assay | 0-20 μM | 48?h | decreases cell viability dose dependently | 24657398 |
| Hep3B | Cell Viability Assay | 0-20 μM | 48?h | decreases cell viability dose dependently | 24657398 |
| A549 | Function Assay | 5?μM | 0-1 h | increases AP-1 activation after 30 min | 25843005 |
| A549 | Function Assay | 0.01–5?μM | 72 h | enhances SP-D protein expression in a dose-dependent manner at concentrations of up to 5?μM? | 25843005 |
| A549 | Function Assay | 0.01–5?μM | 24 h | induces SFTPD?mRNA expression dose dependently | 25843005 |
| Mia-Paca2 | Function Assay | 2/5 μM | 24 h | has a general EMT reversal effect? | 26061747 |
| T24 | Function Assay | 2/5 μM | 24 h | has a general EMT reversal effect? | 26061747 |
| A549 | Function Assay | 2/5 μM | 24 h | has a general EMT reversal effect? | 26061747 |
| SKOV3 | Function Assay | 5 μM | 24 h | induces a significant increase in the promoter activities of E-cad,?CDH1, and?CDH3 | 26061747 |
| HuH7 | Cell Viability Assay | 0-20 μM | 48?h | decreases cell viability dose dependently | 24657398 |
| SK-Hep1 | Cell Viability Assay | 0-20 μM | 48?h | decreases cell viability dose dependently | 24657398 |
| Hep3B | Apoptosis Assay | 0-20 μM | 48?h | induces cell apoptosis dose dependently | 24657398 |
| HepG2 | Apoptosis Assay | 0-20 μM | 48?h | induces cell apoptosis dose dependently | 24657398 |
| PLC5 | Apoptosis Assay | 0-20 μM | 48?h | induces cell apoptosis dose dependently | 24657398 |
| HuH7 | Apoptosis Assay | 0-20 μM | 48?h | induces cell apoptosis dose dependently | 24657398 |
| SK-Hep1 | Apoptosis Assay | 0-20 μM | 48?h | induces cell apoptosis dose dependently | 24657398 |
| NIH3T3 | Function assay | 50 nM | 1 hr | Inhibition of VEGFR2 transfected in mouse NIH3T3 cells at 50 nM incubated for 1 hr measured after 32 hrs washout followed by VEGF stimulation for 10 mins by Western blotting | 18559524 |
| Sf9 | Function assay | 20 mins | Inhibition of mouse GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting, IC50 = 0.013 μM. | 18559524 | |
| Sf9 | Function assay | 20 mins | Inhibition of human GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting, IC50 = 0.021 μM. | 18559524 | |
| HT-29 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 4.9 μM. | 28190652 | |
| SKOV3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay, IC50 = 28.76 μM. | 28190652 | |
| BL21 (DE3) | Function assay | 30 mins | Inhibition of His6-tagged MELK catalytic domain (1 to 340 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using Bcl-GL as substrate measured after 30 mins in presence of [gamma32P]ATP by liquid scintillation counting method, Ki = 0.0056 μM. | 28351607 | |
| BL21 (DE3) | Function assay | 30 mins | Inhibition of His6-tagged MELK catalytic domain (1 to 340 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using Bcl-GL as substrate measured after 30 mins in presence of [gamma32P]ATP by liquid scintillation counting method, IC50 = 0.043 μM. | 28351607 | |
| HT-29 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.83 μM. | 28826084 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 8.28 μM. | 28826084 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 22.62 μM. | 28826084 | |
| NIH/3T3 | Function assay | 42 hrs | Inhibition of PDGFR in mouse NIH/3T3 cells assessed as reduction in recombinant human PDGF-BB-induced cell proliferation after 42 hrs by cell titer 96 aqueous one solution based assay, IC50 = 0.085 μM. | 29152045 | |
| NIH3T3 | Function assay | 1 hr | Inhibition of VEGF-stimulated human VEGFR2 phosphorylation expressed in mouse NIH3T3 cells pretreated for 1 hr measured 32 hrs after drug dose by immunoprecipitation based pulse-chase experiment | 19522465 | |
| H1703 | Growth Inhibition Assay | IC50=0.05 μM | 23729403 | ||
| Sf9 | Function assay | Inhibition of human VEGFR2 expressed in Sf9 cells, IC50 = 0.005 μM. | 19522465 | ||
| BRP | Apoptosis assay | Induction of apoptosis in BRP cells assessed as caspase-3 cleavage | 19522465 | ||
| BRP | Antiangiogenic assay | Antiangiogenic activity BRP cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay | 19522465 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Nintedanib尼達(dá)尼布是一種有效的三重血管激酶抑制劑，作用于VEGFR1/2/3， FGFR1/2/3和PDGFRα/β，在無細(xì)胞試驗(yàn)中IC50分別為34 nM/13 nM/13 nM， 69 nM/37 nM/108 nM和59 nM/65 nM。Phase 3。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶點(diǎn) |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | BIBF1120對(duì)酪氨酸激酶受體如EGFR, HER2, InsR, IGF1R 或者細(xì)胞周期激酶 CDK1, CDK2 和CDK4抑制效果不大， IC50都大于1x103nM。BIBF1120強(qiáng)抑制VEGF-刺激的HUVEC 和VEGF-刺激的HSMEC，EC50分別為9 和 7 nM。相反，BIBF1120 作用于FaDu, Calu-6 和Hela時(shí)EC50則大到幾百倍。[1] |
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|---|---|---|---|---|
| 激酶實(shí)驗(yàn) | 激酶實(shí)驗(yàn) | |||
| VEGFR-2的胞質(zhì)酪氨酸激酶域克隆到pFastBac載體上，與谷胱甘肽巰基轉(zhuǎn)移酶 (GST)相融合。 GST融合蛋白在SF-9昆蟲細(xì)胞中表達(dá)，用重元素萃取分離法提取。HEPEX萃取液包括20 mM HEPES （pH 為7.4）, 100 mM NaCl, 10 mM ss-甘油磷酸鹽, 10 mM 聚硝基磷酸單苯酯, 30mM NaF, 5 mM EDTA, 5% 甘油, 1% Triton X-100, 1 mM Na3VO4, 0.1% SDS, 0.5μg/ml 抑肽素A, 2.5 μg/ml 3,4-二氯異香豆素(絲氨酸蛋白酶的不可逆抑制劑), 2.5 μg/ml反式-環(huán)氧琥珀酰-L-亮氨酰-L-氨基丁烷, 20 KIU/ml 抑肽酶, 2 μg/ml 亮抑肽酶, 1 mM苯甲脒，和0.002% PMSF。谷氨酸和酪氨酸按4:1比例隨機(jī)組成的聚合物作為基底物，每組50ul的反應(yīng)液包括5 % DMSO, 40 mM HEPES （pH 為 7.4）, 5 mM MgCl2, 5 mM MnCl2, 0.5 mg/ml 聚谷氨酸/酪氨酸, 0.05% Triton X-100, 100 μM ATP, 1 μCi [γ-33P]ATP ，和 10 μl酶制劑。實(shí)驗(yàn)在室溫下進(jìn)行20分鐘，最后加入10 μl 5 % H3PO4終止反應(yīng)。沉淀物轉(zhuǎn)移到GF/B 過濾器中，使用與96孔過濾器相配的萬能采集器收集。通過閃爍計(jì)數(shù)器測(cè)定混合物的放射能。 | ||||
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | HUVEC, HUASMC,和BRP細(xì)胞系 | ||
| 濃度 | 50 nM | |||
| 孵育時(shí)間 | 2小時(shí) | |||
| 方法 | 不同的腫瘤細(xì)胞系在96孔板上培養(yǎng)24小時(shí)。然后加入不同濃度的BIBF1120，處理72小時(shí)。通過Alamar-Blue染色的熒光強(qiáng)度測(cè)試EC50值。 |
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| 實(shí)驗(yàn)圖片 | 檢測(cè)方法 | 檢測(cè)指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | p-EGFR / FGFR1 / p-AKT / AKT / p-ERK / ERK Cyclin A / Cyclin D1 / Cyclin E / CDK2 / CDK4 / CDK6 p-SMAD3 / SMAD3 / p-p38 MAPK / p38 MAPK Fibronectin / Collagen 1a1 |
|
27581340 | |
| Immunofluorescence | Vimentin / E-cadherin |
|
29934570 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 在小鼠的Fadu 移植瘤中，按鼠體重，每千克處理100mg BIBF1120,結(jié)果顯示腫瘤血管密度降低76%。BIBF1120 作用于移植瘤模型Caki-1, HT-29, SKOV-3, Calu6 和PAC-120同樣有顯著的抑制效果。BIBF1120已用于治療多種癌癥，包括：非小細(xì)胞肺癌，前列腺癌，卵巢癌，及結(jié)腸直腸癌。且BIBF1120目前處于二期臨床實(shí)驗(yàn)階段。[1] |
|
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | 雌性無胸腺NMRI-nu/nu鼠 |
| Dosages | 100 mg/kg | |
| Administration | 口服處理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06200714 | Recruiting | Idiopathic Pulmonary Fibrosis|Diarrhoea |
Boehringer Ingelheim |
April 30 2024 | -- |
| NCT05676112 | Withdrawn | Pulmonary Fibrosis |
Boehringer Ingelheim|China-Japan Friendship Hospital |
December 29 2023 | -- |
| NCT06070610 | Completed | Healthy |
Boehringer Ingelheim |
November 8 2023 | Phase 1 |
| NCT05755308 | Not yet recruiting | Idiopathic Pulmonary Fibrosis |
Fondazione Policlinico Universitario Agostino Gemelli IRCCS |
October 2023 | Not Applicable |
| NCT06071013 | Not yet recruiting | Non-small Cell Lung Cancer|EGFR Gene Mutation|EGFR-TKI Resistant Mutation |
China Medical University Hospital |
September 28 2023 | Phase 1|Phase 2 |
化學(xué)信息&溶解度
| 分子量 | 539.62 | 分子式 | C31H33N5O4 |
| CAS號(hào) | 656247-17-5 | SDF | Download Nintedanib SDF |
| Smiles | CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)N=C(C3=CC=CC=C3)C4=C(NC5=C4C=CC(=C5)C(=O)OC)O | ||
| 儲(chǔ)存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 10 mg/mL ( (18.53 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
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體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | ||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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