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Nintedanib

尼达尼布,Intedanib,BIBF-1120,BIBF 1120

Nintedanib (BIBF 1120)是三重血管激酶抑制剂，对VEGFR1/2/3，FGFR1/2/3和PDGFRα/β的IC50分别为34 nM/13 nM/13 nM，69 nM/37 nM/108 nM和59NM。

目录号
EY0907
EY0907
EY0907
纯度
98.95%
98.95%
98.95%
规格
5 mg
10 mg
25 mg
原价
580.00_
840.00_
1680.00_
售价
580.00_
840.00_
1680.00_
库存
现货
现货
现货
订购
订购
订购
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  • 生物活性

    BIBF 1120 is an oral bioactive, 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 addition, BIBF1120 suppresses the FGFR subtypes with IC50 of 60, 37 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.

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% propylene glycol

  • 激酶实验

  • 细胞实验

    50 nM

  • 动物实验

    100 mg/kg 口服处理

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Hilberg F, et al. Cancer Res, 2008, 68(12), 4774-4782.

    分子式
    C31H33N5O4    		 分子量
    539.62    		 CAS号
    656247-17-5    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    5 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    2 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02598193 Idiopathic Pulmonary Fibrosis Drug: Nintedanib|Drug: Pirfenidone Hoffmann-La Roche Phase 4 2016-01-14 2017-03-08
    NCT02835833 Renal Cell Carcinoma|Colorectal Adenocarcinoma|Non-squamous Non-small Cell Lung Cancer|Platinum-refractory Ovarian Carcinoma|Cervical Carcinoma Drug: Nintedanib|Drug: Bevacizumab University of Alabama at Birmingham|Boehringer Ingelheim Phase 1 2016-06-01 2017-01-19
    NCT02558387 Recurrent or Metastatic Salivary Gland Cancer of the Head and Neck Drug: BIBF1120 Samsung Medical Center Phase 2 2014-11-01 2015-11-18
    NCT02902484 Cancer of Pancreas Drug: Nintedanib University of Texas Southwestern Medical Center|Boehringer Ingelheim|The University of Texas Health Science Center at San Antonio|South Plains Oncology Consortium Phase 1|Phase 2 2017-01-01 2016-11-22
    NCT01788982 Medullary Thyroid Cancer (MTC)|Differentiated Thyroid Cancer (DTC) Drug: Nintedanib|Drug: Placebo European Organisation for Research and Treatment of Cancer - EORTC Phase 2 2014-05-01 2016-10-11
    NCT02389764 Breast Cancer Drug: BIBF 1120|Behavioral: Phone Call M.D. Anderson Cancer Center|Boehringer Ingelheim Phase 2 2015-06-01 2016-12-15
    NCT02234596 Esophagogastric Adenocarcinoma Drug: Nintedanib Memorial Sloan Kettering Cancer Center Phase 2 2014-09-01 2017-01-17
    NCT03062943 Lymphangioleiomyomatosis Drug: Nintedanib IRCCS Multimedica Phase 2 2016-10-01 2017-02-20
    NCT02299141 Carcinoma, Non-Small-Cell Lung|Non-Small Cell Lung Cancer|Nonsmall Cell Lung Cancer Drug: Nintedanib Washington University School of Medicine|National Comprehensive Cancer Network Phase 1 2015-05-07 2017-02-22
    NCT02579603 Idiopathic Pulmonary Fibrosis Drug: Nintedanib|Drug: Pirfenidone Boehringer Ingelheim Phase 4 2015-10-01 2017-01-25
    NCT02225405 Lung Cancer Drug: Nintedanib|Drug: Cisplatin|Drug: Docetaxel M.D. Anderson Cancer Center|Boehringer Ingelheim Phase 1 2015-04-01 2017-03-08
    NCT02152059 Small Cell Lung Cancer|Platinum-sensitive Drug: BIBF1120 AHS Cancer Control Alberta|Cross Cancer Institute|Boehringer Ingelheim Phase 2 2014-07-01 2016-07-04
    NCT02808247 Sarcoma, Soft Tissue Drug: Nintedanib|Drug: Ifosfamide European Organisation for Research and Treatment of Cancer - EORTC|Boehringer Ingelheim Phase 2 2017-01-01 2016-06-17
    NCT02568449 Recurrent Pleural Malignant Mesothelioma|Stage IV Pleural Mesothelioma Drug: Nintedanib Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) Phase 2 2015-10-01 2016-12-14
    NCT02308553 Cutaneous Malignant Melanoma Drug: Nintedanib|Drug: Nintedanib-Placebo|Drug: Paclitaxel Prof. Dr. med. Dirk Schadendorf|Boehringer Ingelheim|medac GmbH|Alcedis GmbH|University Hospital, Essen Phase 1|Phase 2 2015-01-01 2016-09-12
    NCT02572752 Healthy Drug: Nintedanib|Drug: Nintedanib|Drug: Nintedanib Boehringer Ingelheim Phase 1 2015-08-01 2016-11-08

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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