Nintedanib (BIBF 1120)

目录号:S1010 别名: Intedanib

Nintedanib (BIBF 1120) Chemical Structure

Molecular Weight(MW): 539.62

Nintedanib (BIBF 1120)是一种有效的三重血管激酶抑制剂,作用于VEGFR1/2/3FGFR1/2/3PDGFRα/β,在无细胞试验中IC50分别为34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM和59 nM/65 nM。Phase 3。

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客户使用该产品的7个实验数据:

  • 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.

    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.

  • 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.

  • 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.

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

产品描述 Nintedanib (BIBF 1120)是一种有效的三重血管激酶抑制剂,作用于VEGFR1/2/3FGFR1/2/3PDGFRα/β,在无细胞试验中IC50分别为34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM和59 nM/65 nM。Phase 3。
靶点
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
体外研究

BIBF1120对酪氨酸激酶受体如EGFR, HER2, InsR, IGF1R 或者细胞周期激酶 CDK1, CDK2 和CDK4抑制效果不大, IC50都大于1x103nM。BIBF1120强抑制VEGF-刺激的HUVEC 和VEGF-刺激的HSMEC,EC50分别为9 和 7 nM。相反,BIBF1120 作用于FaDu, Calu-6 和Hela时EC50则大到几百倍。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKOV3 M4DNUGZ2dmO2aX;uJGF{e2G7 NG[4Slk2KML3TR?= Mn7qNlQhcA>? M1jNRWROW09? NHfBZnBqdmS3Y3XzJIEhe2mpbnnmbYNidnRiaX7jdoVie2ViaX6geIhmKHC{b33veIVzKGGldHn2bZRq\XNib3[gSU1k[WRuwrDDSGgyNCCjbnVCpGNFUDN? M4fx[FI3ODZzN{S3
A549 MUTGeY5kfGmxbjDBd5NigQ>? NVOwRotMOi93IN88US=> MXqyOEBp NUPBfmJWTE2VTx?= NHLLXWNp[XNiYTDn[Y5memGuIFXNWEBz\X[ncoPhcEBm\m[nY4VCpC=> NEjKV48zPjB4MUe0Oy=>
T24 NFvXUnBHfW6ldHnvckBCe3OjeR?= MUeyM|Uh|ryP NHznO2wzPCCq M2jNWWROW09? M{TYVYhieyCjIHflcoVz[WxiRV3UJJJmfmW{c3HsJIVn\mWldNMg M2nhVlI3ODZzN{S3
Mia-Paca2 M4rDN2Z2dmO2aX;uJGF{e2G7 NXTad3Q5Oi93IN88US=> Ml7kNlQhcA>? NWrWN3VsTE2VTx?= Mm\FbIF{KGFiZ3Xu[ZJidCCHTWSgdoV3\XK|YXyg[YZn\WO2wrC= NIfGRWMzPjB4MUe0Oy=>
A549 M2npdmZ2dmO2aX;uJGF{e2G7 MXGwMlAy6oDVNdMg{txO NVzBRmIzOjRiaB?= M1noWGROW09? M{fteYlv\HWlZYOgV2ZVWEUEoH3SUmEh\XiycnXzd4lwdiCmb4PlJIRmeGWwZHXueIx6 NFfTO4MzPTh2M{CwOS=>
A549 NE\vPIxHfW6ldHnvckBCe3OjeR?= M4\HTVAvODIkgKO1xsDPxE1? NFXuRoE4OiCq MYLEUXNQ Mn74[Y5p[W6lZYOgV3AuTCCycn;0[YlvKGW6cILld5Nqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJiYYSgZ49v[2WwdILheIlwdnNib3[geZAhfG9iNdMg{txOyqB? NXq1OJpyOjV6NEOwNFU>
A549 MX3GeY5kfGmxbjDBd5NigQ>? NGPDV|U2yqEQvF2= Mlf3NE0yKGh? NVnUZ4FuTE2VTx?= M3;3bYlv[3KnYYPld{BCWC1zIHHjeIl3[XSrb36gJIFnfGW{IEOwJI1qdg>? NGnkTXAzPTh2M{CwOS=>
Hep3B NHfEVZlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWHwfZJoOC1{MDFOwG0> Mn60OFjDqGh? NVftc4Vv\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= MX[yOFY2PzN7OB?=
HepG2 MkmzR4VtdCCYaXHibYxqfHliQYPzZZk> MX:wMVIxKM7:TR?= NEPCbWI1QMLiaB?= M2nad4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NWPONpd5OjR4NUezPVg>
PLC5 NEXEdXZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mn3DNE0zOCEQvF2= NVf1fGc2PDkEoHi= NYm5b4Vs\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= M3HyXFI1PjV5M{m4
HuH7 M{\mNmNmdGxiVnnhZoltcXS7IFHzd4F6 NE[zWZUxNTJyIN88US=> MVi0POKhcA>? NHTqOmRl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NH;VRXAzPDZ3N{O5PC=>
SK-Hep1 NFTJSFFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4i3WVAuOjBizszN M1r0SlQ5yqCq Mmm3[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MVGyOFY2PzN7OB?=
Hep3B NVXS[IxsSXCxcITvd4l{KEG|c3H5 NV\tS|RlOC1{MDFOwG0> NHHkS401QMLiaB?= MYDpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGSxc3Wg[IVx\W6mZX70cJk> MWmyOFY2PzN7OB?=
HepG2 NYHLTZc{SXCxcITvd4l{KEG|c3H5 M{C1UFAuOjBizszN M{HRZlQ5yqCq NIDqN2JqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHTvd4Uh\GWyZX7k[Y51dHl? MlPUNlQ3PTd|OUi=
PLC5 NXfNPW1SSXCxcITvd4l{KEG|c3H5 MUOwMVIxKM7:TR?= MVO0POKhcA>? MXPpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGSxc3Wg[IVx\W6mZX70cJk> M1P5VVI1PjV5M{m4
HuH7 MkjkRZBweHSxc3nzJGF{e2G7 NEL4bHoxNTJyIN88US=> NFrlOZM1QMLiaB?= M3jme4lv\HWlZYOgZ4VtdCCjcH;weI9{cXNiZH;z[UBl\XCnbnTlcpRtgQ>? M4Xze|I1PjV5M{m4
SK-Hep1 M3\CdmFxd3C2b4Ppd{BCe3OjeR?= Mm\oNE0zOCEQvF2= MYO0POKhcA>? NV;CZWNJcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MnL5NlQ3PTd|OUi=
H1703 NWLmTYZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHRfWFKSzVyPUCuNFUh|ryP NIiwPYkzOzd{OUSwNy=>

... Click to View More Cell Line Experimental Data

体内研究 在小鼠的Fadu 移植瘤中,按鼠体重,每千克处理100mg BIBF1120,结果显示肿瘤血管密度降低76%。BIBF1120 作用于移植瘤模型Caki-1, HT-29, SKOV-3, Calu6 和PAC-120同样有显著的抑制效果。BIBF1120已用于治疗多种癌症,包括:非小细胞肺癌,前列腺癌,卵巢癌,及结肠直肠癌。且BIBF1120目前处于二期临床实验阶段。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
+ 展开

激酶实验:

VEGFR-2的胞质酪氨酸激酶域克隆到pFastBac载体上,与谷胱甘肽巯基转移酶 (GST)相融合。 GST融合蛋白在SF-9昆虫细胞中表达,用重元素萃取分离法提取。HEPEX萃取液包括20 mM HEPES (pH 为7.4), 100 mM NaCl, 10 mM ss-甘油磷酸盐, 10 mM 聚硝基磷酸单苯酯, 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 3,4-二氯异香豆素(丝氨酸蛋白酶的不可逆抑制剂), 2.5 μg/ml反式-环氧琥珀酰-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比例随机组成的聚合物作为基底物,每组50ul的反应液包括5 % DMSO, 40 mM HEPES (pH 为 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酶制剂。实验在室温下进行20分钟,最后加入10 μl 5 % H3PO4终止反应。沉淀物转移到GF/B 过滤器中,使用与96孔过滤器相配的万能采集器收集。通过闪烁计数器测定混合物的放射能。
细胞实验:[1]
+ 展开
  • Cell lines: HUVEC, HUASMC,和BRP细胞系
  • Concentrations: 50 nM
  • Incubation Time: 2小时
  • Method: 不同的肿瘤细胞系在96孔板上培养24小时。然后加入不同浓度的BIBF1120,处理72小时。通过Alamar-Blue染色的荧光强度测试EC50值。
    (Only for Reference)
动物实验:[1]
+ 展开
  • Animal Models: 雌性无胸腺NMRI-nu/nu鼠
  • Formulation: 溶于0.5%羟乙基纤维素溶液中
  • Dosages: 100 mg/kg
  • Administration: 口服处理
    (Only for Reference)

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 从左到右依次加入纯溶剂:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 539.62
化学式

C31H33N5O4

CAS号 656247-17-5
稳定性 powder
别名 Intedanib

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02393755 Recruiting Colon Adenocarcinoma|Rectal Adenocarcinoma|Recurrent Colon Carcinoma|Recurrent Rectal Carcinoma|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer Roswell Park Cancer Institute|National Cancer Institute (NCI)|Boehringer Ingelheim|National Comprehensive Cancer Network May 8, 2015 Phase 1|Phase 2
NCT02863055 Not yet recruiting Malignant Pleural Mesothelioma European Organisation for Research and Treatment of Cancer - EORTC February 2017 Phase 2
NCT02999178 Recruiting Lung Diseases, Interstitial Boehringer Ingelheim January 2017 Phase 3
NCT02902484 Not yet recruiting Cancer of Pancreas University of Texas Southwestern Medical Center|Boehringer Ingelheim|The University of Texas Health Science Center at San Antonio|South Plains Oncology Consortium January 2017 Phase 1|Phase 2
NCT02808247 Not yet recruiting Sarcoma, Soft Tissue European Organisation for Research and Treatment of Cancer - EORTC|Boehringer Ingelheim January 2017 Phase 2
NCT02856867 Not yet recruiting Esophagogastric Adenocarcinoma|Metastatic Disease|No Previous Chemotherapy for Metastatic Esophagogastric Cancer European Organisation for Research and Treatment of Cancer - EORTC December 2016 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID