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SML2848

Sigma-Aldrich

尼达尼布

≥98% (HPLC), powder, VEGFR, PDGFR and FGFR inhibitor

别名:

(3Z)-2,3-二氢-3-[[[4-[甲基[2-(4-甲基-1-哌嗪基)乙酰基]氨基]苯基]氨基]苯基亚甲基]-2-氧代-1H-吲哚-6-羧酸甲酯, (Z)-3-(((4-(N-甲基-2-(4-甲基哌嗪-1-基)乙酰氨基)苯基)氨基)(苯基)亚甲基)-2-氧代二氢吲哚-6-羧酸甲脂, (Z)-3-[(4-{甲基-[2-(4-甲基哌嗪-1-基)乙酰基]氨基}苯基氨基)亚甲基]-2-氧代-2,3-二氢-1H-吲哚-6-羧酸甲酯, BIBF 1120, BIBF-1120, BIBF1120

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About This Item

经验公式（希尔记法）:
C31H33N5O4
CAS号:
656247-17-5
分子量:
539.62
MDL编号:
MFCD11974012
UNSPSC代码:
12352200
NACRES:
NA.77

产品名称

尼达尼布, ≥98% (HPLC)

质量水平

100

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

2-8°C

SMILES字符串

O=C(NC1=C2)/C(C1=CC=C2C(OC)=O)=C(C3=CC=CC=C3)\NC4=CC=C(C=C4)N(C(CN5CCN(CC5)C)=O)C

InChI

1S/C31H33N5O4/c1-34-15-17-36(18-16-34)20-27(37)35(2)24-12-10-23(11-13-24)32-29(21-7-5-4-6-8-21)28-25-14-9-22(31(39)40-3)19-26(25)33-30(28)38/h4-14,19,32H,15-18,20H2,1-3H3,(H,33,38)/b29-28-

InChI key

XZXHXSATPCNXJR-ZIADKAODSA-N

生化/生理作用

口服活性，强效ATP竞争性VEGFR，FGFR，PDGFR，Flt3，Lck，Lyn，Src抑制剂，具有体内抗血管生成和抗纤维化功效。
尼达尼布（BIBF1120）是一种口服活性、强效ATP竞争性抑制剂，可抑制血管激酶VEGFR-1/2/3（IC50 = 34/21/13 nM）、FGFR-1/2/3/4（IC50 = 69/37/108/610 nM）、PDGFRα/β（IC50 = 59/65 nM）以及Flt-3、Lck、Lyn和Src（分别为IC50 = 26、16、195、156 nM），但不抑制33种其他激酶。尼达尼布在体内癌症和肺纤维化的培养物和动物模型中表现出抗血管生成和抗纤维化疗效。

警示用语：

Danger

危险分类

Acute Tox. 3 Oral - Eye Dam. 1 - Repr. 2 - Skin Irrit. 2 - STOT RE 1

储存分类代码

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000264192
0000264193
0000392021
0000373145
0000350334

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Xiaoping Cai et al.
Clinical and experimental pharmacology & physiology, 40(9), 662-670 (2013-07-04)
In the present study, we tested whether serum amyloid A (SAA) protein, an established biomarker of inflammation, also plays a role in stimulating neovascularization. To evaluate this possibility, human carotid artery endothelial (HCtAE) cells were cultured and cellular migration and
Wei-Tien Tai et al.
Journal of hepatology, 61(1), 89-97 (2014-03-25)
Nintedanib, a triple angiokinase inhibitor, is currently being evaluated against advanced HCC in phase I/II clinical trials. Here, we report the underlying molecular mechanism by which nintedanib (BIBF-1120) induces an anti-HCC effect. To further elucidate whether the effect of nintedanib
Kanae Kudo et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 17(6), 1373-1381 (2010-12-07)
BIBF 1120 is a potent, orally available triple angiokinase inhibitor that inhibits VEGF receptors (VEGFR) 1, 2, and 3, fibroblast growth factor receptors, and platelet-derived growth factor receptors. This study examined the antitumor effects of BIBF 1120 on hepatocellular carcinoma
Emma Kulimova et al.
Molecular cancer therapeutics, 5(12), 3105-3112 (2006-12-19)
In acute myeloid leukemia (AML), receptor tyrosine kinase ligands promote growth and survival and contribute to AML-associated marrow neoangiogenesis. We have tested simultaneous inhibition of vascular endothelial growth factor, fibroblast growth factor, and platelet-derived growth factor receptor signaling by novel
Katrin E Hostettler et al.
Respiratory research, 15(1), 157-157 (2014-12-17)
Idiopathic pulmonary fibrosis (IPF) is a progressive lung disease with poor prognosis. The kinase inhibitor nintedanib specific for vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR) and fibroblast growth factor receptor (FGFR) significantly reduced the rate of
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