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Merck
CN

SML2848

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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关于此项目

经验公式（希尔记法）:
C31H33N5O4
化学文摘社编号:
656247-17-5
分子量:
539.62
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD11974012

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产品名称

尼达尼布, ≥98% (HPLC)

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

SMILES string

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

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

相关类别

Biochem/physiol Actions

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。

signalword

Danger

Hazard Classifications

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

存储类别

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

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000478596
0000478595
0000478595
0000478596
0000419700

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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
Elaine Reguera-Nuñez et al.
Angiogenesis, 22(4), 535-546 (2019-08-30)
In contrast to VEGF pathway-targeting antibodies, antiangiogenic tyrosine kinase inhibitors (TKIs) have failed to meet primary endpoints in almost all phase III clinical trials when combined with conventional chemotherapy. One exception is the combination of nintedanib and docetaxel as a
Gerald J Roth et al.
Journal of medicinal chemistry, 52(14), 4466-4480 (2009-06-16)
Inhibition of tumor angiogenesis through blockade of the vascular endothelial growth factor (VEGF) signaling pathway is a new treatment modality in oncology. Preclinical findings suggest that blockade of additional pro-angiogenic kinases, such as fibroblast and platelet-derived growth factor receptors (FGFR
Frank Hilberg et al.
Cancer research, 68(12), 4774-4782 (2008-06-19)
Inhibition of tumor angiogenesis through blockade of the vascular endothelial growth factor (VEGF) signaling pathway is a novel treatment modality in oncology. Preclinical findings suggest that long-term clinical outcomes may improve with blockade of additional proangiogenic receptor tyrosine kinases: platelet-derived
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