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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:
分子量:
539.62
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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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

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


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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
Roman C Brands et al.
Oncology letters, 18(3), 2220-2231 (2019-08-28)
Multidrug resistance (MDR) remains one of the major causes of suboptimal outcome following therapy in head and neck squamous cell carcinoma (HNSCC). ATP-binding cassette (ABC) transporters are overexpressed in HNSCC, which contributes to the limited effect of chemotherapeutic treatment. In
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
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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