尼达尼布 (BIBF 1120)

强效的VEGFR，PDGFR和FGFR抑制剂

规格或纯度: ≥98%

CAS编号: 656247-17-5
分子式: C₃₁H₃₃N₅O₄
分子量: 539.62
PubChem编号: 135423438

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货号 (SKU)	包装规格	是否现货
N129725-5mg	5mg	现货
N129725-10mg	10mg	现货
N129725-25mg	25mg	现货
N129725-50mg	50mg	现货
N129725-100mg	100mg	现货
N129725-500mg	500mg	现货
N129725-1g	1g	现货

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fibroblast growth factor receptor 1 Inhibitor fibroblast growth factor receptor 2 Inhibitor fibroblast growth factor receptor 3 Inhibitor fibroblast growth factor receptor 4 Inhibitor fms related receptor tyrosine kinase 1 Inhibitor fms related receptor tyrosine kinase 4 Inhibitor kinase insert domain receptor Inhibitor platelet derived growth factor receptor alpha Inhibitor platelet derived growth factor receptor beta Inhibitor

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基本描述

别名	尼达尼布
英文别名	BIBF 1120\|BDBM445209\|Nintedanib (BIBF 1120)\|Methyl (3Z)-3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylidene)-2-oxo-2,3-dihydro-1h-indole-6-carboxylate\|1H-Indole-6-carboxylic acid, 2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-
规格或纯度	≥98%
英文名称	Nintedanib (BIBF 1120)
生化机理	血管内皮生长因子受体（VEGFRs），血小板源性生长因子受体（PDGFRs）和成纤维细胞生长因子受体（FGFRs）的有效抑制剂（VEGFR亚型的IC50值为13-34 nM，PDGFR亚型的IC50值为59-65 nM，37- FGFR亚型为108 nM）。还抑制Flt-3，Lck，Lyn和Src（IC50值为25-200 nM）。抑制VEGF刺激的内皮细胞，PDGF刺激的周细胞和血管平滑肌细胞的增殖。在小鼠肿瘤异种移植模型中降低血管密度和完整性，并抑制肿瘤生长。
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	Nintedanib (BIBF 1120)是一种有效的三重血管激酶抑制剂，对VEGFR1/2/3， FGFR1/2/3和PDGFRα/β均有抑制作用，其IC50分别为34 nM/13 nM/13 nM， 69 nM/37 nM/108 nM和59 nM/65 nM。BIBF1120 is a potent kinase inhibitor found to affect VEGF, PDGF, and FGF receptors. Nintedanib (BIBF 1120) is a 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. BIBF1120 is a potent kinase inhibitor found to affect VEGF, PDGF, and FGF receptors.

名称和标识符

IUPAC Name	methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate
INCHI	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/h4-14,19,33,38H,15-18,20H2,1-3H3
InChi Key	CPMDPSXJELVGJG-UHFFFAOYSA-N
Canonical SMILES	CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)N=C(C3=CC=CC=C3)C4=C(NC5=C4C=CC(=C5)C(=O)OC)O
Isomeric SMILES	CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)N=C(C3=CC=CC=C3)C4=C(NC5=C4C=CC(=C5)C(=O)OC)O
关联CAS	928326-83-4
PubChem CID	135423438
分子量	539.62

数据库链接

PubChem CID	135423438
ChEMBL Ligand	CHEMBL502835
CAS Registry No.	656247-17-5
DiscoveRx TREEspot	BIBF-1120%20(derivative)\|
Wikipedia	Nintedanib
RCSB PDB Ligand	XIN
PEP	nintedanib
Reactome Reaction	R-HSA-2077420, R-HSA-9674430, R-HSA-9674095
Reactome Drug	R-ALL-9616923
DrugCentral Ligand	4903

PubChem CID

135423438

ChEMBL Ligand

CHEMBL502835

CAS Registry No.

656247-17-5

DiscoveRx TREEspot

BIBF-1120%20(derivative)|

Wikipedia

Nintedanib

RCSB PDB Ligand

XIN

PEP

nintedanib

Reactome Reaction

R-HSA-2077420, R-HSA-9674430, R-HSA-9674095

Reactome Drug

R-ALL-9616923

DrugCentral Ligand

4903

溶解性	溶于DMSO

安全和危险性（GHS）

象形图	Health Hazard
信号词	Danger
危险声明	H373: Causes damage to organs through prolonged or repeated exposure H360: May damage fertility or the unborn child
预防措施声明	P280,P405,P501,P260,P203,P318,P319

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参考文献

1. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J et al.. (2008) BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.. Cancer Res, 68 (12): (4774-82). [PMID:18559524]
2. Stopfer P, Rathgen K, Bischoff D, Lüdtke S, Marzin K, Kaiser R, Wagner K, Ebner T. (2011) Pharmacokinetics and metabolism of BIBF 1120 after oral dosing to healthy male volunteers.. Xenobiotica, 41 (4): (297-311). [PMID:21204634]
3. Dimitroulis IA. (2014) Nintedanib: a novel therapeutic approach for idiopathic pulmonary fibrosis.. Respir Care, 59 (9): (1450-5). [PMID:24782550]
4. Hunninghake GM. (2014) A new hope for idiopathic pulmonary fibrosis.. N Engl J Med, 370 (22): (2142-3). [PMID:24836311]

尼达尼布 (BIBF 1120)

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基本描述

名称和标识符

数据库链接

化学和物理性质

安全和危险性（GHS）

质检证书(COA)

质检报告(COA)

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质检报告COA

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