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Merck
모든 사진(1)

주요 문서

SML2848

Sigma-Aldrich

Nintedanib

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

동의어(들):

(3Z)-2,3-Dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-1H-indole-6-carboxylic acid methyl ester, (Z)-3-[(4-{Methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino}phenylamino)methylene]-2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester, BIBF 1120, BIBF-1120, BIBF1120, Methyl (Z)-3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate

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About This Item

실험식(Hill 표기법):
C31H33N5O4
CAS Number:
Molecular Weight:
539.62
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

제품명

Nintedanib, ≥98% (HPLC)

Quality Level

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°C

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

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

생화학적/생리학적 작용

Nintedanib (BIBF1120) is an orally active, potent ATP-competitive inhibitor against angiokinases 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), as well as Flt-3, Lck, Lyn, and Src (IC50 = 26, 16, 195, 156 nM, repectively), but not 33 other kinases. Nintedanib exhibits antiangiogenic and antifibrotic efficacy in cultures and in animal models of cancers and pulmonary fibrosis in vivo.
Orally active, potent ATP-competitive VEGFR, FGFR, PDGFR, Flt3, Lck, Lyn, Src inhibitor with in vivo antiangiogenic and antifibrotic efficacy.

픽토그램

Skull and crossbonesHealth hazardCorrosion

신호어

Danger

유해 및 위험 성명서

Hazard Classifications

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

Storage Class Code

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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시험 성적서(COA)

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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
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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
Raquel Frenedoso da Silva et al.
Cell and tissue research, 379(2), 407-420 (2019-09-02)
The antiangiogenic therapy for prostate cancer with Nintedanib, a potent inhibitor of important growth factor receptors, has been proven to delay tumor progression and arrest tumor growth; thus, the aim herein is to evaluate Nintedanib effects on tumor cells, besides angiogenesis
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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