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Merck
모든 사진(1)

문서

448101

Sigma-Aldrich

Met Kinase Inhibitor

The Met Kinase Inhibitor, also referenced under CAS 658084-23-2, controls the biological activity of Met Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

동의어(들):

Met Kinase Inhibitor, (3Z)-N-(3-Chlorophenyl)-3-((3,5-dimethyl-4-((4-methylpiperazin-1-yl)carbonyl)-1H-pyrrol-2-yl)methylene)-N-methyl-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide, SU11274

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About This Item

실험식(Hill 표기법):
C28H30ClN5O4S
CAS Number:
Molecular Weight:
568.09
MDL number:
UNSPSC 코드:
12352200

Quality Level

분석

≥98% (HPLC)

형태

powder
solid

제조업체/상표

Calbiochem®

저장 조건

OK to freeze
protect from light

색상

orange

solubility

DMSO: 1 mg/mL

배송 상태

ambient

저장 온도

2-8°C

InChI

1S/C28H30ClN5O4S/c1-17-25(30-18(2)26(17)28(36)34-12-10-32(3)11-13-34)16-23-22-15-21(8-9-24(22)31-27(23)35)39(37,38)33(4)20-7-5-6-19(29)14-20/h5-9,14-16,30H,10-13H2,1-4H3,(H,31,35)/b23-16-

InChI key

FPYJSJDOHRDAMT-KQWNVCNZSA-N

일반 설명

A cell-permeable pyrrole indolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of Met kinase activity (IC50 = 20 nM). Exhibits >60-fold selectivity over Flk and >400-fold selectivity over Ron, FGFR-1, c-Src, Cdk2, PDGFRβ, EGFR, and Tie-2. Shown to inhibit HGF/SF-stimulated cellular signaling and Met-mediated tumorigenesis in various cancer cell lines.

생화학적/생리학적 작용

Cell permeable: yes
Primary Target
met kinase activity
Product competes with ATP.
Reversible: yes
Target IC50: 20 nM against Met kinase activity

포장

Packaged under inert gas

경고

Toxicity: Irritant (B)

제조 메모

Warm as needed for complete solubilization.

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

기타 정보

Ma. P. C., et al. 2005. Cancer Res.65, 1479.
Berthou, S., et al. 2004. Oncogene23, 5387.
Wang, X., et al. 2003. Mol. Cancer Ther.2, 1085.
Sattler, M., et al. 2003. Cancer Res.63, 5462.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

Xueyan Wang et al.
Molecular cancer therapeutics, 2(11), 1085-1092 (2003-11-18)
The hepatocyte growth factor/scatter factor (HGF/SF) receptor, Met, mediates various cellular responses on activation with its ligand, including proliferation, survival, motility, invasion, and tubular morphogenesis. Met expression is frequently up-regulated in sarcomas and carcinomas. Experimental evidence suggests that Met activation
Sylvie Berthou et al.
Oncogene, 23(31), 5387-5393 (2004-04-06)
Point mutations constitute a major mode of oncogenic activation of the Met receptor tyrosine kinase. Met is aberrantly activated in many types of human malignancies and its deregulated activity is correlated with aggressive tumor traits such as abnormal proliferation and
Martin Sattler et al.
Cancer research, 63(17), 5462-5469 (2003-09-23)
The Met receptor tyrosine kinase has been shown to be overexpressed or mutated in a variety of solid tumors and has, therefore, been identified as a good candidate for molecularly targeted therapy. Activation of the Met tyrosine kinase by the
Patrick C Ma et al.
Cancer research, 65(4), 1479-1488 (2005-03-01)
Non-small cell lung cancer (NSCLC) is a difficult disease to treat. The c-Met receptor is an attractive potential target for novel therapeutic inhibition in human cancers. We provide strong evidence that c-Met is overexpressed, activated, and sometimes mutated in NSCLC

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