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Merck
CN

S9820

SU 11274

≥98% (HPLC), powder

别名:

(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

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关于此项目

经验公式(希尔记法):
C28H30ClN5O4S
化学文摘社编号:
分子量:
568.09
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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InChI key

FPYJSJDOHRDAMT-KQWNVCNZSA-N

SMILES string

CN1CCN(CC1)C(=O)c2c(C)[nH]c(\C=C3/C(=O)Nc4ccc(cc34)S(=O)(=O)N(C)c5cccc(Cl)c5)c2C

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-

assay

≥98% (HPLC)

form

powder

color

orange

solubility

DMSO: 10 mg/mL at 60 °C, H2O: insoluble

storage temp.

2-8°C

Application

SU 11274 was used to inhibit c-Met in non-small cell lung cancer cell lines.3
SU11274 has been used:
  • To study the role of hepatocyte growth factor (HGF) in human vestibular schwannoma proliferation.
  • To study its effect on human gastric carcinoma cell line MKN-45.
  • To study the effect of HGF on phosphorylation of epidermal growth factor receptor, c-Met and other signaling pathways.

Biochem/physiol Actions

SU 11274 is a Met tyrosine kinase inhibitor.
SU 11274 is a class I c-Met inhibitor that competes with ATP to bind to the activation loop of c-Met.1 Inhibition of c-Met by SU 11274 is effective in improving the clinical outcome in non-small cell lung cancer cell lines.2
c-Met kinase is a hepatocyte growth factor, involved in tumor invasion process and thus it serves as therapeutic target for cancer. It is found that SU11274 showed decreased tumor progression in human melanoma, by reducing tumor growth and metastasis.

Features and Benefits

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Met page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

存储类别

13 - Non Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

法规信息

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分析证书(COA)

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Mechanism of resistance and novel targets mediating resistance to EGFR and c-Met tyrosine kinase inhibitors in non-small cell lung cancer
Botting GM, et al.
Testing, 10(8), e0136155-e0136155 (2015)
Anum Mughal et al.
Infectious agents and cancer, 8(1), 13-13 (2013-04-10)
c-Met is a receptor tyrosine kinase that encodes protein such as hepatocyte growth factor receptor (HGFR). Inappropriate activity of c-Met can cause wide variety of carcinomas. c-Met inhibitor are relatively new class of small molecules that inhibit the enzymatic activity
Gang Chen et al.
PloS one, 8(3), e59708-e59708 (2013-03-26)
Epidermal growth factor receptor (EGFR) and c-MET receptors are expressed on many non-small cell lung cancer (NSCLC) cells. Current single agent therapeutic targeting of a mutant EGFR has a high efficacy in the clinic, but is not curative. Here, we
Issues in Pharmacology, Pharmacy, Drug Research, and Drug Innovation (2013)
Melanomas: New Insights for the Healthcare Professional, 101-101 (2012)

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