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Merck
모든 사진(1)

문서

PZ0147

Sigma-Aldrich

PHA-665752 hydrate

≥98% (HPLC)

동의어(들):

(3Z)-5-[[(2,6-Dichlorophenyl)methyl]sulfonyl]-3-[[3,5-dimethyl-4-[[(2R)-2-(1-pyrrolidinylmethyl)-1-pyrrolidinyl]carbonyl]-1H-pyrrol-2-yl]methylene]-1,3-dihydro-2H-indol-2-one hydrate

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About This Item

실험식(Hill 표기법):
C32H34Cl2N4O4S · xH2O
CAS Number:
Molecular Weight:
641.61 (anhydrous basis)
MDL number:
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77

분석

≥98% (HPLC)

형태

powder

광학 활성

[α]/D +50 to +70°, c = 0.2 in methanol

색상

light yellow to light brown

solubility

DMSO: ≥20 mg/mL

저장 온도

2-8°C

SMILES string

O.Cc1[nH]c(\C=C2/C(=O)Nc3ccc(cc23)S(=O)(=O)Cc4c(Cl)cccc4Cl)c(C)c1C(=O)N5CCC[C@@H]5CN6CCCC6

InChI

1S/C32H34Cl2N4O4S.H2O/c1-19-29(35-20(2)30(19)32(40)38-14-6-7-21(38)17-37-12-3-4-13-37)16-24-23-15-22(10-11-28(23)36-31(24)39)43(41,42)18-25-26(33)8-5-9-27(25)34;/h5,8-11,15-16,21,35H,3-4,6-7,12-14,17-18H2,1-2H3,(H,36,39);1H2/b24-16-;/t21-;/m1./s1

InChI key

MKHQWLQMOSOUEQ-SCLITUASSA-N

애플리케이션

PHA-665752 hydrate has been used as a c-Met inhibitor:
  • to study its effects on oxidative stress in human mammary epithelial MCF10A cells with extra centrosomes
  • to study its effects on the clonogenicity of T-cell specific transcription factor/ lymphoid enhancer-binding factor-1 (TCF/LEF-1) responsive promoter to drive expression of green fluorescent protein (TOP-GFP) cancer stem cell (CSC) cultures
  • to study its inhibitory effects on melanoma cell lines

생화학적/생리학적 작용

PHA-665752 ia a c-Met kinase inhibitor. PHA-665752 is ATP-competitive, an active-site inhibitor with greater than 50-fold selectivity for c-Met vs a panel of tyrosine and serine-threonine kinases.

특징 및 장점

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.

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

Registered report: Tumour micro-environment elicits innate resistance to RAF inhibitors through HGF secretion
Blum D, et al.
eLife, 3(4), e04034-e04034 (2014)
Oxidative stress in cells with extra centrosomes drives non-cell-autonomous invasion
Arnandis T, et al.
Developmental Cell, 47(4), 409-424 (2018)
Replication Study: Wnt activity defines colon cancer stem cells and is regulated by the microenvironment
Essex A, et al.
eLife, 8(4), e45426-e45426 (2019)
Anthony Essex et al.
eLife, 8 (2019-06-20)
As part of the Reproducibility Project: Cancer Biology we published a Registered Report (Evans et al., 2015), that described how we intended to replicate selected experiments from the paper 'Wnt activity defines colon cancer stem cells and is regulated by
David Blum et al.
eLife, 3 (2014-12-11)
The Reproducibility Project: Cancer Biology seeks to address growing concerns about reproducibility in scientific research by conducting replications of 50 papers in the field of cancer biology published between 2010 and 2012. This Registered Report describes the proposed replication plan

문서

Discover Bioactive Small Molecules for Kinase Phosphatase Biology

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