PZ0147

PHA-665752 hydrate

≥98% (HPLC)

• Synonym(s): (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
• Empirical Formula (Hill Notation): C₃₂H₃₄Cl₂N₄O₄S · xH₂O
• CAS Number: 477575-56-7
• Molecular Weight: 641.61 (anhydrous basis)
• MDL number: MFCD18632554
• UNSPSC Code: 12352200
• PubChem Substance ID: 329823732
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: powder
• optical activity: [α]/D +50 to +70°, c = 0.2 in methanol
• color: light yellow to light brown
• solubility: DMSO: ≥20 mg/mL
• storage temp.: 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

Description

Application

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

Biochem/physiol Actions

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.

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.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable