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PHA-665752

🥰Excellent
Catalog No. T6128Cas No. 477575-56-7
Alias PHA665752, PHA 665752

PHA-665752 is an effective, specific and ATP-competitive c-Met inhibitor (IC50: 9 nM), >50-fold selectivity for c-Met than STKs or RTKs.

PHA-665752

PHA-665752

🥰Excellent
Purity: 99.35%
Catalog No. T6128Alias PHA665752, PHA 665752Cas No. 477575-56-7
PHA-665752 is an effective, specific and ATP-competitive c-Met inhibitor (IC50: 9 nM), >50-fold selectivity for c-Met than STKs or RTKs.
Pack SizePriceAvailabilityQuantity
5 mg56 €In Stock
10 mg88 €In Stock
25 mg179 €In Stock
50 mg278 €In Stock
100 mg462 €In Stock
1 mL x 10 mM (in DMSO)80 €In Stock
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Purity:99.35%
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Product Introduction

Bioactivity
Description
PHA-665752 is an effective, specific and ATP-competitive c-Met inhibitor (IC50: 9 nM), >50-fold selectivity for c-Met than STKs or RTKs.
Targets&IC50
c-Met:9 nM
In vitro
PHA-665752 significantly inhibits c-Met kinase activity with Ki of 4 nM, and exhibits >50-fold selectivity for c-Met compared with various tyrosine and serine-threonine kinases. PHA-665752 potently inhibits the HGF-stimulated c-Met autophosphorylation with IC50 of 25-50 nM. PHA-665752 also significantly blocks HGF- and c-Met-dependent functions such as cell motility and cell proliferation with IC50 of 40-50 nM and 18-42 nM, respectively. In addition, PHA-665752 potently inhibits HGF-stimulated or constitutive phosphorylation of mediators of downstream of c-Met such as Gab-1, ERK, Akt, STAT3, PLC-γ, and FAK in multiple tumor cell lines. [1] PHA-665752 inhibits cell growth in TPR-MET-transformed BaF3 cells with IC50 of <60 nM, and inhibits constitutive cell motility and migration by 92.5% at 0.2 μM. Inhibition of c-Met by PHA665752 (0.2 μM) also induces cell apoptosis of 33.1% and G1 cell cycle arrest with cells in G1 phase increasing from 42.4% to 77.0%. PHA665752 can cooperate with rapamycin to inhibit cell growth of TPR-MET-transformed BaF3 cells and non-small cell lung cancer H441 cells. [2]
In vivo
Administration of PHA-665752 induces a dose-dependent tumor growth inhibition of S114 xenografts by 20 %, 39% and 68%, at dose of 7.5, 15, and 30 mg/kg/day, respectively. [1] PHA665752 treatment significantly reduces the tumor growth of NCI-H69, NCI-H441 and A549 in mouse xenografts by 99%, 75%, and 59%, respectively. PHA665752 also significantly inhibits angiogenesis by >85%, due to decreasing the production of vascular endothelial growth factor and increasing the production of the angiogenesis inhibitor thrombospondin-1. [3]
Kinase Assay
In vitro enzyme assay: The c-Met kinase domain GST-fusion protein is used for the c-Met assay. The IC50 value of PHA-665752 for the inhibition of c-Met is based on phosphorylation of kinase peptide substrates or poly-glu-tyr in the presence of ATP and divalent cation (MgCl2 or MnCl2 10-20 mM). The linear range (i.e., the time period over which the rate remains equivalent to the initial rate) is determined for c-Met, and the kinetic measurement and IC50 determination are performed within this range.
Cell Research
For proliferation assays, cells are grown in medium with 0.1% FBS for 48 hours after which they are treated with various concentrations of PHA-665752 in HGF (50 ng/mL) in a medium containing 2% FBS. After 18 hours, cells are incubated with BrdUrd for 1 hour, fixed, and stained with anti-BrdUrd peroxidase-conjugated antibody, and plates are read at 630 nm. For apoptosis assays, cells are grown in medium with 2% FBS in presence and absence of HGF (50 ng/mL) and various concentrations of PHA-665752 for 72 hours. After 72 hours, a mixture containing ethidium bromide and acridine orange is added, and apoptotic cells (bright orange cells or cell fragments) are counted by fluorescence microscopy.(Only for Reference)
AliasPHA665752, PHA 665752
Chemical Properties
Molecular Weight641.61
FormulaC32H34Cl2N4O4S
Cas No.477575-56-7
SmilesC(=C\1/C=2C(NC1=O)=CC=C(S(CC3=C(Cl)C=CC=C3Cl)(=O)=O)C2)\C4=C(C)C(C(=O)N5[C@@H](CN6CCCC6)CCC5)=C(C)N4
Relative Density.1.404 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 60 mg/mL (93.51 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.5586 mL7.7929 mL15.5858 mL77.9290 mL
5 mM0.3117 mL1.5586 mL3.1172 mL15.5858 mL
10 mM0.1559 mL0.7793 mL1.5586 mL7.7929 mL
20 mM0.0779 mL0.3896 mL0.7793 mL3.8964 mL
50 mM0.0312 mL0.1559 mL0.3117 mL1.5586 mL

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