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PHA-665752

Catalog No. T6128   CAS 477575-56-7
Synonyms: PHA 665752, PHA665752

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
PHA-665752 Chemical Structure
PHA-665752, CAS 477575-56-7
Pack Size Availability Price/USD Quantity
5 mg In stock $ 59.00
10 mg In stock $ 93.00
25 mg In stock $ 189.00
50 mg In stock $ 293.00
100 mg In stock $ 487.00
1 mL * 10 mM (in DMSO) In stock $ 85.00
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Purity: 99.35%
Purity: 97.05%
Purity: 97.01%
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Biological Description
Chemical Properties
Storage & Solubility Information
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)
Synonyms PHA 665752, PHA665752
Molecular Weight 641.61
Formula C32H34Cl2N4O4S
CAS No. 477575-56-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 64.2 mg/mL (100 mM)

TargetMolReferences and Literature

1. Christensen JG, et al. Cancer Res, 2003, 63(21), 7345-7355. 2. Ma PC, et al. Clin Cancer Res, 2005, 11(6), 2312-2319. 3. Puri N, et al. Cancer Res, 2007, 67(8), 3529-3534.

TargetMolCitations

1. Yuan S, Gong Y, Chen R, et al. Chinese herbal formula QHF inhibits hepatocellular carcinoma metastasis via HGF/c-Met signaling pathway. Biomedicine & Pharmacotherapy. 2020, 132: 110867.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Bioactive Compound Library Anti-Cancer Compound Library Osteogenesis Compound Library Kinase Inhibitor Library Preclinical Compound Library Cytokine Inhibitor Library NO PAINS Compound Library Anti-Colorectal Cancer Compound Library

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Keywords

PHA-665752 477575-56-7 Angiogenesis Apoptosis Autophagy Cytoskeletal Signaling Tyrosine Kinase/Adaptors VEGFR FGFR Bcr-Abl c-Met/HGFR Inhibitor inhibit PHA 665752 PHA665752 inhibitor

 

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