PHA-665752 is potent, selective and ATP-competitive inhibitor of MET kinase. (IC50 values are 9, 68, 200, 1400, 3000, 3800 and 6000 nM for MET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively and > 10000 nM for IGF-IR, PDGFR, AURORA2, PKA, PKB&al
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of MET proto-oncogene; receptor tyrosine kinase
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
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
1.Christensen JG, Schreck R, Burrows J, Kuruganti P, Chan E, Le P, Chen J, Wang X, Ruslim L, Blake R et al.. (2003) A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo.. Cancer Res, 63 (21):(7345-55). [PMID:14612533]
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