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PHA-665752

HY-11107

(PHA 665752; PHA665752)

PHA-665752

PHA-665752 Chemical Structure

PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM, >50-fold selectivity for c-Met than RTKs or STKs.

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10 mM * 1 mL in DMSO $90 In-stock
10 mg $82 In-stock
50 mg $330 In-stock
100 mg $580 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €88 In-stock
10 mg €80 In-stock
50 mg €323 In-stock
100 mg €568 In-stock
200 mg Get quote
500 mg Get quote

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Product name: PHA-665752
Cat. No.: HY-11107

PHA-665752 Data Sheet

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    Purity: 99.27%

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Biological Activity of PHA-665752

PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM, >50-fold selectivity for c-Met than RTKs or STKs.
IC50 value: 9 nM
Target: c-Met
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].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 641.61 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C32H34Cl2N4O4S
CAS No 477575-56-7
Solvent & Solubility

DMSO ≥125mg/mL Water <1.2mg/mL Ethanol ≥124mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 1.5586 mL 7.7929 mL 15.5858 mL
5 mM 0.3117 mL 1.5586 mL 3.1172 mL
10 mM 0.1559 mL 0.7793 mL 1.5586 mL

References on PHA-665752

Inhibitor Kit

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