PHA-665752

Catalog No.S1070

PHA-665752 Chemical Structure

Molecular Weight(MW): 641.61

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

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Cited by 36 Publications

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Biological Activity

Description PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM in cell-free assays, >50-fold selectivity for c-Met than RTKs or STKs.
Targets
c-Met [1]
(Cell-free assay)
RON [1]
(Cell-free assay)
Flk1 [1]
(Cell-free assay)
9 nM 68 nM 200 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-SNU-5 M1zMc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3Xd5FKSzVyPUCuNVI{PzVizszN NUDkSGR1W0GQR1XS
LB2241-RCC MkLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4mz[WlEPTB;MD6xOVcxOiEQvF2= NWe2fHJXW0GQR1XS
KINGS-1 M3\tdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;YXWZPUUN3ME2wMlM2QTFzIN88US=> MmLqV2FPT0WU
ALL-PO NH\xU4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHS5UWxKSzVyPUCuPFEzPzdizszN NWHFUZNQW0GQR1XS
SK-LMS-1 NHjLS3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PSUGlEPTB;MD64PVg1PiEQvF2= MnW3V2FPT0WU
MV-4-11 NXnWPHBQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV73T2VbUUN3ME2xMlI6PDdizszN Mnf5V2FPT0WU
SUP-T1 MkHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnx[4FKSzVyPUKuNVM6PjRizszN MkTSV2FPT0WU
MRK-nu-1 NVz5[ZVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrLdYJFUUN3ME2yMlQxODV4IN88US=> NF7rTmRUSU6JRWK=
ES1 NW\4d5l5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LTSWlEPTB;Mz6zOFg3PiEQvF2= M{exO3NCVkeHUh?=
NOS-1 MnTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmqzTWM2OD12LkO5PFY4KM7:TR?= MljTV2FPT0WU
KM12 NXuwOmR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTRwNEG4JO69VQ>? M2r2N3NCVkeHUh?=
Becker M{DUXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjMVVJ6UUN3ME21MlI1PjZizszN MYnTRW5ITVJ?
NCI-SNU-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4S3NWlEPTB;NT62N|c{OyEQvF2= MoXMV2FPT0WU
EW-22 NV32NI46T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn65TWM2OD15LkezOlE1KM7:TR?= M4PvcHNCVkeHUh?=
ES6 NVWzU2JNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTdwOEG5OUDPxE1? NEezeVNUSU6JRWK=
A498 MnvSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRThwMki0OFYh|ryP NEnZcG9USU6JRWK=
EW-16 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PQZWlEPTB;OT62OVQ{KM7:TR?= NEjlUZJUSU6JRWK=
CTV-1 NVv4dI5uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPETWM2OD17Lki1NFI1KM7:TR?= NYnxb3F2W0GQR1XS
ETK-1 NIexb3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mof3TWM2OD1zMD6yPVMyKM7:TR?= MX7TRW5ITVJ?
NCI-H1395 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkf0TWM2OD1zMD64NFI1KM7:TR?= NVvK[|lqW0GQR1XS
DOHH-2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DuNGlEPTB;MUCuPVI3PCEQvF2= MUXTRW5ITVJ?
GI-1 NV\UVndPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTPTWM2OD1zMT64OVk3KM7:TR?= NF;aPWJUSU6JRWK=
HT-144 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmqwTWM2OD1zND6yNVY{KM7:TR?= MVfTRW5ITVJ?
ES5 MoK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ztSWlEPTB;MUSuOFY4KM7:TR?= NWD1TYFYW0GQR1XS
NALM-6 M3Xie2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nmTGlEPTB;MUWuNlE6PiEQvF2= M3f4dnNCVkeHUh?=
KNS-81-FD M2nWdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWS2d4NZUUN3ME2xOU42QDR7IN88US=> NH;LVXJUSU6JRWK=
TE-15 NVK4WIg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TwS2lEPTB;MU[uOVc4OSEQvF2= NXrESnh3W0GQR1XS
SCC-15 NHnpdGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonuTWM2OD1zOD6zOFk5KM7:TR?= NHnqcppUSU6JRWK=
EoL-1-cell MmD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTF6LkS1OFUh|ryP MXvTRW5ITVJ?
NCI-H720 NWDvOYx7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jkd2lEPTB;MUiuO|cyKM7:TR?= MYHTRW5ITVJ?
NB14 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIS1UFZKSzVyPUG5MlU1OjVizszN MUfTRW5ITVJ?
KE-37 MkH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\RfWJKSzVyPUG5MlgzOzNizszN MYrTRW5ITVJ?
LXF-289 M2S4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfuTWM2OD1zOT64OlI6KM7:TR?= MlW2V2FPT0WU
RPMI-8402 M4PZTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvCTWM2OD1{MD6zNlY6KM7:TR?= M4TiT3NCVkeHUh?=
SK-N-DZ NYf1V3JbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTJzLkKxN|Eh|ryP NXHESoh4W0GQR1XS
ACN Mk[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XDZ2lEPTB;MkKuNlQ6PyEQvF2= NX[0e4ZJW0GQR1XS
TE-11 NFnKNJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXLSG1rUUN3ME2yOk4xPjlizszN M1rVeHNCVkeHUh?=
COLO-800 NUjhc2pbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DaO2lEPTB;MkeuNVch|ryP MY\TRW5ITVJ?
MOLT-13 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XwVWlEPTB;MkeuNVg1PyEQvF2= NV;IeHpbW0GQR1XS
697 M4Xk[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTJTWM2OD1{OD63OlM{KM7:TR?= NGL4cGdUSU6JRWK=
VA-ES-BJ NIPBR5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2K4[2lEPTB;MkmuN|czQSEQvF2= M3zVb3NCVkeHUh?=
EW-13 M3Pv[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TMRmlEPTB;MkmuOVA1PSEQvF2= MY\TRW5ITVJ?
NB7 M3rCeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTN{LkK2OlUh|ryP NIDERVVUSU6JRWK=
MONO-MAC-6 NH6yb3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\VTWM2OD1|Mj64O|k2KM7:TR?= NIX4eWRUSU6JRWK=
SW962 M1XFbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHC[YVKUUN3ME2zN{41PTF|IN88US=> Mk\UV2FPT0WU
KS-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTrdGp5UUN3ME2zN{46PDhzIN88US=> MoC0V2FPT0WU
KU812 M3vlWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfDNpVKSzVyPUO0MlU4ODJizszN NXXwNmFVW0GQR1XS
IMR-5 NXuySJFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYK0ZXdPUUN3ME2zO{41OzF6IN88US=> NW\JcJFtW0GQR1XS
BC-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nYfGlEPTB;M{iuNFM{KM7:TR?= Moi2V2FPT0WU
NCI-H510A MlTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33XTGlEPTB;M{iuNlA{OiEQvF2= M1HIXHNCVkeHUh?=
EW-18 NHTl[oRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3f4WmlEPTB;NECuPFMxOyEQvF2= NVHyWHlDW0GQR1XS
CCRF-CEM NFLacm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTR{LkK3PVch|ryP MlnFV2FPT0WU
HH MljmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXOd|FKSzVyPUSzMlUxPjlizszN MYLTRW5ITVJ?
NCI-H2171 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnCdGV5UUN3ME20Ok4xOjd{IN88US=> Ml62V2FPT0WU
LC-2-ad NGjUU2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3kN4ZRUUN3ME20PU4yPDF|IN88US=> Mn;IV2FPT0WU

... Click to View More Cell Line Experimental Data

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

Kinase Assay:[1]
+ Expand

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:[1]
+ Expand
  • Cell lines: S114, GTL-16, NCI-H441, and BxPC-3
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 18, or 72 hours
  • Method: 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)
Animal Research:[1]
+ Expand
  • Animal Models: Female athymic mice (nu/nu) bearing S114 or GTL-16 tumor xenografts
  • Formulation: Formulated in vehicle (L-lactate (pH 4.8) and 10% polyethylene glycol)
  • Dosages: ~30 mg/kg/day
  • Administration: Injection via bolus i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 128 mg/mL (199.49 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+castor oil
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 641.61
Formula

C32H34Cl2N4O4S

CAS No. 477575-56-7
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    I need to use S1070 for intraperitoneal application in mice. Could you tell me the solvent you use, please?

  • Answer:

    The highest concentration of PHA-665752 (S1070) in 4% DMSO+30% PEG 300+5% Tween 80+ddH2O is 5mg/ml. If you want to get higher concentration, the concentration of DMSO and PEG will be higher. For example, it can be dissolved in 8% DMSO+50% PEG 300+5% Tween 80+ddH2O at 10mg/ml clearly.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID