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 28 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 MlG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\nbGJQUUN3ME2wMlEzOzd3IN88US=> M1jXPHNCVkeHUh?=
LB2241-RCC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPnfmVQUUN3ME2wMlE2PzB{IN88US=> NHzlOItUSU6JRWK=
KINGS-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH[2NYxKSzVyPUCuN|U6OTFizszN MXnTRW5ITVJ?
ALL-PO Mmj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwOEGyO|ch|ryP MkDkV2FPT0WU
SK-LMS-1 NF71fmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LtSWlEPTB;MD64PVg1PiEQvF2= MXXTRW5ITVJ?
MV-4-11 MlPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rEXWlEPTB;MT6yPVQ4KM7:TR?= M2TVSHNCVkeHUh?=
SUP-T1 Mm\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTJwMUO5OlQh|ryP MWXTRW5ITVJ?
MRK-nu-1 NX\KZVlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXK0eY5XUUN3ME2yMlQxODV4IN88US=> Mn7kV2FPT0WU
ES1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTNwM{S4OlYh|ryP NWewUplkW0GQR1XS
NOS-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUixPIg{UUN3ME20MlM6QDZ5IN88US=> MlnLV2FPT0WU
KM12 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTRwNEG4JO69VQ>? NXrMPWhqW0GQR1XS
Becker Mn7MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLSfpZZUUN3ME21MlI1PjZizszN M1PNPHNCVkeHUh?=
NCI-SNU-1 NVLN[pFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTVwNkO3N|Mh|ryP M2nubnNCVkeHUh?=
EW-22 NIfVdm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7WNHFFUUN3ME23Mlc{PjF2IN88US=> MmfyV2FPT0WU
ES6 NXHRWY93T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnPcnVRUUN3ME23MlgyQTVizszN MlX0V2FPT0WU
A498 NGPmcmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnEb5N4UUN3ME24MlI5PDR4IN88US=> MYPTRW5ITVJ?
EW-16 NVf2blN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TpW2lEPTB;OT62OVQ{KM7:TR?= Mmm1V2FPT0WU
CTV-1 NXH6dXN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jHW2lEPTB;OT64OVAzPCEQvF2= NVfScoE6W0GQR1XS
ETK-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTFyLkK5N|Eh|ryP MWPTRW5ITVJ?
NCI-H1395 NIfoVIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPmTWM2OD1zMD64NFI1KM7:TR?= MYHTRW5ITVJ?
DOHH-2 MlzUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHH0cVVKSzVyPUGwMlkzPjRizszN NITSOWdUSU6JRWK=
GI-1 NVTKVIxyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\DTWM2OD1zMT64OVk3KM7:TR?= NWLUfYN5W0GQR1XS
HT-144 MoLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTF2LkKxOlMh|ryP MnjYV2FPT0WU
ES5 NWj2U2t2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTF2LkS2O{DPxE1? M{X6SXNCVkeHUh?=
NALM-6 NV;EWHluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvDeJJYUUN3ME2xOU4zOTl4IN88US=> M{TBRnNCVkeHUh?=
KNS-81-FD M3j4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXMRZI4UUN3ME2xOU42QDR7IN88US=> MnLrV2FPT0WU
TE-15 NX\yb4g2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1uxbGlEPTB;MU[uOVc4OSEQvF2= NUfUXpp3W0GQR1XS
SCC-15 NXH6N281T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWC1VJNIUUN3ME2xPE4{PDl6IN88US=> MkO1V2FPT0WU
EoL-1-cell NYDFbGs2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vXXWlEPTB;MUiuOFU1PSEQvF2= M2fGR3NCVkeHUh?=
NCI-H720 M1PHeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XsUWlEPTB;MUiuO|cyKM7:TR?= MoL0V2FPT0WU
NB14 MnryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHWyTpFKSzVyPUG5MlU1OjVizszN NEf1TY5USU6JRWK=
KE-37 NH\3fWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjWNFN{UUN3ME2xPU45OjN|IN88US=> NWflOmUyW0GQR1XS
LXF-289 NFHWXGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTF7Lki2Nlkh|ryP M37HWHNCVkeHUh?=
RPMI-8402 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjCO3Q{UUN3ME2yNE4{OjZ7IN88US=> NWHHS2JuW0GQR1XS
SK-N-DZ M{LDdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTJzLkKxN|Eh|ryP M4rWcXNCVkeHUh?=
ACN NUjEeGVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWWxT4YxUUN3ME2yNk4zPDl5IN88US=> NGXJcopUSU6JRWK=
TE-11 M1zMNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrte2pNUUN3ME2yOk4xPjlizszN MXHTRW5ITVJ?
COLO-800 NHWxWVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1Ta[mlEPTB;MkeuNVch|ryP M3\C[XNCVkeHUh?=
MOLT-13 MojDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\QSmlEPTB;MkeuNVg1PyEQvF2= MmXyV2FPT0WU
697 M1SzPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHiPVVKSzVyPUK4Mlc3OzNizszN M{fGcXNCVkeHUh?=
VA-ES-BJ NFH2O2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmruTWM2OD1{OT6zO|I6KM7:TR?= NXOzdJV[W0GQR1XS
EW-13 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTJ7LkWwOFUh|ryP NIPpSm1USU6JRWK=
NB7 M1TOTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHtXGhKSzVyPUOyMlI3PjVizszN NFHocFBUSU6JRWK=
MONO-MAC-6 NF3sWYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LnTWlEPTB;M{KuPFc6PSEQvF2= M4TjZnNCVkeHUh?=
SW962 M1jBOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnYe3ZnUUN3ME2zN{41PTF|IN88US=> NEj0SnFUSU6JRWK=
KS-1 NXLi[WNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWf4TowyUUN3ME2zN{46PDhzIN88US=> NWDFdIo3W0GQR1XS
KU812 MkDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rPOGlEPTB;M{SuOVcxOiEQvF2= M1TYcHNCVkeHUh?=
IMR-5 NILIdVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXzOY1KSzVyPUO3MlQ{OThizszN NEXo[IpUSU6JRWK=
BC-1 NXvKUldTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4X2ZmlEPTB;M{iuNFM{KM7:TR?= MUnTRW5ITVJ?
NCI-H510A MmfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTNUI1KSzVyPUO4MlIxOzJizszN M1vRfHNCVkeHUh?=
EW-18 NUDZW|N6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2i2VGlEPTB;NECuPFMxOyEQvF2= M2[4R3NCVkeHUh?=
CCRF-CEM MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrIN5JKSzVyPUSyMlI4QTdizszN M{DSenNCVkeHUh?=
HH M1n6fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vtbWlEPTB;NEOuOVA3QSEQvF2= NGT5dXVUSU6JRWK=
NCI-H2171 MoT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmD1TWM2OD12Nj6wNlczKM7:TR?= MYDTRW5ITVJ?
LC-2-ad Ml6wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jHNWlEPTB;NEmuNVQyOyEQvF2= MVjTRW5ITVJ?

... 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