BMS-777607

Catalog No.S1561

BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM in cell-free assays, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases. Phase 1/2.

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BMS-777607 Chemical Structure

BMS-777607 Chemical Structure
Molecular Weight: 512.89

Validation & Quality Control

Customer Product Validation(6)

Quality Control & MSDS

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Product Information

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  • Research Area
  • Inhibition Profile
  • BMS-777607 Mechanism

Product Description

Biological Activity

Description BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM in cell-free assays, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases. Phase 1/2.
Targets Axl [1]
(Cell-free assay)
RON [1]
(Cell-free assay)
Met [1]
(Cell-free assay)
Tyro3 [1]
(Cell-free assay)

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IC50 1.1 nM 1.8 nM 3.9 nM 4.3 nM
In vitro BMS-777607 is a selective ATP-competitive Met kinase inhibitor which potently blocks the autophosphorylation of c-Met with IC50 of 20 nM in GTL-16 cell lysates, and demonstrates selective inhibition of proliferation in Met-driven tumor cell lines, such as GTL-16 cell line, H1993 and U87. [1] BMS-777607 inhibits hepatocyte growth factor (HGF)-triggered c-Met autophosphorylation with IC50 of <1 nM in PC-3 and DU145 prostate cancer cells. BMS 777607 has little effect on tumor cell growth, but exhibits inhibitory effect on HGF-induced cell scattering in PC-3 and DU145 cells, with almost complete inhibition at 0.5 μM. BMS 777607 also suppresses stimulated cell migration and invasion in a dose-dependent fashion (IC50 < 0.1 μM) in both cell lines. [2] Application of BMS 777607 (~10 μM) to the highly metastatic murine KHT cells for 2 hours potently eliminates basal levels of autophosphorylated c-Met with IC50 of 10 nM without affecting the total c-Met, leading to dose-dependent inhibition of phosphorylation of downstream signaling molecules including ERK, Akt, p70S6K and S6. Treatment with BMS-777607 (~1 μM) for 24 hours potently inhibits the KHT cell scatter, motility and invasion at doses in the nanomolar range which consists with MET gene knockdown, and modestly affects cell proliferation and colony formation. [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
GTL-16NY\6fmFyU2mwYYPlJIF{e2G7MVLEUXNQMYTpcohq[mm2czDN[ZQhc2mwYYPlJJdqfGhiSVO1NEBw\iBzMECgcm0>M2jtZVE6OjZyN{Gx
H1993NV;sUJhiT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=NEHqb|h,OTBizszNM13WW2ROW09?NVjpNGRwUUN3ME2xOVAhdk1?MlzxNVkzPjB5MUG=
U87M3TibGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7M3e1[p4yOCEQvF2=MXjEUXNQNGK3VpBKSzVyPUG2NEBvVQ>?NGTJfo4yQTJ4MEexNS=>
PC-3MnTESpVv[3Srb36gZZN{[Xl?NX;pTFdIOC5zIN88US=>MUPEUXNQMnqx[ZhpcWKrdIOgbY5pcWKrdH;yfUBm\m[nY4Sgc44hUEeILXnu[JVk\WRiY3XscEB{[2G2dHXybY5oMUKyNFUyPTl2Mx?=
DU145MWHGeY5kfGmxbjDhd5NigQ>?MlS5NE4yKM7:TR?=MVfEUXNQNV;TVI52\XiqaXLpeJMhcW6qaXLpeI9zgSCnZn\lZ5Qhd25iSFfGMYlv\HWlZXSgZ4VtdCC|Y3H0eIVzcW6pMoLINlA2OTV7NEO=
PC-3MlXiSpVv[3Srb36gZZN{[Xl?M{X1fFAvODFizszNM2TPR2ROW09?NEX0VYJ{fXCycnXzd4V{KEiJRj3pcoR2[2WmIHPlcIwhdWmpcnH0bY9vNFfuXowzODVzNUm0Ny=>
DU145M4\ZVmZ2dmO2aX;uJIF{e2G7MlTwNE4xOSEQvF2=NHHwfWNFVVORNHzxVYJ{fXCycnXzd4V{KEiJRj3pcoR2[2WmIHPlcIwhdWmpcnH0bY9vNF[w[FIzODVzNUm0Ny=>
PC-3MnjqSpVv[3Srb36gZZN{[Xl?MlXjNE4yKM7:TR?=M4r0RWROW09?NEnP[ohqdXCjaYLzJGhITi2vZXTpZZRm\CClZXzsJIlvfmG|aX;uNGTGSG4zODVzNUm0Ny=>
DU145NFrmO|NHfW6ldHnvckBie3OjeR?=NF6wXXgxNjFizszNM{n0V2ROW09?MUnpcZBicXK|IFjHSk1u\WSrYYTl[EBk\WyuIHnueoF{cW:wNIHOV4ozODVzNUm0Ny=>
PC-3M{DjWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7MmHVglExKM7:TR?=NHLqcWRFVVORMnXPdoVlfWOnczDj[YxtKHC{b3zp[oVz[XSrb36=M{O3UVIxPTF3OUSz
KHTNWX6NIltU2mwYYPlJIF{e2G7M4XOS2ROW09?MlvkZoxw[2u|IITo[UBkNU2ndDDzbYdv[WyrbnegdIF1cHejeTD3bZRpKEmFNUCgc4YhOTBibl2=M1LKeVIzOjh4NUKz
KHTMV;GeY5kfGmxbjDhd5NigQ>?MoX2glEh|ryPNHnWc4lFVVORM173[pBz\X[nboTzJJNxd262YX7lc5V{KEuKVDDj[YxtKHOlYYT0[ZJqdmdid3n0bEBKSzVyIH;mJFAvOS1yLkWg{txOMnn6NlIzQDZ3MkO=
KHTMkTrSpVv[3Srb36gZZN{[Xl?MoTMglAvPSEQvF2=MVTEUXNQMUDpcohq[mm2czDj[YxtKG2rZ4LheIlwdg>?NVfwSFdjOjJ{OE[1NlM>
KHTMYDGeY5kfGmxbjDhd5NigQ>?NGexWW9,OC53IN88US=>NUfLS3dnTE2VTx?=NYXDbWxxcW6qaXLpeJMh[2WubDDpcpZie2mxbh?=M3;YXFIzOjh4NUKz
KHTMljtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?NUCxNI11hjFyIN88US=>MUPEUXNQMny1bY5pcWKrdIOgT2hVKGOnbHygdJJwdGmoZYLheIlwdg>?MlrKNlIzQDZ3MkO=
T-47DM3\YZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7MVn+OUDPxE1?NGDuV2lFVVORNEfWTXJqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44>M1;DW|I{PDZ6NUK5
ZR-75-1NV\MfGUxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=Mkn2glUh|ryPM{nzeWROW09?NUHQd4x4cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vMWSyN|Q3QDV{OR?=
T-47DNULNVJM1TnWwY4Tpc44h[XO|YYm=MV6xNEDPxE1?MlrUSG1UVw>?NH3JR5lKdmS3Y3XzJJBwdHmybH;p[Jkh[nliOE[gKS=>NUHIRlBTOjN2Nki1Nlk>
ZR-75-1MU\GeY5kfGmxbjDhd5NigQ>?MXGxNEDPxE1?NXHaeJBxTE2VTx?=NY\QclByUW6mdXPld{Bxd2y7cHzvbYR6KGK7IEi4KS=>NH7LN4kzOzR4OEWyPS=>
T-47DMne0SpVv[3Srb36gZZN{[Xl?NYLZdnlNOTBizszNM3XBPWROW09?NIDFS5pqdmirYnn0d{BCXVKNLVKg[pVv[3Srb36gZY5lKGmwZIXj[ZMhcXS|IIDyc5RmcW5iZHXndoFl[XSrb36=MYiyN|Q3QDV{OR?=
CHRFM2\KVmZ2dmO2aX;uJIF{e2G7MWqxNEDPxE1?MoC0SG1UVw>?MnW3bY5pcWKrdIOgZ4VtdCCmaY\pd4lwdg>?Mln5NlU{ODR7MEC=
HPDEM3y2bmZ2dmO2aX;uJIF{e2G7NYC2OZJNOTBizszNMYfEUXNQMYLicI9kc3NiY3;ud5RqfHW2aY\lJIFkfGm4YYTpc44h[W6mIHTlZ5Jm[XOnZDDBT3Qhe2mpbnHsbY5oMX2yOlQ4PzNzNB?=
U118MGMWrLbY5ie2ViYYPzZZk>M1XLUZ4{KM7:TR?=NUjicop[TE2VTx?=NX[zdpNr[myxY3vzJGFZVCCyaH;zdIhwenmuYYTpc44>M4fUWVI3QDR6NUK0
SF126NGDJT5VMcW6jc3WgZZN{[Xl?NVLHZZZEhjNizszNM1\YVWROW09?NF;aZ29jdG:la4OgRXhNKHCqb4PwbI9zgWyjdHnvci=>M4PndVI3QDR6NUK0
U118MGMlnWR5l1d3irY3n0fUBie3OjeR?=MYOxNk42KM7:TR?=M4i0ZWROW09?NUHOcXFN\GWlcnXhd4V{KGeuaX;tZUBk\WyuII\pZYJqdGm2eR?=NUnyU|k5OjZ6NEi1NlQ>
SF126MXjDfZRwgGmlaYT5JIF{e2G7NUjTUJp5OTJwNTFOwG0>NYnkW|lmTE2VTx?=M13XdIRm[3KnYYPld{BodGmxbXGgZ4VtdCC4aXHibYxqfHl?M3z6TFI3QDR6NUK0
U118MGMoG0RZBweHSxc3nzJIF{e2G7M4\VXFEzNjVizszNMnLCSG1UVw>?M2nlZolv\HWlZYOg[4xqd22jIHPlcIwh[XCxcITvd4l{NV\DZ|dIOjZ6NEi1NlQ>
SF126NF3wOZVCeG:ydH;zbZMh[XO|YYm=NH[xdVIyOi53IN88US=>NITtZWFFVVORMnPQbY5lfWOnczDncIlwdWFiY3XscEBieG:ydH;zbZM>M4XxWFI3QDR6NUK0
U118MGNEi0TZZHfW6ldHnvckBie3OjeR?=M4DsO|EzNjVizszNMYjEUXNQMWHicI9kc3NiZ3zpc41iKGOnbHygcYloemG2aX;uJIFv\CCrbo\hd4l3\SCpcn;3eIgheGG2dHXyci=>MWWyOlg1QDV{NB?=
SF126MYnGeY5kfGmxbjDhd5NigQ>?Mme4NVIvPSEQvF2=NFzQclJFVVORM3LROoJtd2OtczDncIlwdWFiY3XscEBucWe{YYTpc44h[W6mIHnueoF{cX[nIHfyc5d1cCCyYYT0[ZJvMnnRNlY5PDh3MkS=

... Click to View More Cell Line Experimental Data

In vivo Oral administration of BMS 777607 (6.25-50 mg/kg) significantly reduces tumor volumes of the GTL-16 human tumor xenografts in athymic mice with no observed toxicity. [1] Administration of BMS 777607 (25 mg/kg/day) decreases the number of KHT lung tumor nodules (28.3%), improves the morphological hemorrhage, and significantly impairs the metastatic phenotype in the 6-8 week-old female C3H/HeJ mice injected with rodent fibrosarcoma KHT cells without apparent systemic toxicity compared to the control treatment. A low dose of BMS 777607 (10 mg/kg) also offers a mild but not significant inhibition of lung nodule formation compared to the vehicle control. [3]
Features A potent inhibitor of the Met family, and >40-fold selectivity vs. Lck, VEGFR2, and TrkA/B and >500-fold selective vs. other receptor and non-receptor kinases.

Protocol(Only for Reference)

Kinase Assay: [4]

Met Kinase Assay The kinase reaction consists of baculovirus expressed GST-Met, 3 μg of poly(Glu/Tyr), 0.12 μCi 33P γ-ATP, 1 μM ATP in 30 μL of kinase buffer (20 mM Tris-Cl, 5 mM MnCl2, 0.1 mg/mL BSA, 0.5 mM DTT). Reactions are incubated for 1 hour at 30 °C and stopped by the addition of cold trichloroacetic acid (TCA) to a final concentration of 8%. TCA precipitates are collected onto GF/C unifilter plates using a Filtermate universal harvester, and the filters are quantitated using a TopCount 96-well liquid scintillation counter. Dose response curves are generated to determine the concentration required to inhibit 50% of substrate phosphorylation (IC50). BMS 777607 is dissolved at 10 mM in dimethylsulfoxide (DMSO) and evaluated at 10 concentrations, in duplicate.

Cell Assay: [3]

Cell lines Rodent fibrosarcoma KHT cells
Concentrations Dissolved in DMSO as a stock solution (10 mM), final concentration ~10 μM.
Incubation Time 2, 24 and 96 hours
Method KHT cells are exposed to serial dilution of BMS 777607 for 96 hours, then the MTT assay and trypan blue exclusion are used for the determination of cell proliferation and cell death, respectively. KHT cell colonies are incubated with BMS 777607 for 24 hours and then stained with crystal violet (0.1%) and photographed for the assessment of cell scattering. 2 mm scratch on the confluent KHT cell monolayer is made using a sterilized 1 ml pipette tip followed by treated with BMS-777607 for 24 hours, then the number of cells that have migrated into the denuded area is counted on 4 random fields for the evaluation of cell migration. For the examination of cell invasion, the commercial transwell inserts (8 μm pore membrane) pre-loaded with Matrigel are incubated with serum-free medium in the presence or absence of BMS 777607 at 37 °C for 2 hours to allow rehydration of Matrigel. Then cells suspended in serum-free medium are loaded onto the top chamber (5 × 103/insert) and complete medium (containing 10% FBS) is used in the lower chamber as a chemoattractant. After incubation for 24 hours, the Matrigel is removed and the inserts are stained with crystal violet. Invaded cells on the underside of the filter are photographed and counted.

Animal Study: [3]

Animal Models Rodent fibrosarcoma KHT cells are established in female C3H/HeJ mice.
Formulation Dissolved in DMSO as a stock solution (10 mM).
Dosages 10-25 mg/kg.
Administration Oral gavage once daily.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Schroeder GM, et al. J Med Chem, 2009, 52(5), 1251-1254.

[2] Dai Y, et al. Mol Cancer Ther, 2010, 9(6), 1554-1561.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-07)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01721148 Active, not recruiting Malignant Solid Tumour Aslan Pharmaceuticals October 2012 Phase 1
NCT00605618 Completed Advanced Solid Tumors Bristol-Myers Squibb March 2008 Phase 1|Phase 2

Chemical Information

Download BMS-777607 SDF
Molecular Weight (MW) 512.89
Formula

C25H19ClF2N4O4

CAS No. 1025720-94-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 47 mg/mL (91.63 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide

Customer Product Validation (6)


Click to enlarge
Rating
Source Mol Cancer Ther 2014 13(1), 37-48. BMS-777607 purchased from Selleck
Method Clonogenic growth assay
Cell Lines L3.6pl cells and CSCs+24/44/ESA
Concentrations 0-5 μM
Incubation Time 12 d
Results More than 70% reduction in colonogenic growth wasobserved when BMS-777607 was used at 5 μmol/L.

Click to enlarge
Rating
Source Mol Cancer Ther 2014 13(1), 37-48. BMS-777607 purchased from Selleck
Method Clonogenic assay
Cell Lines L3.6pl and CSCs+24/44/ESA
Concentrations 0-5 uM
Incubation Time 12 d
Results The inhibitory effect of BMS-777607 onsurvival and proliferation of L3.6pl and CSCs+24/44/ESAwas determined by the clonogenic assay. Briefly, L3.6pl cells (6,000 cells/well) in minimum essential media (MEM) with 5% FBS were cultured in duplicate in a 24-well plate and then treated with different amounts of BMS-777607 for 12 days.CSCs+24/44/ESA in stem cell culture media were incubated for 18 days in the ultra-low attachment culture plate coated with a thin layer of 0.2% of agarose tofacilitate cell anchored growth. Clonogenic cells were stained with Hema-3 staining solution (Fisher Scienti fi c), photographed using an Olympus BK71microscope equipped with CCD camera, and counted. The number of clonogenic growth from individual groups is presented.

Click to enlarge
Rating
Source Mol Oncol 2013 10.1016/j.molonc.2013.12.014. BMS-777607 purchased from Selleck
Method immunofluorescent analysis
Cell Lines T-47D and ZR-75-1 cells
Concentrations 5 uM
Incubation Time 72 h
Results Abnormal accumulation of survivin and its disassociation with condensed DNA and mitotic spindle. Both T-47D and ZR-75-1 cells were treated with 5 μM BMS-777607 for 72 h followed by immunofluorescent analysis using antibodies specific to survivin and a-tubulin. Cells were also stained with DAPI for nuclear DNA.

Click to enlarge
Rating
Source Mol Oncol 2013 8, 469-82. BMS-777607 purchased from Selleck
Method immunofluorescent analysis
Cell Lines T-47D and ZR-75-1 cells
Concentrations 5 uM
Incubation Time 3 d
Results BMS-777607 increases p21/WAF1 and survivin expression but down-regulates Rb expression. T-47D and ZR-75-1 cells (2×106 cells in 60 mm diameter culture dish) were treated with 5 mM BMS-777607 for different time intervals. Cellular proteins (50 mg per sample) from cell lysates were subjected to Western blot analysis using individual antibodies specific to p53, p21/WAF1, survivin, regular and phospho-Rb. B-actin was used as the loading control.

Click to enlarge
Rating
Source Acta Pharmacol Sin 2013 34, 1545-53. BMS-777607 purchased from Selleck
Method clonogenic assay
Cell Lines T-47D, ZR-751, and MCF-7 Cells
Concentrations 1, 2.5, 5 uM
Incubation Time 10 d
Results Effect of BMS-777607 on growth and survival of breast cancer cells. A, the effect of BMS-777607 on survival and proliferation of MCF-7, ZR-75-1, and T-47D cells was determined by clonogenic assay. Briefly, cells (8,000 cells per well) in RPMI-1640 with 5% FBS were cultured in duplicate in a 24-well plate and then treated with different amounts of BMS-777607 for 10 days. Clonogenic cells were stained with Hema-3 staining solution (Fisher Scientific) and photographed using an Olympus BK71 microscope equipped with CCD camera. B, numbers of clonogenic cells in duplicate from 3 cell lines were counted.

Click to enlarge
Rating
Source 2014 Dr.Wang from Southern Medical Hospital. BMS-777607 purchased from Selleck
Method Western blot
Cell Lines A549 cells
Concentrations 0-10 uM
Incubation Time 2 h
Results Effect of MEK inhibitor BMS-777607 in A549 cells. A549 cells were incubated with increasing concentrations of BMS-777607 for 2 h. The cell lysates were harvested and phosphorylation of indicated proteins was determined by Western blotting.

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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