BMS-777607

For research use only.

Catalog No.S1561

38 publications

BMS-777607 Chemical Structure

CAS No. 1025720-94-8

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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10mM (1mL in DMSO) GBP 204 In stock
GBP 98 In stock
GBP 171 In stock
GBP 548 In stock
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Selleck's BMS-777607 has been cited by 38 publications

Purity & Quality Control

Choose Selective c-Met Inhibitors

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.
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.
Targets
Axl [1]
(Cell-free assay)
RON [1]
(Cell-free assay)
Met [1]
(Cell-free assay)
Tyro3 [1]
(Cell-free assay)
Mer [1]
(Cell-free assay)
1.1 nM 1.8 nM 3.9 nM 4.3 nM 14 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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC-3 M4rRcGZ2dmO2aX;uJIF{e2G7 MlT2NE4yKM7:TR?= M1:wUGROW09? MXnlfIhq[mm2czDpcohq[mm2b4L5JIVn\mWldDDvckBJT0ZvaX7keYNm\CClZXzsJJNk[XS2ZYLpcoc> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0N{c,OjB3MUW5OFM9N2F-
DU145 MUTGeY5kfGmxbjDhd5NigQ>? M33yc|AvOSEQvF2= MUXEUXNQ NUP1PVdX\XiqaXLpeJMhcW6qaXLpeI9zgSCnZn\lZ5Qhd25iSFfGMYlv\HWlZXSgZ4VtdCC|Y3H0eIVzcW6p NXXBOXVyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDNpPkKwOVE2QTR|PD;hQi=>
PC-3 NF\ROVRHfW6ldHnvckBie3OjeR?= NX;SNItCOC5yMTFOwG0> MoLlSG1UVw>? M{izTZN2eHC{ZYPz[ZMhUEeILXnu[JVk\WRiY3XscEBucWe{YYTpc44> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0N{c,OjB3MUW5OFM9N2F-
DU145 MWjGeY5kfGmxbjDhd5NigQ>? MmPXNE4xOSEQvF2= MkjISG1UVw>? NYmwWFdXe3WycILld5NmeyCKR1[tbY5lfWOnZDDj[YxtKG2rZ4LheIlwdg>? M1vYc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQ{Lz5{MEWxOVk1OzxxYU6=
PC-3 MlewSpVv[3Srb36gZZN{[Xl? MYSwMlEh|ryP MYXEUXNQ Mn2zbY1x[Wm{czDIS2YudWWmaXH0[YQh[2WubDDpcpZie2mxbh?= M1ezTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQ{Lz5{MEWxOVk1OzxxYU6=
DU145 Mnz2SpVv[3Srb36gZZN{[Xl? NH7EbmoxNjFizszN M1;qd2ROW09? NG\JUJhqdXCjaYLzJGhITi2vZXTpZZRm\CClZXzsJIlvfmG|aX;u MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0N{c,OjB3MUW5OFM9N2F-
PC-3 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWfsWYZPhjFyIN88US=> MlnGSG1UVw>? NGnWOWtz\WS3Y3XzJINmdGxicILvcIln\XKjdHnvci=> NVfkO2p4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDNpPkKwOVE2QTR|PD;hQi=>
KHT MmXBT4lv[XOnIHHzd4F6 M3f0N2ROW09? M2rOV4Jtd2OtczD0bIUh[y2PZYSgd4lodmGuaX7nJJBifGi5YYmge4l1cCCLQ{WwJI9nKDFyIH7N NHPHSJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK4OlUzOyd-MkKyPFY2OjN:L3G+
KHT NYHjZlJNTnWwY4Tpc44h[XO|YYm= Mn7YglEh|ryP MnWySG1UVw>? NFzQZWtxemW4ZX70d{B{eG:wdHHu[Y92eyCNSGSgZ4VtdCC|Y3H0eIVzcW6pIIfpeIghUUN3MDDv[kAxNjFvMD61JO69VQ>? NHTwe5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK4OlUzOyd-MkKyPFY2OjN:L3G+
KHT NWTLXWVsTnWwY4Tpc44h[XO|YYm= NHTGZZN,OC53IN88US=> MUXEUXNQ NW\OO3ZZcW6qaXLpeJMh[2WubDDtbYdz[XSrb36= NILSVZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK4OlUzOyd-MkKyPFY2OjN:L3G+
KHT NUPEVGtDTnWwY4Tpc44h[XO|YYm= NFHQSXV,OC53IN88US=> MWnEUXNQ MXvpcohq[mm2czDj[YxtKGmwdnHzbY9v M1zHeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Mki2OVI{Lz5{MkK4OlUzOzxxYU6=
KHT Moq5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NETvSo1,OTBizszN NULkZW9kTE2VTx?= NWXGVIU1cW6qaXLpeJMhU0iWIHPlcIwheHKxbHnm[ZJifGmxbh?= NHzVZVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK4OlUzOyd-MkKyPFY2OjN:L3G+
T-47D MnrPS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFvwfHp,PSEQvF2= MVrEUXNQ MoL3bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR4OEWyPUc,OjN2Nki1Nlk9N2F-
ZR-75-1 M1;mVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2fu[Z42KM7:TR?= NUHDTmpjTE2VTx?= NXXmbWtScW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NGDPR4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S2PFUzQSd-MkO0Olg2Ojl:L3G+
T-47D M{DOZmZ2dmO2aX;uJIF{e2G7 MVexNEDPxE1? NHT0fWJFVVOR NYnKUXhRUW6mdXPld{Bxd2y7cHzvbYR6KGK7IEi2JEU> NIj5N4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S2PFUzQSd-MkO0Olg2Ojl:L3G+
ZR-75-1 MVPGeY5kfGmxbjDhd5NigQ>? NVW2boRPOTBizszN NInoZWdFVVOR Mn:yTY5lfWOnczDwc4x6eGyxaXT5JIJ6KDh6JR?= NFj6Zm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S2PFUzQSd-MkO0Olg2Ojl:L3G+
T-47D M1[0NGZ2dmO2aX;uJIF{e2G7 MVyxNEDPxE1? NFn2S5JFVVOR MY\pcohq[mm2czDBWXJMNUJiZoXuZ5Rqd25iYX7kJIlv\HWlZYOgbZR{KHC{b4TlbY4h\GWpcnHkZZRqd25? NEDSRXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S2PFUzQSd-MkO0Olg2Ojl:L3G+
CHRF Mn\VSpVv[3Srb36gZZN{[Xl? NUDJelhCOTBizszN NIToWHNFVVOR NI[xSVRqdmirYnn0d{Bk\WyuIHTpeol{cW:w MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyNEmwNEc,OjV|MES5NFA9N2F-
HPDE MYPGeY5kfGmxbjDhd5NigQ>? MnvCNVAh|ryP M4[5bmROW09? MmT3Zoxw[2u|IHPvcpN1cXS3dHn2[UBi[3SrdnH0bY9vKGGwZDDk[YNz\WG|ZXSgRWtVKHOrZ37hcIlv\w>? NYPQSIhYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0O|c{OTRpPkK2OFc4OzF2PD;hQi=>
U118MG M2T3W2tqdmG|ZTDhd5NigQ>? MX3+N{DPxE1? NVOxUZNjTE2VTx?= MnXFZoxw[2u|IFHYUEBxcG:|cHjvdplt[XSrb36= M3HjS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
SF126 MUnLbY5ie2ViYYPzZZk> NIDnVHR,OyEQvF2= NGOxW2tFVVOR MVTicI9kc3NiQWjMJJBpd3OyaH;yfYxifGmxbh?= NX;kTWt6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFg2OjRpPkK2PFQ5PTJ2PD;hQi=>
U118MG M4m1V2N6fG:6aXPpeJkh[XO|YYm= Mm\0NVIvPSEQvF2= M3;KOmROW09? NGPuSWtl\WO{ZXHz[ZMh\2yrb33hJINmdGxidnnhZoltcXS7 MmnoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NEi1NlQoRjJ4OES4OVI1RC:jPh?=
SF126 NXLIT2N2S3m2b4jpZ4l1gSCjc4PhfS=> MWKxNk42KM7:TR?= MXrEUXNQ NWnGUZlw\GWlcnXhd4V{KGeuaX;tZUBk\WyuII\pZYJqdGm2eR?= Ml\BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NEi1NlQoRjJ4OES4OVI1RC:jPh?=
U118MG MnTFRZBweHSxc3nzJIF{e2G7 M4PO[lEzNjVizszN NH3nRYdFVVOR MWTpcoR2[2W|IHfsbY9u[SClZXzsJIFxd3C2b4Ppdy=> M4O3d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
SF126 M{XDWGFxd3C2b4Ppd{Bie3OjeR?= M2\CcFEzNjVizszN M4rufmROW09? NH7mNXFqdmS3Y3XzJIdtcW:vYTDj[YxtKGGyb4D0c5Nqew>? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh2OEWyOEc,OjZ6NEi1NlQ9N2F-
U118MG NWnybWRETnWwY4Tpc44h[XO|YYm= Mn3rNVIvPSEQvF2= MofWSG1UVw>? NGDRUmhjdG:la4Og[4xqd22jIHPlcIwhdWmpcnH0bY9vKGGwZDDpcpZie2m4ZTDndo94fGhicHH0eIVzdg>? NGDQ[|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PFUzPCd-Mk[4OFg2OjR:L3G+
SF126 Ml\3SpVv[3Srb36gZZN{[Xl? NHjsW4kyOi53IN88US=> MX7EUXNQ NH64SmJjdG:la4Og[4xqd22jIHPlcIwhdWmpcnH0bY9vKGGwZDDpcpZie2m4ZTDndo94fGhicHH0eIVzdg>? NF;tNmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PFUzPCd-Mk[4OFg2OjR:L3G+
GTL16 NV7yO45LTnWwY4Tpc44h[XO|YYm= MlzWN|AhdWmwcx?= NIfPUWFKdmirYnn0bY9vKG:oIF3leEBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gS3RNOTZiY3XscJMh[W[2ZYKgN|AhdWmwczygTWM2OCB;IECuNFIh|ryPLh?= M{W2[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7Mk[wO|EyLz5zOUK2NFcyOTxxYU6=
GTL16 MlvXRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NFPTVFE4OiCqcoO= MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IF3leE1l\XCnbnTlcpQhcHWvYX6gS3RNOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VWyCjc4PhfUwhUUN3MDC9JFAvOSEQvF2u M{OyPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7Mk[wO|EyLz5zOUK2NFcyOTxxYU6=
NCI-H1993 MV3BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NFnnPJI4OiCqcoO= MlflRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDN[ZQu\GWyZX7k[Y51KGi3bXHuJG5EUS2KMUm5N{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTTJIF{e2G7LDDJR|UxKD1iMD6xOUDPxE1w MnLHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{NkC3NVEoRjF7Mk[wO|EyRC:jPh?=
U87 NVrvWFRFSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M2T4NlczKGi{cx?= MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IF3leE1lemm4ZX6gbJVu[W5iVUi3JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkG2JO69VS5? NF;Kb4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK2NFcyOSd-MUmyOlA4OTF:L3G+
BAF3 NIfFc4FEgXSxdH;4bYNqfHliYYPzZZk> MkTEO|IhcHK| NULjT3M{S3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIGTQVk1O\XRiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{NCCLQ{WwJF0hOC5zOEi0JO69VS5? NH7PZmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe5Nlc4PCd-MkS3PVI4PzR:L3G+
DU145 NGfUV3dCdnSraX72ZZNqfmViYYPzZZk> M2DrXlEhcHJ? MXrBcpRqcW64YYPpeoUh[WO2aY\peJkhcW5iaIXtZY4hTFVzNEWgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCKR1[tbY5lfWOnZDDj[YxtKG2xdHnsbZR6KHC{ZXnuZ5Vj[XSnZDDmc5IhOSCqcjDi[YZwemViSFfGJJRz\WG2bXXueEBu\WG|dYLl[EBi\nSncjCyOEBpenNiYomgZ4VtdCC|Y3H0eIVzcW6pIHHzd4F6NCCLQ{WwJF0hOC5{IN88UU4> M2e3eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwPFMxLz5{NEmwNFg{ODxxYU6=
MKN45 M2nKTGN6fG:2b4jpZ4l1gSCjc4PhfS=> MkXEO|IhcHK| NFzteYlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOU052NTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMtKEmFNUCgQUAxNjJ6NUig{txONg>? M3XiUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{myO|c1Lz5{NEe5Nlc4PDxxYU6=
NCI-H1993 Mn;IR5l1d3SxeHnjbZR6KGG|c3H5 M3;6flQ5KGi{cx?= NGDjbJdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0lvSEG5PVMh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEGuNVA5KM7:TT6= NVS5Wld5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA5OzBpPkK0PVAxQDNyPD;hQi=>
GTL16 NIX0V45HfW6ldHnvckBie3OjeR?= MWW2MlI2KG2pL3vn MXzDcYF5KGmwIHj1cYFvKEeWTEG2JINmdGy|IIjlco9oemGodHXkJIF1cHmvaXOgcY92e2ViYYSgOk4zPSCvZz;r[{wheG9uIFPtZZghRSB2LkWg{txONg>? NH7JNGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK2NFcyOSd-MUmyOlA4OTF:L3G+
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SJ-GBM2 M2CzTZFJXFNiYYPzZZk> MofFdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= M1jaXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673 NV;YfIRqeUiWUzDhd5NigQ>? M2ju[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| Mor6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC Ml3FdWhVWyCjc4PhfS=> MWTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= Mo\TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 M{DtSJFJXFNiYYPzZZk> M{\J[5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO= NFOySoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 MX\xTHRUKGG|c3H5 Ml\BdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| M3\mdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 MXjxTHRUKGG|c3H5 NVvnOpp5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> NHTCbow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 M2TLU5FJXFNiYYPzZZk> NYfSd417eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl? M1\xcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC MWPxTHRUKGG|c3H5 M2rMTZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN? NVjKSXB1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 NGW1SWpyUFSVIHHzd4F6 MWfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTTk1ISk1{IHPlcIx{ NYT5OZRnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32 Mnn2dWhVWyCjc4PhfS=> MXPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz M2nJSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) Ml\FdWhVWyCjc4PhfS=> M{\BWZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG1IKDZ|IDi2MXRIKFJrIHPlcIx{ MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MGHU3 M1;kc2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MVW3NkBpenN? NWLJR2p2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNS2hWOyClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfS=> NYizXW5MRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzNFk3PzFpPkOwN|A6PjdzPD;hQi=>
RT112 Ml34RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NF;SZW04OiCqcoO= NFPndHJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGLUNVEzKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5 MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODNyOU[3NUc,OzB|MEm2O|E9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-c-Met / c-Met / p-FAK / p-c-Src / p-Akt / p-S6K / p-S6; 

PubMed: 22639908     


Effect of BMS-777607 on c-Met signaling in PC-3 cells PC-3 cells were treated with indicated doses of BMS-777607 for 1 h (A) or with BMS-777607 (1 μM) for indicated times (B). Whole cell lysates were harvested and analyzed by Western blot, with actin as a loading control. Data represent 1 of 2 independent experiments.

p53 / p21 / Survivin / p-Rb / Rb ; 

PubMed: 24444656     


BMS-777607 increases p21/WAF1 and survivin expression but down-regulates Rb expression. T-47D and ZR-75-1 cells were treated with 5 μM BMS-777607 for different time intervals. Cellular proteins (50 μg 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.

22639908 24444656
Immunofluorescence
α-tubulin / survivin; 

PubMed: 24444656     


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 α-tubulin. Cells were also stained with DAPI for nuclear DNA. Images shown here are from one of two experiments with similar results.

24444656
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]

Protocol

Kinase Assay:[4]
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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 Research:[3]
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  • 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.
    (Only for Reference)
Animal Research:[3]
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  • Animal Models: Rodent fibrosarcoma KHT cells are established in female C3H/HeJ mice.
  • Dosages: 10-25 mg/kg.
  • Administration: Oral gavage once daily.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 47 mg/mL (91.63 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+45% PEG 300+5% Tween 80+ddH2O
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 512.89
Formula

C25H19ClF2N4O4

CAS No. 1025720-94-8
Storage powder
in solvent
Synonyms N/A
Smiles CCOC1=C(C(=O)N(C=C1)C2=CC=C(C=C2)F)C(=O)NC3=CC(=C(C=C3)OC4=C(C(=NC=C4)N)Cl)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

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Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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:

    What formulation can we use to dissolve S1561 for mice in vivo study?

  • Answer:

    S1561 BMS-777607 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30 mg/ml is a suspension. It is fine for oral gavage. If you are going to use it for injection, please try the following vehicle: 4% DMSO+30% PEG 300+ddH2O. BMS-777607 can be dissolved in it at 5 mg/ml as a clear solution.

c-Met Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID