BMS-777607

Catalog No.S1561 Synonyms: BMS 817378

For research use only.

BMS-777607 (BMS 817378) 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.

BMS-777607 Chemical Structure

CAS No. 1025720-94-8

Selleck's BMS-777607 has been cited by 49 publications

Purity & Quality Control

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Biological Activity

Description BMS-777607 (BMS 817378) 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)
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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 MULGeY5kfGmxbjDhd5NigQ>? M3nYfFAvOSEQvF2= MXnEUXNQ MlPW[ZhpcWKrdIOgbY5pcWKrdH;yfUBm\m[nY4Sgc44hUEeILXnu[JVk\WRiY3XscEB{[2G2dHXybY5o NFTxc4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1Oyd-MkC1NVU6PDN:L3G+
DU145 NYPOWph5TnWwY4Tpc44h[XO|YYm= NXnIO4p[OC5zIN88US=> MXnEUXNQ M1LuZYV5cGmkaYTzJIlvcGmkaYTvdpkh\W[oZXP0JI9vKEiJRj3pcoR2[2WmIHPlcIwhe2OjdITldolv\w>? M3G0b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQ{Lz5{MEWxOVk1OzxxYU6=
PC-3 MWDGeY5kfGmxbjDhd5NigQ>? NFPTU3oxNjBzIN88US=> MVfEUXNQ Mnzyd5VxeHKnc4Pld{BJT0ZvaX7keYNm\CClZXzsJI1q\3KjdHnvci=> NEnDb4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1Oyd-MkC1NVU6PDN:L3G+
DU145 M4P3emZ2dmO2aX;uJIF{e2G7 MlvLNE4xOSEQvF2= NWjMNlNNTE2VTx?= MXLzeZBxemW|c3XzJGhITi2rbnT1Z4VlKGOnbHygcYloemG2aX;u Ml7YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3MUW5OFMoRjJyNUG1PVQ{RC:jPh?=
PC-3 MnjtSpVv[3Srb36gZZN{[Xl? NEXoN2IxNjFizszN NHnX[|BFVVOR NUPrVYhscW2yYXnyd{BJT0ZvbXXkbYF1\WRiY3XscEBqdn[jc3nvci=> M1TmVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQ{Lz5{MEWxOVk1OzxxYU6=
DU145 MVjGeY5kfGmxbjDhd5NigQ>? MnfvNE4yKM7:TR?= NH3yTJBFVVOR NX\NWlM4cW2yYXnyd{BJT0ZvbXXkbYF1\WRiY3XscEBqdn[jc3nvci=> M3f3N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQ{Lz5{MEWxOVk1OzxxYU6=
PC-3 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmfqglExKM7:TR?= M1;CcWROW09? MmXDdoVlfWOnczDj[YxtKHC{b3zp[oVz[XSrb36= NUXsemkxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDNpPkKwOVE2QTR|PD;hQi=>
KHT MYDLbY5ie2ViYYPzZZk> NIS2foVFVVOR MnLxZoxw[2u|IITo[UBkNU2ndDDzbYdv[WyrbnegdIF1cHejeTD3bZRpKEmFNUCgc4YhOTBibl2= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ6NkWyN{c,OjJ{OE[1NlM9N2F-
KHT MlvJSpVv[3Srb36gZZN{[Xl? M2DBXZ4yKM7:TR?= NYW5dWJTTE2VTx?= NGTaempxemW4ZX70d{B{eG:wdHHu[Y92eyCNSGSgZ4VtdCC|Y3H0eIVzcW6pIIfpeIghUUN3MDDv[kAxNjFvMD61JO69VQ>? NUTMe5RMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyPFY2OjNpPkKyNlg3PTJ|PD;hQi=>
KHT NGLySJVHfW6ldHnvckBie3OjeR?= MoizglAvPSEQvF2= NGX6OYtFVVOR Mn3wbY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? MlnDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
KHT M2n2N2Z2dmO2aX;uJIF{e2G7 NXnmR3lphjBwNTFOwG0> M{TpTWROW09? MYnpcohq[mm2czDj[YxtKGmwdnHzbY9v MkfzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
KHT NIPHOJRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH[xXFJ,OTBizszN M{\qb2ROW09? MkLYbY5pcWKrdIOgT2hVKGOnbHygdJJwdGmoZYLheIlwdg>? MnLLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
T-47D MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NY[3PZpohjVizszN M1jU[GROW09? NVO0PYtlcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M4rLNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NE[4OVI6Lz5{M{S2PFUzQTxxYU6=
ZR-75-1 M1Xp[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVzl[3I6hjVizszN M{TRWGROW09? MUTpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= Ml\uQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2Nki1NlkoRjJ|NE[4OVI6RC:jPh?=
T-47D NVixNnZQTnWwY4Tpc44h[XO|YYm= NFr4RosyOCEQvF2= NFLacoVFVVOR MkHlTY5lfWOnczDwc4x6eGyxaXT5JIJ6KDh4IDW= Ml;BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2Nki1NlkoRjJ|NE[4OVI6RC:jPh?=
ZR-75-1 NF7jN3pHfW6ldHnvckBie3OjeR?= NFPlbGgyOCEQvF2= MlXlSG1UVw>? MkjzTY5lfWOnczDwc4x6eGyxaXT5JIJ6KDh6JR?= MnvRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2Nki1NlkoRjJ|NE[4OVI6RC:jPh?=
T-47D NInZOYZHfW6ldHnvckBie3OjeR?= M1;sU|ExKM7:TR?= M3zoU2ROW09? MWPpcohq[mm2czDBWXJMNUJiZoXuZ5Rqd25iYX7kJIlv\HWlZYOgbZR{KHC{b4TlbY4h\GWpcnHkZZRqd25? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR4OEWyPUc,OjN2Nki1Nlk9N2F-
CHRF NEHtW4tHfW6ldHnvckBie3OjeR?= M1jJcFExKM7:TR?= MUjEUXNQ NGLFXWtqdmirYnn0d{Bk\WyuIHTpeol{cW:w MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyNEmwNEc,OjV|MES5NFA9N2F-
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SF126 NWe5[4tzU2mwYYPlJIF{e2G7 MVn+N{DPxE1? MmjFSG1UVw>? MkXjZoxw[2u|IFHYUEBxcG:|cHjvdplt[XSrb36= M3rVXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
U118MG Mnf2R5l1d3irY3n0fUBie3OjeR?= NWn0ZWo{OTJwNTFOwG0> NEnIVVFFVVOR NV;lT3Mz\GWlcnXhd4V{KGeuaX;tZUBk\WyuII\pZYJqdGm2eR?= MmLkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NEi1NlQoRjJ4OES4OVI1RC:jPh?=
SF126 NVPzeVRrS3m2b4jpZ4l1gSCjc4PhfS=> MYSxNk42KM7:TR?= M{DFWmROW09? Mlr1[IVkemWjc3XzJIdtcW:vYTDj[YxtKH[rYXLpcIl1gQ>? NHiyOWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PFUzPCd-Mk[4OFg2OjR:L3G+
U118MG M36zNGFxd3C2b4Ppd{Bie3OjeR?= MkC4NVIvPSEQvF2= MVnEUXNQ Mn7sbY5lfWOnczDncIlwdWFiY3XscEBieG:ydH;zbZM> NETyVmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PFUzPCd-Mk[4OFg2OjR:L3G+
SF126 MXvBdI9xfG:|aYOgZZN{[Xl? MVWxNk42KM7:TR?= M2P1bGROW09? M3LSWolv\HWlZYOg[4xqd22jIHPlcIwh[XCxcITvd4l{ NF;pOGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PFUzPCd-Mk[4OFg2OjR:L3G+
U118MG MkSwSpVv[3Srb36gZZN{[Xl? MWixNk42KM7:TR?= MWTEUXNQ Mk\BZoxw[2u|IHfsbY9u[SClZXzsJI1q\3KjdHnvckBidmRiaX72ZZNqfmViZ4Lve5RpKHCjdITldo4> NWrwOVNNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFg2OjRpPkK2PFQ5PTJ2PD;hQi=>
SF126 MYDGeY5kfGmxbjDhd5NigQ>? Mn3uNVIvPSEQvF2= NIDGd2FFVVOR Mlu5Zoxw[2u|IHfsbY9u[SClZXzsJI1q\3KjdHnvckBidmRiaX72ZZNqfmViZ4Lve5RpKHCjdITldo4> M17hR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
GTL16 MVTGeY5kfGmxbjDhd5NigQ>? NWDYSppUOzBibXnudy=> NV\GcG5OUW6qaXLpeIlwdiCxZjDN[ZQheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGdVVDF4IHPlcIx{KGGodHXyJFMxKG2rboOsJGlEPTBiPTCwMlAzKM7:TT6= MmLGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{NkC3NVEoRjF7Mk[wO|EyRC:jPh?=
GTL16 M2fBOGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M4\YZ|czKGi{cx?= MlLsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDN[ZQu\GWyZX7k[Y51KGi3bXHuJGdVVDF4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEmFNUCgQUAxNjFizszNMi=> NHfvR2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK2NFcyOSd-MUmyOlA4OTF:L3G+
NCI-H1993 MXvBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NHHKUms4OiCqcoO= MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IF3leE1l\XCnbnTlcpQhcHWvYX6gUmNKNUhzOUmzJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkG1JO69VS5? NET3TGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK2NFcyOSd-MUmyOlA4OTF:L3G+
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DU145 NVXUXYN3SW62aXnueoF{cX[nIHHzd4F6 M{\Yb|EhcHJ? NH7E[m9CdnSraX72ZZNqfmViYXP0bZZqfHliaX6gbJVu[W5iRGWxOFUh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDIS2YucW6mdXPl[EBk\WyuIH3veIltcXS7IIDy[Ylv[3WkYYTl[EBnd3JiMTDodkBj\W[xcnWgTGdHKHS{ZXH0cYVvfCCvZXHzeZJm\CCjZoTldkAzPCCqcoOgZpkh[2WubDDzZ4F1fGW{aX7nJIF{e2G7LDDJR|UxKD1iMD6yJO69VS5? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEizNEc,OjR7MEC4N|A9N2F-
MKN45 M4rZemN6fG:2b4jpZ4l1gSCjc4PhfS=> NUjJRZRQPzJiaILz NXew[oFKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUuQNEWgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{NCCLQ{WwJF0hOC5{OEW4JO69VS5? MmTGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5OUK3O|QoRjJ2N{myO|c1RC:jPh?=
NCI-H1993 NYKyfVhqS3m2b4TvfIlkcXS7IHHzd4F6 NVvQc3pbPDhiaILz MoTzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNUhzOUmzJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLkGwPEDPxE1w MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEizNEc,OjR7MEC4N|A9N2F-
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A673 MWDxTHRUKGG|c3H5 NEn5NItyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= NHjFfpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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LAN-5 NHXqdWVyUFSVIHHzd4F6 M37zbpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= Mn74QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 NEjjb2tyUFSVIHHzd4F6 NIG5R|ZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
A673 M4TkPJFJXFNiYYPzZZk> NU\CZYdDeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl? M2TXdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC MVHxTHRUKGG|c3H5 NXLtdFhxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= M{jYSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 MUTxTHRUKGG|c3H5 MYLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTTk1ISk1{IHPlcIx{ NXr3eXhzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32 M1vxNZFJXFNiYYPzZZk> M1uyepFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM> NYOyO3NsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) MVzxTHRUKGG|c3H5 MVHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDNS{A3OyBqNj3US{BTMSClZXzsdy=> NFTM[YM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MGHU3 NXT3OVBMSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NXHQR|REPzJiaILz MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2JSGWzJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7 NXjVe3RPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzNFk3PzFpPkOwN|A6PjdzPD;hQi=>
RT112 NIW0ZopCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NVXIcG81PzJiaILz M3qzXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmSxNVIh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYm= M17QU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{C5OlcyLz5|MEOwPVY4OTxxYU6=
Assay
Methods Test Index PMID
Western blot p-c-Met / c-Met / p-FAK / p-c-Src / p-Akt / p-S6K / p-S6 ; p53 / p21 / Survivin / p-Rb / Rb 22639908 24444656
Immunofluorescence α-tubulin / survivin 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 (from 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 Research:[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 Research:[3]
  • Animal Models: Rodent fibrosarcoma KHT cells are established in female C3H/HeJ mice.
  • Dosages: 10-25 mg/kg.
  • Administration: Oral gavage once daily.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 512.89
Formula

C25H19ClF2N4O4

CAS No. 1025720-94-8
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01721148 Completed Drug: ASLAN002( BMS 777607) Malignant Solid Tumour Aslan Pharmaceuticals October 2012 Phase 1
NCT00605618 Completed Drug: BMS-777607 Advanced Solid Tumors Bristol-Myers Squibb March 2008 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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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.

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