BMS-777607

For research use only.

Catalog No.S1561 Synonyms: BMS 817378

43 publications

BMS-777607 Chemical Structure

CAS No. 1025720-94-8

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.

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Selleck's BMS-777607 has been cited by 43 publications

Purity & Quality Control

Choose Selective c-Met Inhibitors

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)
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 NHP6SndHfW6ldHnvckBie3OjeR?= MoT0NE4yKM7:TR?= MWfEUXNQ NYfkWHNX\XiqaXLpeJMhcW6qaXLpeI9zgSCnZn\lZ5Qhd25iSFfGMYlv\HWlZXSgZ4VtdCC|Y3H0eIVzcW6p MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0N{c,OjB3MUW5OFM9N2F-
DU145 NVHuT45jTnWwY4Tpc44h[XO|YYm= M3\ae|AvOSEQvF2= MlnkSG1UVw>? NW\iXoV3\XiqaXLpeJMhcW6qaXLpeI9zgSCnZn\lZ5Qhd25iSFfGMYlv\HWlZXSgZ4VtdCC|Y3H0eIVzcW6p M3f5ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQ{Lz5{MEWxOVk1OzxxYU6=
PC-3 M{XYTmZ2dmO2aX;uJIF{e2G7 NVK3UXV7OC5yMTFOwG0> M2WwPWROW09? M1;5R5N2eHC{ZYPz[ZMhUEeILXnu[JVk\WRiY3XscEBucWe{YYTpc44> MoDzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3MUW5OFMoRjJyNUG1PVQ{RC:jPh?=
DU145 MV3GeY5kfGmxbjDhd5NigQ>? NI\nPZgxNjBzIN88US=> Mnn5SG1UVw>? MU\zeZBxemW|c3XzJGhITi2rbnT1Z4VlKGOnbHygcYloemG2aX;u NGfIRXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1Oyd-MkC1NVU6PDN:L3G+
PC-3 NHXqXVBHfW6ldHnvckBie3OjeR?= MVOwMlEh|ryP MVPEUXNQ M3\jOYlueGGrcoOgTGdHNW2nZHnheIVlKGOnbHygbY53[XOrb36= NHS4clM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1Oyd-MkC1NVU6PDN:L3G+
DU145 MXLGeY5kfGmxbjDhd5NigQ>? M1nv[lAvOSEQvF2= NYPGfodoTE2VTx?= MVvpcZBicXK|IFjHSk1u\WSrYYTl[EBk\WyuIHnueoF{cW:w M1\mdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQ{Lz5{MEWxOVk1OzxxYU6=
PC-3 NV;BcmdiT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXywPWdthjFyIN88US=> NHXrZ4pFVVOR M1vNTpJm\HWlZYOgZ4VtdCCycn;sbYZmemG2aX;u NHLHW409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1Oyd-MkC1NVU6PDN:L3G+
KHT MnSyT4lv[XOnIHHzd4F6 NIXGeJNFVVOR MorQZoxw[2u|IITo[UBkNU2ndDDzbYdv[WyrbnegdIF1cHejeTD3bZRpKEmFNUCgc4YhOTBibl2= MnzlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
KHT M2TTe2Z2dmO2aX;uJIF{e2G7 NGGwb49,OSEQvF2= M{D6UmROW09? Mmn3dJJmfmWwdIOgd5BwdnSjbnXveZMhU0iWIHPlcIwhe2OjdITldolv\yC5aYToJGlEPTBib3[gNE4yNTBwNTFOwG0> MnKzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
KHT MoLtSpVv[3Srb36gZZN{[Xl? M{LwNZ4xNjVizszN Ml7VSG1UVw>? M2e3bolvcGmkaYTzJINmdGxibXnndoF1cW:w M2\0SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Mki2OVI{Lz5{MkK4OlUzOzxxYU6=
KHT NIi0ZXJHfW6ldHnvckBie3OjeR?= NICzbGF,OC53IN88US=> MVLEUXNQ MmXQbY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>? NVjhU4tVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyPFY2OjNpPkKyNlg3PTJ|PD;hQi=>
KHT M{TDfWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{XnVJ4yOCEQvF2= NFfvZ3dFVVOR NV;aT2pmcW6qaXLpeJMhU0iWIHPlcIwheHKxbHnm[ZJifGmxbh?= MoKzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
T-47D MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUHpZYxPhjVizszN NXnSd2FxTE2VTx?= NV3lWFRucW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MoPjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2Nki1NlkoRjJ|NE[4OVI6RC:jPh?=
ZR-75-1 M{\QZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1T0TZ42KM7:TR?= NVW2fHRwTE2VTx?= NEKwfFVqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR4OEWyPUc,OjN2Nki1Nlk9N2F-
T-47D M{\0OWZ2dmO2aX;uJIF{e2G7 NInpOHEyOCEQvF2= M2K3[2ROW09? Mke1TY5lfWOnczDwc4x6eGyxaXT5JIJ6KDh4IDW= M{TCb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NE[4OVI6Lz5{M{S2PFUzQTxxYU6=
ZR-75-1 MmnMSpVv[3Srb36gZZN{[Xl? M2L1WVExKM7:TR?= M4nYbWROW09? MWfJcoR2[2W|IIDvcJlxdG:rZImgZpkhQDhn NH3xdmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S2PFUzQSd-MkO0Olg2Ojl:L3G+
T-47D NVfkdm5GTnWwY4Tpc44h[XO|YYm= MoGyNVAh|ryP NV7qU2l[TE2VTx?= MXPpcohq[mm2czDBWXJMNUJiZoXuZ5Rqd25iYX7kJIlv\HWlZYOgbZR{KHC{b4TlbY4h\GWpcnHkZZRqd25? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR4OEWyPUc,OjN2Nki1Nlk9N2F-
CHRF MnXwSpVv[3Srb36gZZN{[Xl? NEO5fmYyOCEQvF2= M3jaZ2ROW09? M2i0TYlvcGmkaYTzJINmdGxiZHn2bZNqd25? NIjUV4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwOFkxOCd-MkWzNFQ6ODB:L3G+
HPDE Mk\qSpVv[3Srb36gZZN{[Xl? NFvubWQyOCEQvF2= M{LlZ2ROW09? MYficI9kc3NiY3;ud5RqfHW2aY\lJIFkfGm4YYTpc44h[W6mIHTlZ5Jm[XOnZDDBT3Qhe2mpbnHsbY5o Mlf6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2N{ezNVQoRjJ4NEe3N|E1RC:jPh?=
U118MG M1ruZ2tqdmG|ZTDhd5NigQ>? MlTFglMh|ryP MUnEUXNQ MlP5Zoxw[2u|IFHYUEBxcG:|cHjvdplt[XSrb36= NUDKfYJHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFg2OjRpPkK2PFQ5PTJ2PD;hQi=>
SF126 NV62VZNlU2mwYYPlJIF{e2G7 NGTwfWZ,OyEQvF2= NGjDSmhFVVOR MUXicI9kc3NiQWjMJJBpd3OyaH;yfYxifGmxbh?= NFLRV|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PFUzPCd-Mk[4OFg2OjR:L3G+
U118MG NUKxN4g6S3m2b4jpZ4l1gSCjc4PhfS=> MW[xNk42KM7:TR?= NGXsTmtFVVOR M1PLOYRm[3KnYYPld{BodGmxbXGgZ4VtdCC4aXHibYxqfHl? M3\nd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
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U118MG Mnn6RZBweHSxc3nzJIF{e2G7 MYSxNk42KM7:TR?= NVL1S4hqTE2VTx?= NWThc3BkcW6mdXPld{BodGmxbXGgZ4VtdCCjcH;weI9{cXN? MnXXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NEi1NlQoRjJ4OES4OVI1RC:jPh?=
SF126 NVvDSHlrSXCxcITvd4l{KGG|c3H5 NU\qfpR6OTJwNTFOwG0> MY\EUXNQ M1TIcolv\HWlZYOg[4xqd22jIHPlcIwh[XCxcITvd4l{ MlX0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NEi1NlQoRjJ4OES4OVI1RC:jPh?=
U118MG MXjGeY5kfGmxbjDhd5NigQ>? MXWxNk42KM7:TR?= M{nNe2ROW09? MoP1Zoxw[2u|IHfsbY9u[SClZXzsJI1q\3KjdHnvckBidmRiaX72ZZNqfmViZ4Lve5RpKHCjdITldo4> NX;y[FNqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFg2OjRpPkK2PFQ5PTJ2PD;hQi=>
SF126 NVrZfGtLTnWwY4Tpc44h[XO|YYm= MnTFNVIvPSEQvF2= MVjEUXNQ M{fQ[IJtd2OtczDncIlwdWFiY3XscEBucWe{YYTpc44h[W6mIHnueoF{cX[nIHfyc5d1cCCyYYT0[ZJv MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh2OEWyOEc,OjZ6NEi1NlQ9N2F-
GTL16 MUjGeY5kfGmxbjDhd5NigQ>? NVLWeFlqOzBibXnudy=> NYLjN4l[UW6qaXLpeIlwdiCxZjDN[ZQheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGdVVDF4IHPlcIx{KGGodHXyJFMxKG2rboOsJGlEPTBiPTCwMlAzKM7:TT6= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ4MEexNUc,OTl{NkC3NVE9N2F-
GTL16 NFLWVo9CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M3H5Z|czKGi{cx?= M4L1WmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgUYV1NWSncHXu[IVvfCCqdX3hckBIXExzNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCLQ{WwJF0hOC5zIN88UU4> NYXhVmZCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyOlA4OTFpPkG5NlYxPzFzPD;hQi=>
NCI-H1993 NIj6SVhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M{Due|czKGi{cx?= M4TJR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgUYV1NWSncHXu[IVvfCCqdX3hckBPS0lvSEG5PVMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OCB;IECuNVUh|ryPLh?= NIfO[YY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK2NFcyOSd-MUmyOlA4OTF:L3G+
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BAF3 NH7XUohEgXSxdH;4bYNqfHliYYPzZZk> Ml\VO|IhcHK| NH\3fGhEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiVGDSMW1mfCCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMtKEmFNUCgQUAxNjF6OESg{txONg>? MlnCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5OUK3O|QoRjJ2N{myO|c1RC:jPh?=
DU145 MUjBcpRqcW64YYPpeoUh[XO|YYm= MWSxJIhz M{jaWGFvfGmrbo\hd4l3\SCjY4Tpeol1gSCrbjDoeY1idiCGVUG0OUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFjHSk1qdmS3Y3XkJINmdGxibX;0bYxqfHlicILlbY5kfWKjdHXkJIZweiBzIHjyJIJm\m:{ZTDIS2YhfHKnYYTt[Y51KG2nYYP1doVlKGGodHXyJFI1KGi{czDifUBk\WyuIIPjZZR1\XKrbnegZZN{[XluIFnDOVAhRSByLkKg{txONg>? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEizNEc,OjR7MEC4N|A9N2F-
MKN45 NXj1NmtxS3m2b4TvfIlkcXS7IHHzd4F6 MYm3NkBpenN? Mm\mR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWtPPDViY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzMEBKSzVyIE2gNE4zQDV6IN88UU4> Ml3EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5OUK3O|QoRjJ2N{myO|c1RC:jPh?=
NCI-H1993 M13nUGN6fG:2b4jpZ4l1gSCjc4PhfS=> Mlz4OFghcHK| NWrDdGdJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkOLLVixPVk{KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxMlExQCEQvF2u NEG4bHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFg{OCd-MkS5NFA5OzB:L3G+
GTL16 NEX2U4ZHfW6ldHnvckBie3OjeR?= Ml[4Ok4zPSCvZz;r[y=> NWXBV4EzS22jeDDpckBpfW2jbjDHWGwyPiClZXzsd{B5\W6xZ4Lh[pRm\CCjdHj5cYlkKG2xdYPlJIF1KDZwMkWgcYcwc2duIIDvMEBEdWG6IE2gOE42KM7:TT6= NWmzSGFmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyOlA4OTFpPkG5NlYxPzFzPD;hQi=>
GTL16 MUjGeY5kfGmxbjDhd5NigQ>? M4HISlUxKG2pL3vn MlrrR41igCCrbjDoeY1idiCJVFyxOkBk\WyuczD4[Y5w\3KjZoTl[EBifGi7bXnjJI1wfXOnIHH0JFUxKG2pL3vnMEBxdyxiQ33hfEA:KDR|Lkeg{txONg>? NHvwOmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK2NFcyOSd-MUmyOlA4OTF:L3G+
SJ-GBM2 MmPDdWhVWyCjc4PhfS=> NFz3ZoJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> NHXUeno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 MV7xTHRUKGG|c3H5 MmXidWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? M1G1ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC M4jCcJFJXFNiYYPzZZk> NFfhVYVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> M1TWUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 NFWyfoJyUFSVIHHzd4F6 MkfudWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?= NETDTnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 NUfQSGR6eUiWUzDhd5NigQ>? NUnXVIo4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz M1zQT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 MWTxTHRUKGG|c3H5 M17tUZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= NGLKS2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 MX7xTHRUKGG|c3H5 NWLIR45YeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC NH\TOW9yUFSVIHHzd4F6 MkHmdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2PQzDj[Yxtew>? MlzWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2 NGPSO29yUFSVIHHzd4F6 NHXaNJhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUi2JQl2yJINmdGy| MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
TC32 NGDhUIxyUFSVIHHzd4F6 MYPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz NFvmOoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MG 63 (6-TG R) NHrZfmxyUFSVIHHzd4F6 MYDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDNS{A3OyBqNj3US{BTMSClZXzsdy=> NF;NN5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MGHU3 MXTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NH3BSYU4OiCqcoO= Mn7DRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPR1jVN{Bk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeR?= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODNyOU[3NUc,OzB|MEm2O|E9N2F-
RT112 NVKycZFKSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M1PP[VczKGi{cx?= NGTRfpJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGLUNVEzKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5 M2K5dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{C5OlcyLz5|MEOwPVY4OTxxYU6=

... 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 BMS 817378
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

Bio Calculators

Molarity Calculator

Molarity Calculator

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)

  • Mass
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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).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

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.

  • * Indicates a Required Field

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