BMS-777607

For research use only. Not for use in humans.

目录号：S1561 别名： BMS 817378

BMS-777607 Chemical Structure

CAS No. 1025720-94-8

BMS-777607 (BMS 817378)是一种Met相关的抑制剂，作用于c-Met，Axl，Ron和Tyro3，在无细胞试验中IC50分别为3.9 nM，1.1 nM，1.8 nM和4.3 nM，作用于Met相关靶点比作用于Lck， VEGFR-2，和TrkA/B选择性高40倍，比作用于其他受体和非受体激酶选择性高500多倍。Phase 1/2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2041.38 现货
RMB 976.53 现货
RMB 1706.13 现货
RMB 5498.71 现货
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客户使用Selleck生产的BMS-777607发表文献47篇：

产品安全说明书

c-Met抑制剂选择性比较

生物活性

产品描述 BMS-777607 (BMS 817378)是一种Met相关的抑制剂，作用于c-Met，Axl，Ron和Tyro3，在无细胞试验中IC50分别为3.9 nM，1.1 nM，1.8 nM和4.3 nM，作用于Met相关靶点比作用于Lck， VEGFR-2，和TrkA/B选择性高40倍，比作用于其他受体和非受体激酶选择性高500多倍。Phase 1/2。
特性 BMS 777607是有效的Met家族成员抑制剂，比作用于Lck, VEGFR-2,和TrkA/B的选择性高40多倍，比作用同样其他受体和非受体激酶选择性高500多倍。
靶点
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
体外研究

BMS-777607是ATP竞争性Met激酶选择性抑制剂，有效抑制c-Met自磷酸化，作用于GTL-16细胞裂解物， IC50为20 nM，且选择性抑制Met驱动的肿瘤细胞系如GTL-16细胞系, H1993和 U87增殖。[1] BMS-777607 作用于DU145前列腺癌细胞，抑制肝细胞生长因子 (HGF)引起的c-Met自磷酸化， IC50<1 nM 。BMS 777607对肿瘤细胞生长作用效果不大，但是作用于PC-3 和DU145 细胞，抑制HGF诱导的细胞分散。BMS 777607作用于这两种细胞，也抑制刺激的细胞迁移和入侵，IC50<0.1 μM，这种作用存在剂量依赖性。[2] BMS 777607(~10 μM)作用于高度转移性鼠科KHT细胞2小时，有效清除自磷酸化的c-Met水平，IC50为10 nM，不影响全部 c-Met,导致下游信号分子包括 ERK, Akt, p70S6K 和 S6受抑制，这种作用存在剂量依赖性。纳摩尔级BMS-777607(~1 μM)处理24小时,有效抑制KHT细胞分散，活动，和入侵，这与MET基因抑制相关,适当影响细胞增殖和集落形成。[3]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC-3 MlfDSpVv[3Srb36gZZN{[Xl? Mn;CNE4yKM7:TR?= Mm\kSG1UVw>? NE\0cFFmgGirYnn0d{BqdmirYnn0c5J6KGWoZnXjeEBwdiCKR1[tbY5lfWOnZDDj[YxtKHOlYYT0[ZJqdmd? NHfSdpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1Oyd-MkC1NVU6PDN:L3G+
DU145 MVrGeY5kfGmxbjDhd5NigQ>? MUSwMlEh|ryP NWrTVVJrTE2VTx?= MX\lfIhq[mm2czDpcohq[mm2b4L5JIVn\mWldDDvckBJT0ZvaX7keYNm\CClZXzsJJNk[XS2ZYLpcoc> NIT6cGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1Oyd-MkC1NVU6PDN:L3G+
PC-3 MWfGeY5kfGmxbjDhd5NigQ>? MojnNE4xOSEQvF2= NWrnbpVrTE2VTx?= MYLzeZBxemW|c3XzJGhITi2rbnT1Z4VlKGOnbHygcYloemG2aX;u NELVXoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1Oyd-MkC1NVU6PDN:L3G+
DU145 Moj4SpVv[3Srb36gZZN{[Xl? NV3XO|ZPOC5yMTFOwG0> MWrEUXNQ MmTKd5VxeHKnc4Pld{BJT0ZvaX7keYNm\CClZXzsJI1q\3KjdHnvci=> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0N{c,OjB3MUW5OFM9N2F-
PC-3 NHvtfXlHfW6ldHnvckBie3OjeR?= NFO1foExNjFizszN MkHQSG1UVw>? M2jzRYlueGGrcoOgTGdHNW2nZHnheIVlKGOnbHygbY53[XOrb36= MoTsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3MUW5OFMoRjJyNUG1PVQ{RC:jPh?=
DU145 MWfGeY5kfGmxbjDhd5NigQ>? M2LRfFAvOSEQvF2= M17yPWROW09? MXzpcZBicXK|IFjHSk1u\WSrYYTl[EBk\WyuIHnueoF{cW:w MmDFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3MUW5OFMoRjJyNUG1PVQ{RC:jPh?=
PC-3 NHG5UHZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MW\+NVAh|ryP NFfYZ29FVVOR MVPy[YR2[2W|IHPlcIwheHKxbHnm[ZJifGmxbh?= NHyzblM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1Oyd-MkC1NVU6PDN:L3G+
KHT MkPCT4lv[XOnIHHzd4F6 MV\EUXNQ MkTMZoxw[2u|IITo[UBkNU2ndDDzbYdv[WyrbnegdIF1cHejeTD3bZRpKEmFNUCgc4YhOTBibl2= NVjj[nE1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyPFY2OjNpPkKyNlg3PTJ|PD;hQi=>
KHT MXrGeY5kfGmxbjDhd5NigQ>? Mo\sglEh|ryP NHm3[XFFVVOR MWDwdoV3\W62czDzdI9vfGGwZX;1d{BMUFRiY3XscEB{[2G2dHXybY5oKHerdHigTWM2OCCxZjCwMlEuOC53IN88US=> NHrCXm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK4OlUzOyd-MkKyPFY2OjN:L3G+
KHT M3PPWmZ2dmO2aX;uJIF{e2G7 M1u4RZ4xNjVizszN MoC2SG1UVw>? MnvMbY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ6NkWyN{c,OjJ{OE[1NlM9N2F-
KHT MXTGeY5kfGmxbjDhd5NigQ>? MVr+NE42KM7:TR?= MkDnSG1UVw>? NUT6ZYN{cW6qaXLpeJMh[2WubDDpcpZie2mxbh?= MkflQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
KHT M4jyV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NI\lZ4t,OTBizszN MWDEUXNQ Ml3WbY5pcWKrdIOgT2hVKGOnbHygdJJwdGmoZYLheIlwdg>? Ml:1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
T-47D M3[0Umdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXfGdIRthjVizszN MkDLSG1UVw>? Ml\NbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NX7PT2h2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0Olg2OjlpPkKzOFY5PTJ7PD;hQi=>
ZR-75-1 NE\STpRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NI\RVI9,PSEQvF2= NInrc5ZFVVOR NEfn[FdqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NFywcow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S2PFUzQSd-MkO0Olg2Ojl:L3G+
T-47D MkjSSpVv[3Srb36gZZN{[Xl? NYD1OINXOTBizszN NUXoUIJJTE2VTx?= M{\TSmlv\HWlZYOgdI9tgXCub3nkfUBjgSB6NjCl MoHkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2Nki1NlkoRjJ|NE[4OVI6RC:jPh?=
ZR-75-1 NHj3[2dHfW6ldHnvckBie3OjeR?= MnzBNVAh|ryP NGD1XmxFVVOR MkG3TY5lfWOnczDwc4x6eGyxaXT5JIJ6KDh6JR?= NXKzNYRQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0Olg2OjlpPkKzOFY5PTJ7PD;hQi=>
T-47D NHr3[G1HfW6ldHnvckBie3OjeR?= M3j0ZlExKM7:TR?= MUPEUXNQ MlvPbY5pcWKrdIOgRXVTUy2EIH\1coN1cW:wIHHu[EBqdmS3Y3XzJIl1eyCycn;0[YlvKGSnZ4Lh[IF1cW:w NWrOS|huRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0Olg2OjlpPkKzOFY5PTJ7PD;hQi=>
CHRF MmjuSpVv[3Srb36gZZN{[Xl? NXLiWoN3OTBizszN NVv5UXJ5TE2VTx?= M2q3SolvcGmkaYTzJINmdGxiZHn2bZNqd25? NV\oPIpRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzNFQ6ODBpPkK1N|A1QTByPD;hQi=>
HPDE MVfGeY5kfGmxbjDhd5NigQ>? MkjLNVAh|ryP M3;yW2ROW09? Ml7wZoxw[2u|IHPvcpN1cXS3dHn2[UBi[3SrdnH0bY9vKGGwZDDk[YNz\WG|ZXSgRWtVKHOrZ37hcIlv\w>? MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR5N{OxOEc,OjZ2N{ezNVQ9N2F-
U118MG M3nRO2tqdmG|ZTDhd5NigQ>? NHzRcIt,OyEQvF2= NVPHeXF7TE2VTx?= M{PUUoJtd2OtczDBXGwheGixc4Doc5J6dGG2aX;u NIPGcZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PFUzPCd-Mk[4OFg2OjR:L3G+
SF126 MkT4T4lv[XOnIHHzd4F6 MkThglMh|ryP NGH5OZRFVVOR M3;oZ4Jtd2OtczDBXGwheGixc4Doc5J6dGG2aX;u NVPxdFVTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFg2OjRpPkK2PFQ5PTJ2PD;hQi=>
U118MG NXfUOGo6S3m2b4jpZ4l1gSCjc4PhfS=> MnO2NVIvPSEQvF2= MYLEUXNQ M{XPRYRm[3KnYYPld{BodGmxbXGgZ4VtdCC4aXHibYxqfHl? M2fSWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
SF126 M4XEWGN6fG:6aXPpeJkh[XO|YYm= MlHlNVIvPSEQvF2= MYnEUXNQ NFPBXHpl\WO{ZXHz[ZMh\2yrb33hJINmdGxidnnhZoltcXS7 NXPtbJJ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFg2OjRpPkK2PFQ5PTJ2PD;hQi=>
U118MG M{HUUmFxd3C2b4Ppd{Bie3OjeR?= MofzNVIvPSEQvF2= MXfEUXNQ NGDhS5VqdmS3Y3XzJIdtcW:vYTDj[YxtKGGyb4D0c5Nqew>? M2jLZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
SF126 NU[5NJpUSXCxcITvd4l{KGG|c3H5 NGK4bHkyOi53IN88US=> NFyzVGxFVVOR MYPpcoR2[2W|IHfsbY9u[SClZXzsJIFxd3C2b4Ppdy=> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh2OEWyOEc,OjZ6NEi1NlQ9N2F-
U118MG MlXWSpVv[3Srb36gZZN{[Xl? NUXNW4RqOTJwNTFOwG0> MV\EUXNQ NIrVSlVjdG:la4Og[4xqd22jIHPlcIwhdWmpcnH0bY9vKGGwZDDpcpZie2m4ZTDndo94fGhicHH0eIVzdg>? MnnLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NEi1NlQoRjJ4OES4OVI1RC:jPh?=
SF126 NH36endHfW6ldHnvckBie3OjeR?= M1TwPFEzNjVizszN M17tPGROW09? Mkj5Zoxw[2u|IHfsbY9u[SClZXzsJI1q\3KjdHnvckBidmRiaX72ZZNqfmViZ4Lve5RpKHCjdITldo4> NYHoTlFjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFg2OjRpPkK2PFQ5PTJ2PD;hQi=>
GTL16 NWX2UYM4TnWwY4Tpc44h[XO|YYm= MkTjN|AhdWmwcx?= M3[zVWlvcGmkaYTpc44hd2ZiTXX0JJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDHWGwyPiClZXzsd{Bi\nSncjCzNEBucW6|LDDJR|UxKD1iMD6wNkDPxE1w MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ4MEexNUc,OTl{NkC3NVE9N2F-
GTL16 NVf5OW1GSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NHXWTFk4OiCqcoO= NH:wNoxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JG1mfC2mZYDlcoRmdnRiaIXtZY4hT1SOMU[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMTFOwG0v MmHiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{NkC3NVEoRjF7Mk[wO|EyRC:jPh?=
NCI-H1993 MV7BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? Ml7IO|IhcHK| M1P4WmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgUYV1NWSncHXu[IVvfCCqdX3hckBPS0lvSEG5PVMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OCB;IECuNVUh|ryPLh?= M3TNUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7Mk[wO|EyLz5zOUK2NFcyOTxxYU6=
U87 MmjNRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NXPpXJJzPzJiaILz M{[yUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgUYV1NWS{aY\lckBpfW2jbjDVPFch[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OCB;IECuNVYh|ryPLh?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ4MEexNUc,OTl{NkC3NVE9N2F-
BAF3 NFjEW2lEgXSxdH;4bYNqfHliYYPzZZk> NHfyeYI4OiCqcoO= MVXDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJIV5eHKnc4PpcochXFCULV3leEBie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOsJGlEPTBiPTCwMlE5QDRizszNMi=> NIDqR209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe5Nlc4PCd-MkS3PVI4PzR:L3G+
DU145 NUPl[plKSW62aXnueoF{cX[nIHHzd4F6 MWCxJIhz M3zXZ2FvfGmrbo\hd4l3\SCjY4Tpeol1gSCrbjDoeY1idiCGVUG0OUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFjHSk1qdmS3Y3XkJINmdGxibX;0bYxqfHlicILlbY5kfWKjdHXkJIZweiBzIHjyJIJm\m:{ZTDIS2YhfHKnYYTt[Y51KG2nYYP1doVlKGGodHXyJFI1KGi{czDifUBk\WyuIIPjZZR1\XKrbnegZZN{[XluIFnDOVAhRSByLkKg{txONg>? MmntQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC4N|AoRjJ2OUCwPFMxRC:jPh?=
MKN45 NWnZbI5ZS3m2b4TvfIlkcXS7IHHzd4F6 MoG2O|IhcHK| MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNT241PSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOsJGlEPTBiPTCwMlI5PThizszNMi=> M{TOTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{myO|c1Lz5{NEe5Nlc4PDxxYU6=
NCI-H1993 M{mwbWN6fG:2b4jpZ4l1gSCjc4PhfS=> NGTjT3E1QCCqcoO= NVzxOVg3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkOLLVixPVk{KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxMlExQCEQvF2u M4P0WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwPFMxLz5{NEmwNFg{ODxxYU6=
GTL16 NG\1RmVHfW6ldHnvckBie3OjeR?= NHmwcVI3NjJ3IH3nM4to NUDxepZtS22jeDDpckBpfW2jbjDHWGwyPiClZXzsd{B5\W6xZ4Lh[pRm\CCjdHj5cYlkKG2xdYPlJIF1KDZwMkWgcYcwc2duIIDvMEBEdWG6IE2gOE42KM7:TT6= NGKzZY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK2NFcyOSd-MUmyOlA4OTF:L3G+
GTL16 NX3JXIZbTnWwY4Tpc44h[XO|YYm= M{HDRVUxKG2pL3vn M13MNWNu[XhiaX6gbJVu[W5iR2TMNVYh[2WubIOgfIVvd2e{YX\0[YQh[XSqeX3pZ{Bud3W|ZTDheEA2OCCvZz;r[{wheG9uIFPtZZghRSB2Mz63JO69VS5? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ4MEexNUc,OTl{NkC3NVE9N2F-
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A673 NGPid5ByUFSVIHHzd4F6 M{fzOZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| MlzpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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LAN-5 MXnxTHRUKGG|c3H5 MmLadWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| NUXJflFCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 MnPhdWhVWyCjc4PhfS=> Mm\udWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= M13mR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673 M2XGRZFJXFNiYYPzZZk> NEnMZ2FyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBCPjd|IHPlcIx{MQ>? NE\ue|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC MVHxTHRUKGG|c3H5 NWXZeI8xeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= NULYWHRPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 NEDLZYVyUFSVIHHzd4F6 M4m2TJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNLNUeETUKgZ4VtdHN? NHHWUpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
TC32 NFrocnNyUFSVIHHzd4F6 MWrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz M4r3dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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MGHU3 MUDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MkDvO|IhcHK| MlfORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPR1jVN{Bk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeR?= NEDvSI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEOwPVY4OSd-M{CzNFk3PzF:L3G+
RT112 MWjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NVr1R2xzPzJiaILz NVvlXGJuSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSWFEyOiClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfS=> NGGxfJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEOwPVY4OSd-M{CzNFk3PzF:L3G+

... 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
体内研究 BMS 777607按6.25-50 mg/kg剂量口服处理给药携带GTL-16人类移植瘤的无胸腺小鼠，明显降低肿瘤体积，且没有毒性。[1] BMS 777607按25 mg/kg剂量每天处理6-8周大的注射啮齿类纤维肉瘤KHT细胞的雌性C3H/HeJ小鼠，降低 KHT肺肿瘤结节数量,提高形态出血, 且明显修复损害转移表型，与对照组相比，没有明显毒性。BMS 777607按 10 mg/kg 低剂量处理，也适度但不显著抑制肺结节形成。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验：[4]
- 合并

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.
细胞实验：[3]
- 合并
  • Cell lines: 啮齿类纤维肉瘤KHT细胞
  • Concentrations: 溶于DMSO，作为储存液(10 mM), 终浓度为10 μM 左右
  • Incubation Time: 2, 24和96小时
  • Method: 用连续稀释的BMS 777607 处理KHT细胞96小时，然后进行MTT实验和台酚蓝排除，分别测定细胞增殖和细胞死亡。KHT细胞集落和BMS 777607温育24小时，然后用结晶紫(0.1%)染色，然后显影，测定细胞分散情况。使用无菌的1 ml吸管端在融合的KHT单层细胞上划2 mm 痕，随后用BMS-777607处理24小时，在4块随机区域中计数迁移到剥蚀地细胞数，用于测定细胞迁移情况。为了测定细胞入侵，用Matrigel预包被的转移嵌入板(8 μm 孔膜)，和无血清培养基在有或无BMS 777607存在时，在37oC下温育2小时,使Matrigel再水化。悬浮在无血清培养基上的细胞装到小室顶端，悬浮在含10% FBS的完全培养基上的细胞装到小室底端，作为化学引诱物。温育24小时，移除 Matrigel，用结晶紫染色。显影并计数在滤液下面的入侵细胞。
    (Only for Reference)
动物实验：[3]
- 合并
  • Animal Models: 携带啮齿类纤维肉瘤KHT细胞的雌性C3H/HeJ小鼠
  • Dosages: 10-25 mg/kg
  • Administration: 饲喂处理，每天一次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 47 mg/mL (91.63 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)：
4% DMSO+45% PEG 300+5% Tween 80+ddH2O
 5mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 512.89
化学式

C25H19ClF2N4O4
CAS号 1025720-94-8
储存条件 粉状
溶于溶剂
别名 BMS 817378

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1：

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

  • 回答：

    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.

免费分装抑制剂
Selleck产品目录册

c-Met Signaling Pathway Map

c-Met Inhibitors with Unique Features

  • 选择性强的c-Met抑制剂

    PF-04217903 : C-Met-selective, IC50=4.8 nM.

  • 活性最高的c-Met抑制剂

    INCB28060 : C-Met, IC50=0.13 nM.

  • FDA批准的c-Met抑制剂

    Crizotinib (PF-02341066) : Approved by FDA for non-small cell lung carcinoma (NSCLC).

  • 最新的c-Met抑制剂

    EMD 1214063 New : Potent and selective c-Met inhibitor with IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer.

相关c-Met产品

  • NPS-1034 New

    NPS-1034是一种双Met (c-Met)/Axl抑制剂，IC50分别为48 nM和10.3 nM。

  • Erlotinib (OSI-774) New

    Erlotinib (OSI-774, CP358774, NSC 718781, Tarceva)是一种EGFR抑制剂，IC50 为 2 nM，对EGFR的敏感性比对人c-Src 或 v-Ab高1000多倍。Erlotinib可诱导自噬。

  • Bemcentinib (R428) New

    Bemcentinib (R428, BGB324)是一种Axl抑制剂，IC50为14 nM，作用于Axl比作用于Abl选择性高100倍以上。作用于Axl选择性也比作用于Mer和Tyro3(高50到100倍)及InsR， EGFR， HER2，和PDGFRβ(高100倍以上)高。

  • Crizotinib (PF-02341066)

    Crizotinib (PF-02341066) 克唑替尼是一种有效的c-Met和ALK抑制剂，在细胞试验中IC50分别为11 nM 和 24 nM。它同时也是有效的ROS1抑制剂，其Ki值小于0.025 nM。Crizotinib可在多种肺癌细胞系中通过抑制STAT3通路来诱导自噬。

  • Foretinib (GSK1363089)

    Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) 是一种ATP竞争性的HGFR和VEGFR抑制剂，对Met (c-Met)和KDR作用最强，在无细胞试验中IC50分别为0.4 nM和0.9 nM。对Ron， Flt-1/3/4， Kit (c-Kit)， PDGFRα/β和Tie-2作用效果稍弱，对FGFR1和EGFR几乎没有抑制活性。Phase 2。

  • Capmatinib (INCB28060)

    Capmatinib (INCB28060, INC280, NVP-INC280)是一种新型的，ATP竞争性c-MET抑制剂，无细胞试验中IC50为0.13 nM，对RONβ，EGFR和HER-3无活性。Capmatinib (INCB28060)可抑制 Wnt/β-catenin 和 EMT 信号通路并诱导c-MET扩增阳性的弥漫性胃癌中的凋亡。Phase 1。

    Features:INCB28060 对c-MET RTK家族的RONβ以及EGFR RTK家族的EGFR和HER-3不具有活性。

  • Tivantinib (ARQ 197)

    Tivantinib (ARQ 197) 是第一个非ATP竞争性的c-Met抑制剂，在无细胞试验中Ki为0.355 μM，对Ron几乎没有作用活性，对EGFR，InsR，PDGFRα和FGFR1/4没有抑制作用。Tivantinib (ARQ 197) 可诱导G2/M期细胞阻滞和凋亡。Phase 3。

    Features:ARQ-197是第一个应用到晚期人类临床试验的c-Met选择性抑制剂。

  • PHA-665752

    PHA-665752是一种有效的，选择性的，ATP竞争性c-Met抑制剂，在无细胞试验中IC50为9 nM，对c-Met的选择性比对 RTKs和 STKs高50倍以上。

  • PF-04217903

    PF-04217903是一种选择性的，ATP竞争性c-Met抑制剂，在A549细胞中IC50为4.8 nM，对致癌基因突变型敏感(对Y1230C突变型没有活性)。Phase 1。

  • SU11274

    SU11274 (PKI-SU11274) 是一种选择性Met (c-Met)抑制剂，在无细胞试验中IC50为10 nM，对PGDFRβ，EGFR和Tie2没有作用。SU11274 可诱导自噬、凋亡和细胞周期阻滞。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID