BMS-777607

目录号:S1561 别名: BMS 817378

仅限科研使用

BMS-777607 (BMS 817378)是一种Met相关的抑制剂,作用于c-MetAxlRonTyro3,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。

BMS-777607 Chemical Structure

CAS: 1025720-94-8

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 5498.71 现货
大包装 有超大折扣
大剂量询单有大折扣!

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如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的BMS-777607发表文献49篇:

产品安全说明书

c-Met抑制剂选择性比较

相关c-Met产品

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-MetAxlRonTyro3,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)
点击更多
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 NU\mUIFHTnWwY4Tpc44h[XO|YYm= M4HQRlAvOSEQvF2= M3XMRWROW09? MnL6[ZhpcWKrdIOgbY5pcWKrdH;yfUBm\m[nY4Sgc44hUEeILXnu[JVk\WRiY3XscEB{[2G2dHXybY5o NGrQ[Ws9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1Oyd-MkC1NVU6PDN:L3G+
DU145 M1PXd2Z2dmO2aX;uJIF{e2G7 MWCwMlEh|ryP MVHEUXNQ NHTFe5hmgGirYnn0d{BqdmirYnn0c5J6KGWoZnXjeEBwdiCKR1[tbY5lfWOnZDDj[YxtKHOlYYT0[ZJqdmd? NVrWVYNKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDNpPkKwOVE2QTR|PD;hQi=>
PC-3 MV7GeY5kfGmxbjDhd5NigQ>? Mk\yNE4xOSEQvF2= M1TsTmROW09? NVjpXnNye3WycILld5NmeyCKR1[tbY5lfWOnZDDj[YxtKG2rZ4LheIlwdg>? MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0N{c,OjB3MUW5OFM9N2F-
DU145 NIS5WGdHfW6ldHnvckBie3OjeR?= NV;LSoY1OC5yMTFOwG0> NEW2ZYdFVVOR NELSSYl{fXCycnXzd4V{KEiJRj3pcoR2[2WmIHPlcIwhdWmpcnH0bY9v NX60SoNlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDNpPkKwOVE2QTR|PD;hQi=>
PC-3 NGjEbHpHfW6ldHnvckBie3OjeR?= MVWwMlEh|ryP M4nNbGROW09? NWL5Zpo6cW2yYXnyd{BJT0ZvbXXkbYF1\WRiY3XscEBqdn[jc3nvci=> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0N{c,OjB3MUW5OFM9N2F-
DU145 NFK1TXJHfW6ldHnvckBie3OjeR?= NXPkZVV1OC5zIN88US=> MWHEUXNQ NHHrRZZqdXCjaYLzJGhITi2vZXTpZZRm\CClZXzsJIlvfmG|aX;u NWXN[Is{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDNpPkKwOVE2QTR|PD;hQi=>
PC-3 NV;TPGdwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1y5[54yOCEQvF2= NX\neZg{TE2VTx?= M4\3eZJm\HWlZYOgZ4VtdCCycn;sbYZmemG2aX;u MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0N{c,OjB3MUW5OFM9N2F-
KHT MlL5T4lv[XOnIHHzd4F6 Mn\ESG1UVw>? MmflZoxw[2u|IITo[UBkNU2ndDDzbYdv[WyrbnegdIF1cHejeTD3bZRpKEmFNUCgc4YhOTBibl2= NGrPWGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK4OlUzOyd-MkKyPFY2OjN:L3G+
KHT MlL4SpVv[3Srb36gZZN{[Xl? M2jYcZ4yKM7:TR?= MlHWSG1UVw>? NV:ycXRpeHKndnXueJMhe3CxboThcoVwfXNiS1jUJINmdGxic3PheJRmemmwZzD3bZRpKEmFNUCgc4YhOC5zLUCuOUDPxE1? NYPE[IV[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyPFY2OjNpPkKyNlg3PTJ|PD;hQi=>
KHT MoC3SpVv[3Srb36gZZN{[Xl? M3fzcZ4xNjVizszN NYLOZ5NFTE2VTx?= MX7pcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? MnHUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
KHT NEGxWGVHfW6ldHnvckBie3OjeR?= M3P4Sp4xNjVizszN MUXEUXNQ NW\vNIxkcW6qaXLpeJMh[2WubDDpcpZie2mxbh?= MnewQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
KHT Mn3SS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2nI[p4yOCEQvF2= NFfvTmpFVVOR MoH0bY5pcWKrdIOgT2hVKGOnbHygdJJwdGmoZYLheIlwdg>? M4G3VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Mki2OVI{Lz5{MkK4OlUzOzxxYU6=
T-47D NF7WbYFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1e3Op42KM7:TR?= NX3HepQxTE2VTx?= M2DseIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> Ml;VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2Nki1NlkoRjJ|NE[4OVI6RC:jPh?=
ZR-75-1 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkS3glUh|ryP MVXEUXNQ M1\qVYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M3fvcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NE[4OVI6Lz5{M{S2PFUzQTxxYU6=
T-47D MmXOSpVv[3Srb36gZZN{[Xl? M3HwblExKM7:TR?= M2G2bGROW09? MWHJcoR2[2W|IIDvcJlxdG:rZImgZpkhQDZiJR?= NYfmNlZnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0Olg2OjlpPkKzOFY5PTJ7PD;hQi=>
ZR-75-1 NIfWSldHfW6ldHnvckBie3OjeR?= MV2xNEDPxE1? NXn3Z4dbTE2VTx?= NVLRdWhLUW6mdXPld{Bxd2y7cHzvbYR6KGK7IEi4KS=> NVv2U3RbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0Olg2OjlpPkKzOFY5PTJ7PD;hQi=>
T-47D NWDmSY1yTnWwY4Tpc44h[XO|YYm= MYGxNEDPxE1? MnzJSG1UVw>? Mnr5bY5pcWKrdIOgRXVTUy2EIH\1coN1cW:wIHHu[EBqdmS3Y3XzJIl1eyCycn;0[YlvKGSnZ4Lh[IF1cW:w NF65TpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S2PFUzQSd-MkO0Olg2Ojl:L3G+
CHRF MX7GeY5kfGmxbjDhd5NigQ>? NWGxcYU2OTBizszN MoeySG1UVw>? M1zBUolvcGmkaYTzJINmdGxiZHn2bZNqd25? MonlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MES5NFAoRjJ3M{C0PVAxRC:jPh?=
HPDE NXLRRZVRTnWwY4Tpc44h[XO|YYm= M{\De|ExKM7:TR?= MYLEUXNQ NWTGZmNJ[myxY3vzJINwdnO2aYT1eIl3\SCjY4TpeoF1cW:wIHHu[EBl\WO{ZXHz[YQhSUuWIIPp[45idGmwZx?= M2m1cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NEe3N|E1Lz5{NkS3O|MyPDxxYU6=
U118MG Ml[3T4lv[XOnIHHzd4F6 NGnQ[3N,OyEQvF2= MULEUXNQ Mk[4Zoxw[2u|IFHYUEBxcG:|cHjvdplt[XSrb36= NVXneGlTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFg2OjRpPkK2PFQ5PTJ2PD;hQi=>
SF126 NF3UNWhMcW6jc3WgZZN{[Xl? NVrKZ49xhjNizszN NFy4ZmZFVVOR M2PyXYJtd2OtczDBXGwheGixc4Doc5J6dGG2aX;u NHT0bFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PFUzPCd-Mk[4OFg2OjR:L3G+
U118MG M4W4bmN6fG:6aXPpeJkh[XO|YYm= MoHCNVIvPSEQvF2= Mnr0SG1UVw>? MXrk[YNz\WG|ZYOg[4xqd22jIHPlcIwhfmmjYnnsbZR6 NFX5W489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PFUzPCd-Mk[4OFg2OjR:L3G+
SF126 NHLkWmNEgXSxeHnjbZR6KGG|c3H5 NYfMXZh5OTJwNTFOwG0> MXLEUXNQ NGTzTXJl\WO{ZXHz[ZMh\2yrb33hJINmdGxidnnhZoltcXS7 NX21S4pmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFg2OjRpPkK2PFQ5PTJ2PD;hQi=>
U118MG NF;sSolCeG:ydH;zbZMh[XO|YYm= MmrQNVIvPSEQvF2= NVHTW4l5TE2VTx?= M4DCSYlv\HWlZYOg[4xqd22jIHPlcIwh[XCxcITvd4l{ M4rSdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
SF126 M2\PdWFxd3C2b4Ppd{Bie3OjeR?= MnzFNVIvPSEQvF2= M4LnTGROW09? MVPpcoR2[2W|IHfsbY9u[SClZXzsJIFxd3C2b4Ppdy=> MmTxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NEi1NlQoRjJ4OES4OVI1RC:jPh?=
U118MG M{jkS2Z2dmO2aX;uJIF{e2G7 MkLaNVIvPSEQvF2= NV7RXJR{TE2VTx?= MlH3Zoxw[2u|IHfsbY9u[SClZXzsJI1q\3KjdHnvckBidmRiaX72ZZNqfmViZ4Lve5RpKHCjdITldo4> M3jWVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
SF126 MmK2SpVv[3Srb36gZZN{[Xl? M1HhfVEzNjVizszN MmnhSG1UVw>? NHztWlBjdG:la4Og[4xqd22jIHPlcIwhdWmpcnH0bY9vKGGwZDDpcpZie2m4ZTDndo94fGhicHH0eIVzdg>? M3f0[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
GTL16 NGKzWWxHfW6ldHnvckBie3OjeR?= NFS4cnQ{OCCvaX7z MYXJcohq[mm2aX;uJI9nKE2ndDDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iR2TMNVYh[2WubIOgZYZ1\XJiM{CgcYlveyxiSVO1NEA:KDBwMEKg{txONg>? NWS3UnhNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyOlA4OTFpPkG5NlYxPzFzPD;hQi=>
GTL16 MWHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MUK3NkBpenN? M2\wWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgUYV1NWSncHXu[IVvfCCqdX3hckBIXExzNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCLQ{WwJF0hOC5zIN88UU4> MlvtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{NkC3NVEoRjF7Mk[wO|EyRC:jPh?=
NCI-H1993 MmHlRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M3vVOFczKGi{cx?= MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IF3leE1l\XCnbnTlcpQhcHWvYX6gUmNKNUhzOUmzJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkG1JO69VS5? NF;nTJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK2NFcyOSd-MUmyOlA4OTF:L3G+
U87 M4TITmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NFvJbIM4OiCqcoO= NV\lU4NmSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBO\XRvZILpeoVvKGi3bXHuJHU5PyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRUKGG|c3H5MEBKSzVyIE2gNE4yPiEQvF2u M1i4OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7Mk[wO|EyLz5zOUK2NFcyOTxxYU6=
BAF3 MmHRR5l1d3SxeHnjbZR6KGG|c3H5 NFLmTG44OiCqcoO= MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJIV5eHKnc4PpcochXFCULV3leEBie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOsJGlEPTBiPTCwMlE5QDRizszNMi=> MmrCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5OUK3O|QoRjJ2N{myO|c1RC:jPh?=
DU145 Moq5RY51cWmwdnHzbZZmKGG|c3H5 M2jkNFEhcHJ? Ml\DRY51cWmwdnHzbZZmKGGldHn2bZR6KGmwIHj1cYFvKESXMUS1JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiSFfGMYlv\HWlZXSgZ4VtdCCvb4TpcIl1gSCycnXpcoN2[mG2ZXSg[o9zKDFiaIKgZoVnd3KnIFjHSkB1emWjdH3lcpQhdWWjc4Xy[YQh[W[2ZYKgNlQhcHK|IHL5JINmdGxic3PheJRmemmwZzDhd5NigSxiSVO1NEA:KDBwMjFOwG0v NWLjcm5NRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA5OzBpPkK0PVAxQDNyPD;hQi=>
MKN45 M4\RSWN6fG:2b4jpZ4l1gSCjc4PhfS=> MofwO|IhcHK| NVrZW|VJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUuQNEWgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{NCCLQ{WwJF0hOC5{OEW4JO69VS5? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd7Mke3OEc,OjR5OUK3O|Q9N2F-
NCI-H1993 NV3J[JoxS3m2b4TvfIlkcXS7IHHzd4F6 M3;JSlQ5KGi{cx?= NGrmPHJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0lvSEG5PVMh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEGuNVA5KM7:TT6= NYXIS49GRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA5OzBpPkK0PVAxQDNyPD;hQi=>
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OHS-50 NHjZV|ByUFSVIHHzd4F6 NHfYRoFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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MG 63 (6-TG R) MkHEdWhVWyCjc4PhfS=> NIfCXGxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBOTyB4MzCoOk1VTyCUKTDj[Yxtew>? Ml;mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MGHU3 M1voWWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NY[2XVk3PzJiaILz M1TGUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVfIWVMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYm= NG[3PHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEOwPVY4OSd-M{CzNFk3PzF:L3G+
RT112 MorURY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M{fn[FczKGi{cx?= M1n5UGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmSxNVIh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYm= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODNyOU[3NUc,OzB|MEm2O|E9N2F-
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
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]
  • 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]
  • 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。
动物实验:[3]
  • 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

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

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

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

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操作手册

如果有其他问题,请给我们留言。

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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.