BMS-754807

目录号:S1124

仅限科研使用

BMS-754807是一种有效的IGF-1R/InsR可逆性抑制剂,在无细胞试验中IC50为1.8 nM/1.7 nM,对Met (c-Met),Aurora A/B,TrkA/B和Ron作用稍弱,对Flt3, Lck,MK2,PKA,PKC等几乎没有抑制活性。Phase 2。

BMS-754807 Chemical Structure

CAS: 1001350-96-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2211.3 现货
RMB 1480.09 现货
RMB 6299.66 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
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-754807发表文献41篇:

产品安全说明书

IGF-1R抑制剂选择性比较

相关IGF-1R产品

生物活性

产品描述 BMS-754807是一种有效的IGF-1R/InsR可逆性抑制剂,在无细胞试验中IC50为1.8 nM/1.7 nM,对Met (c-Met),Aurora A/B,TrkA/B和Ron作用稍弱,对Flt3, Lck,MK2,PKA,PKC等几乎没有抑制活性。Phase 2。
特性 胰岛素样生长因子-1R/IR家族激酶的多重抑制剂
靶点
Insulin Receptor [1]
(Cell-free assay)
IGF-1R [1]
(Cell-free assay)
TrkB [1]
(Cell-free assay)
Met [1]
(Cell-free assay)
TrkA [1]
(Cell-free assay)
点击更多
1.7 nM 1.8 nM 4.1 nM 5.6 nM 7.4 nM
体外研究

BMS-754807 有效抑制人类多种不同组织来源的肿瘤细胞系的生长,包括间充质(尤文氏肉瘤,横纹肌肉瘤,神经母细胞瘤,和脂肪肉瘤),上皮(乳腺,肺,胰腺,结肠,和胃),和造血(多发性骨髓瘤和白血病)组织,IC50值从5 nM 到 365 nM。BMS-754807 抑制 IGF-1R-Sal 细胞和 RH41细胞增殖,IC50分别为7 nM 和5 nM。BMS-754807作用于IGF-1R-Sal, Rh41 和 Geo细胞,抑制IGF-1R磷酸化,IC50分别为13 nM, 6 nM 和 21 nM。BMS-754807作用于 IGF-1R-Sal, Rh41 和Geo细胞,抑制Akt磷酸化,IC50 分别为22 nM, 13 nM 和 16 nM。BMS-754807诱导Rh41细胞凋亡。[1] BMS-754807作用于IGF-Sal 细胞系,抑制IGF-1R (IC50 = 13nM) 和下游靶点Akt (IC50 = 22nM) 和MAPK(IC50 = 13nM) 的磷酸化。[2] 在儿科临床前期试验计划(PPTP)中,BMS-754807作用于23种细胞系,平均EC50值为0.62 µM。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
IGF-Sal M365eWtqdmG|ZTDhd5NigQ>? MlHMbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCLR1[tNXIhMEmFNUCgQUAyO26PKTDhcoQhfGinIHTve45{fHKnYX2geIFz\2W2czDBb5QhMEmFNUCgQUAzOm6PKTDhcoQhVUGSSzCoTWM2OCB;IEGzcm0q MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd5OECyOEc,OTl5N{iwNlQ9N2F-
IGF-Sal NH;kPZlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVrRVm9xUUN3ME23JI5O NGXYV289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe3PFAzPCd-MUm3O|gxOjR:L3G+
CCRF-CEM (ALL) NYXwPY9NT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnfOglUh|ryP NH;ZVldFVVOR NVS4eYIzUUN3ME2xMlI{QSEQvF2= NGnncGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
PC3 NXLYPGFsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWHIc|d3hjVizszN MUTEUXNQ M4TwbGlEPTB;MD65OlUh|ryP M36yUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
JD NI\lSIpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MW\+OUDPxE1? NUPuR21kTE2VTx?= M2j3WWlEPTB;MD6zPVEh|ryP M{TGc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
DU145 M2jMcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVz6OmtuhjVizszN MX;EUXNQ M1;tOmlEPTB;MT60OlUh|ryP NWTRZVc2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
KAG Mnz0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWf+OUDPxE1? MmjnSG1UVw>? M2THe2lEPTB;MT62OlUh|ryP NV\VUFdtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
K-562 (CML) M37PdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFn4[lJ,PSEQvF2= NYf6ZnpLTE2VTx?= NXLzenZuUUN3ME2yMlMxOiEQvF2= MkDnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
B6-P210 (Murine ALL) MmTyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mn;kglUh|ryP M4XnVmROW09? NUTK[4Z4UUN3ME2xMlI6OyEQvF2= NIfNXXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
LN CAP-FGC NVnvSJZRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXfWOllzhjVizszN M13ufGROW09? Ml7uTWM2OD1zLkSzOEDPxE1? NVrnV5Q3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
VW NVLCdVJIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlziglUh|ryP M376dGROW09? MYfJR|UxRTBwMEG5JO69VQ>? NXLKdnZURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
MV411 (B Myelomonocytic) M1PXcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX7+OUDPxE1? NVvXW45oTE2VTx?= MV7JR|UxRTBwM{Og{txO Ml:5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
MDA-PCa-2b MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYf+OUDPxE1? M4HmcWROW09? NGrNenNKSzVyPUCuNFk5KM7:TR?= Ml;xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
LG NWP2S4pXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVj+OUDPxE1? MoGzSG1UVw>? M3fLR2lEPTB;MD6wN|gh|ryP NF[zU|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
RS411 (B cell precursor-ALL) MnvCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFTNXlF,PSEQvF2= MVvEUXNQ MW\JR|UxRTBwMUCyJO69VQ>? NGHOTVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
22-r-1 MlTGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXTPPVd7hjVizszN MYnEUXNQ MnLHTWM2OD1yLkG3OUDPxE1? NX;KOZg5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
5838 NHnTOlBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4PIOJ42KM7:TR?= M37ufmROW09? NY\j[GxVUUN3ME2wMlA{PCEQvF2= M3L1SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
P388 (Murine) MlHvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXn+OUDPxE1? NULs[WJXTE2VTx?= MnLNTWM2OD12LkK3JO69VQ>? M1:zdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
A2780/S Mm[wS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUL+OUDPxE1? Mo\GSG1UVw>? NWe1OYU2UUN3ME2wMlEzOiEQvF2= NGPseWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
RDES NYrZNphST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV;+OUDPxE1? M2D3XGROW09? MUTJR|UxRTBwMEGyJO69VQ>? NHPUR|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
B6-T315I (Murine B-ALL) NVfHTG5IT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUWwb4tXhjVizszN Mn21SG1UVw>? M{njPGlEPTB;Mj64N{DPxE1? NUi4OYVpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
TOV 112D NH\ncoNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYLlOmJzhjVizszN M4XGXGROW09? M3jEO2lEPTB;Mj6xOFYh|ryP NFmyelM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
TC32 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWn+OUDPxE1? MXzEUXNQ MlvITWM2OD1yLkCwPEDPxE1? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
HL60 (acute myelocytic) M1rEUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoH2glUh|ryP NGn5VYFFVVOR M1fqbWlEPTB;MD6xNkDPxE1? Mn;TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
TOV 21G NXi1RXVlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlrzglUh|ryP MlPGSG1UVw>? NX;ib|dTUUN3ME20MlI4QSEQvF2= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
TC71 M3z2UWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4O1Wp42KM7:TR?= NH3ydphFVVOR M1S5WWlEPTB;MD6wNVQh|ryP NF\wOnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
HPN-ALL (T-cell) NYrHdmtZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF32dZd,PSEQvF2= NXPac|NqTE2VTx?= M{jZdGlEPTB;MD61NkDPxE1? M1;DSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
A2780R NGfwPXpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH;PdnF,PSEQvF2= MoPaSG1UVw>? MlryTWM2OD1zLkW2OEDPxE1? M3\HfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
Rh1 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFn2SVh,PSEQvF2= M2DmXGROW09? M{PFfmlEPTB;MD6wNlch|ryP NVr2UGVCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
Kasumi-1 (acute myeloid) NIfkSYxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGr4cod,PSEQvF2= NXS5RotTTE2VTx?= NW\vOll{UUN3ME2wMlE3KM7:TR?= NHf3fXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
sk-ov-3 M17HcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF[4enp,PSEQvF2= NGfKWpVFVVOR NXTjb5Y2UUN3ME21MlEh|ryP MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
ME MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NITiU3l,PSEQvF2= M1HXdWROW09? M1XmcmlEPTB;MD6wNVUh|ryP Mkj1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
L1210 (Murine lymphocytic) MofUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIH5VnR,PSEQvF2= M{K0VmROW09? M{DqPGlEPTB;Mj6zPUDPxE1? M3vPbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
sw-626 NHfGeldIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUTyUYNkhjVizszN NYPYOmdtTE2VTx?= NFH4cJlKSzVyPUKuN|A3KM7:TR?= MlvIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
CTR MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVf+OUDPxE1? NV3VN5ZlTE2VTx?= NWLPbWNiUUN3ME2wMlI2OyEQvF2= Ml:xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
ML2 (Myelomonocytic) MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MU\+OUDPxE1? NYj5U4JvTE2VTx?= MUPJR|UxRTBwMEmg{txO M3PvSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
ovcar-3 M{DEOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4fKcZ42KM7:TR?= NHexPJRFVVOR MXvJR|UxRTVizszN MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
Rh36 NYPC[VZvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mo\3glUh|ryP NIfS[ppFVVOR NV\EN2tsUUN3ME2xMlQ{OiEQvF2= M4LldlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
MOLM-13 (acute myeloid) MnvvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{jz[Z42KM7:TR?= MWfEUXNQ MkfmTWM2OD1yLkSyJO69VQ>? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
ovcar-4 M3;BOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlLTglUh|ryP MV;EUXNQ MoDXTWM2OD1zIN88US=> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
Rh41 NVfUN294T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEe4dnh,PSEQvF2= MYrEUXNQ MnX0TWM2OD1yLkCwOUDPxE1? NGLidmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
Mutz 2 (acute myeloid) MlvSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVr+OUDPxE1? Mki2SG1UVw>? M3nV[mlEPTB;MT6xOUDPxE1? NIHyfYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
ovcar-5 MoDtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mn7GglUh|ryP NWLKVJk6TE2VTx?= M1viSmlEPTB;MD6wOUDPxE1? NGn1NoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
RD1 NXvkOHZlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlfhglUh|ryP MULEUXNQ MU\JR|UxRTBwME[4JO69VQ>? MmSyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
OCI-AML 2 (acute myeloid) MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX;+OUDPxE1? NFnDR4RFVVOR NF\MPFFKSzVyPUOuN|Mh|ryP MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
786-O M3Ww[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MorYglUh|ryP MUXEUXNQ M1rFZmlEPTB;MT62OFch|ryP MkLIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
A673 NHXu[2RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoSwglUh|ryP MYHEUXNQ NYXNRVlZUUN3ME2wMlQxQCEQvF2= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
TALL-1 (T-cell) NEnBVFRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1G5VJ42KM7:TR?= NFHQXmVFVVOR NUe5WFdLUUN3ME2xMlI5KM7:TR?= NUmxc4VYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
151-B M4nXSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFn5Zll,PSEQvF2= M4nyXmROW09? MlHmTWM2OD1{Lk[3JO69VQ>? NXv0bYI6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
PFSK-1 NEnWcJJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmTEglUh|ryP NXHZXYo3TE2VTx?= NVzNV|BMUUN3ME2wMlE{OiEQvF2= NIjQdVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
THP-1 NVfiW41uT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGPKenV,PSEQvF2= M{Wxb2ROW09? M3XYSmlEPTB;Nj61PEDPxE1? NIHkW3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
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SK-NAS M2W1Omdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIjwU4J,PSEQvF2= M2qzRmROW09? NYTrdI0zUUN3ME2wMlQ6PyEQvF2= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
CTLL2 NXXLRmdIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1f0fJ42KM7:TR?= MVLEUXNQ MnrFTWM2OD5zLkCwJO69VQ>? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
HTB-47 MkfnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGTDZVZ,PSEQvF2= M3;pfmROW09? NV;CUm9yUUN3ME2yMlA2PiEQvF2= M33jXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
LAN-1 NH\DdmVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWD+OUDPxE1? NEntToNFVVOR NW\lRYYyUUN3ME2wMlA1KM7:TR?= NIniNYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
ST486 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIDWdlV,PSEQvF2= MWLEUXNQ M1LtUmlEPTB;MT6xPUDPxE1? Mor1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
HS766T NXjDNXlRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoK4glUh|ryP M1PVT2ROW09? MYXJR|UxRTJwMECxJO69VQ>? NIrQc2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
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Daudi (Burkitt's) M4\IbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUfacnNGhjVizszN MVzEUXNQ NXLib2tOUUN3ME2yMlY{PyEQvF2= NGPvN|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
Aspc-1 MoPDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYj+OUDPxE1? NW\rbpNFTE2VTx?= M{HDc2lEPTB;MD6zO|kh|ryP NV2yNJdVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
SK-NSH M{HFfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1uwZ542KM7:TR?= NXHTPYl2TE2VTx?= MYXJR|UxRTBwMUO5JO69VQ>? NEKzfGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
MEC-1 (Chronic B cell) MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1ftXZ42KM7:TR?= NXzl[3gxTE2VTx?= M1uyTmlEPTB;Mj62N|ch|ryP NUfhS2k5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
Capan-2 MmfjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF3a[nd,PSEQvF2= NEX3SHhFVVOR M{LkV2lEPTB;MT63O|Qh|ryP MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
SHSY5Y MkfLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWT+OUDPxE1? NIPiXIdFVVOR M2PhT2lEPTB;MD6xNFYh|ryP NWW3NFR1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
U937 (Histioocytic) M3zLPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVjEe4RjhjVizszN NFzy[nlFVVOR NGT0XFdKSzVyPkWuNFAh|ryP NYfKfmwxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
Bxpc-1 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NILUZlB,PSEQvF2= M{HMZmROW09? NUftRnljUUN3ME2xMlkzPCEQvF2= NVP1VFRzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
Bxpc-3 Mk\BS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkLHglUh|ryP MYnEUXNQ MlPMTWM2OD53LkCwJO69VQ>? NGnwV5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
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PANC-1 M{Tuemdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVX+OUDPxE1? Mk\ySG1UVw>? NXK3eW9EUUN3ME61MlAxKM7:TR?= Ml3kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
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RPMI 8226 NVvpN3psT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH\F[VJ,PSEQvF2= NGDYU|BFVVOR M1rQRWlEPTB;MT6yPVMh|ryP NIi4Xmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
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U266 B1 MnHHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYnBTVFPhjVizszN NULs[Vk5TE2VTx?= MYjJR|UxRTFwNk[5JO69VQ>? NFzVeYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
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NCI-446 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVv2bG5ChjVizszN MkDoSG1UVw>? MVPJR|UxRTFwMUW0JO69VQ>? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
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JJN3 NUWxNppCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV\ufJhqhjVizszN M{\VUmROW09? M4PkOGlEPTB;Mj60N|Mh|ryP NVPOdGxnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
SU.86.86 NHv3R5ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHqyVmN,PSEQvF2= M1:wUWROW09? M{O0W2lEPTB;Mj62O|Ih|ryP MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
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MDA-MB-468 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnPZglUh|ryP MWrEUXNQ MWDJR|UxRTBwNUC0JO69VQ>? MnvhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
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PF-382 NWnxeYpQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnhSYFKdmirYnn0bY9vKG:oIHj1cYFvKFCILUO4NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPDJwMEK0NkDPxE1w NX7IWHV6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd3NES4M{c,W0GQR1XSQE9iRg>?
IST-SL1 NYHFXJd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn:4TY5pcWKrdHnvckBw\iCqdX3hckBKW1RvU1yxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1Oi5|MkS3JO69VS5? M2CwO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4PTR2OD:nQnNCVkeHUkyvZV4>
MKN7 MmD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1voU2lvcGmkaYTpc44hd2ZiaIXtZY4hVUuQNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gOFIvPDl5NzFOwG0v NYjnTm1PRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd3NES4M{c,W0GQR1XSQE9iRg>?
CP50-MEL-B M1n2PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGNRPTBvTVXMMWIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDR{Lk[5NFEh|ryPLh?= MoHDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc2PDR6Lze+V2FPT0WUPD;hQi=>
K052 NUL5O4Q2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJcohq[mm2aX;uJI9nKGi3bXHuJGsxPTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IESzMlA3QThizszNMi=> Ml7hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc2PDR6Lze+V2FPT0WUPD;hQi=>
23132-87 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfETY5pcWKrdHnvckBw\iCqdX3hckAzOzF|Mj24O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPDNwNUK4OkDPxE1w MkfyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc2PDR6Lze+V2FPT0WUPD;hQi=>
GAK M4nx[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3sTY5pcWKrdHnvckBw\iCqdX3hckBISUtiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IES0MlEzPyEQvF2u NVKxbGJkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd3NES4M{c,W0GQR1XSQE9iRg>?
Mewo M4O4bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGSzdZlKdmirYnn0bY9vKG:oIHj1cYFvKE2nd3:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQ2NjV6N{ig{txONg>? NH73U3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzV2NEivK|5USU6JRWK8M4E,
RMG-I MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoD1TY5pcWKrdHnvckBw\iCqdX3hckBTVUdvSTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gOFUvPzN5MjFOwG0v MoHDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc2PDR6Lze+V2FPT0WUPD;hQi=>
BE-13 NVG1T3lsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJcohq[mm2aX;uJI9nKGi3bXHuJGJGNTF|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC0OU46Ozl{IN88UU4> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|U1PDhxJ{7TRW5ITVJ:L3G+
SW684 M32yeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\Jcohq[mm2aX;uJI9nKGi3bXHuJHNYPjh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC0O{41QTZ7IN88UU4> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|U1PDhxJ{7TRW5ITVJ:L3G+
Assay
Methods Test Index PMID
Western blot p-IGFIRRβ/InsRβ / IGFIRβ / p-AKT / AKT / p-ERK / ERK 26136493
Growth inhibition assay Cell viability 30754629
体内研究 BMS-754807(12.5mg/kg,口服)作用于携带 IGF-1R-Sal肿瘤的裸鼠,抑制肿瘤和血清中IGF-1R磷酸化。BMS-754807作用于一组选定的上皮(IGF-1R-Sal, GEO, 和Colo205),造血(JJN3)和间质(RD1和Rh41)移植瘤模型,抑制肿瘤生长,肿瘤生长抑制率从53%至115%不等。[1] BMS-754807 (6.25 mg/kg) 作用于转基因的IGF-Sal肿瘤小鼠模型,完全抑制肿瘤生长,且抑制pIGF-1R 和 pAKT。BMS-754807与小鼠血浆和人类血浆的蛋白结合率分别为98.5% 和95.9%。BMS-754807 (25 mg/kg)作用于携带KT-5 (Wilms), KT-14 (rhabdoid), Rh28 (rhabdomyosarcoma), 和 OS-1移植瘤的小鼠模型,显著抑制肿瘤。[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:[1]
  • 激酶抑制实验:

    在体外激酶实验中使用重组人类 IGF-1受体酶测定BMS-754807,在生化实验中使用合成肽KKSRGDYMTMQIG 作为磷酸受体底物测定BMS-754807。在Ubottom 384孔板中使用 30 μL实验缓冲液 (100 mM Hepes pH 7.4, 10 mM MgCl2, 0.015% Brij35 and 4 mM DTT)来进行酶活测定。通过结合ATP,1.5 μM 荧光标记肽底物, 酶和BMS-754807而开始反应,反应持续60分钟。加入EDTA终止反应。通过电泳分离荧光底物和磷酸化产物,然后在Caliper LabChip 3000上分析反应混合物。通过对剂量反应曲线进行非线性回归分析而获得IC50值。

细胞实验:[1]
  • Cell lines: IGF-1R-Sal, RH41 和 Geo 细胞系
  • Concentrations: 365 nM
  • Incubation Time: 72 小时
  • Method: 细胞按最佳密度培养在RPMI + GLUTAMAX培养基中,培养基中含有有10% 热灭活的胎牛血清(FBS),10mMHepes,青霉素和链霉素。BMS-754807处理细胞72小时后,通过测定3H-胸甘渗透到DNA中的程度而测评细胞增殖。结果表示为IC50。
动物实验:[1]
  • Animal Models: 携带IGF-1R-Sal, GEO, Colo205, JJN3, RD1 或 Rh41 肿瘤的裸鼠
  • Dosages: 150 mg/kg
  • Administration: 口服

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):
2% DMSO+30% PEG 300+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 461.49
化学式

C23H24FN9O

CAS号 1001350-96-4
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
NCT01525823 Completed Drug: BMS-754807 (IGR-IR/IR Inhibitor)|Drug: Metformin Healthy Volunteers Bristol-Myers Squibb February 2012 Phase 1
NCT00908024 Terminated Drug: BMS-754807|Drug: cetuximab (Erbitux®) Colorectal Cancer|Head and Neck Cancer|Neoplasm Metastasis Bristol-Myers Squibb October 2009 Phase 1|Phase 2
NCT00898716 Completed Drug: BMS-754807 Neoplasms Bristol-Myers Squibb September 2009 Phase 1
NCT00788333 Completed Drug: BMS-754807|Drug: trastuzumab (Herceptin®) Breast Cancer Bristol-Myers Squibb July 2009 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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