PLX-4720

For research use only. Not for use in humans.

目录号:S1152

PLX-4720 Chemical Structure

CAS No. 918505-84-7

PLX-4720是一种有效的,选择性的B-RafV600E抑制剂,无细胞试验中IC50为13 nM,同样有效地作用于c-Raf-1(Y340D和Y341D突变型),作用于B-RafV600E比作用于野生型B-Raf选择性高10倍。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1266.55 现货
RMB 976.01 现货
RMB 2186.24 现货
RMB 3906.63 现货
RMB 5496.89 现货
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客户使用Selleck生产的PLX-4720发表文献153篇:

产品安全说明书

Raf抑制剂选择性比较

生物活性

产品描述 PLX-4720是一种有效的,选择性的B-RafV600E抑制剂,无细胞试验中IC50为13 nM,同样有效地作用于c-Raf-1(Y340D和Y341D突变型),作用于B-RafV600E比作用于野生型B-Raf选择性高10倍。
靶点
C-Raf-1 (Y340D/Y341D) [1]
(Cell-free assay)
B-Raf (V600E) [1]
(Cell-free assay)
BRK [1]
(Cell-free assay)
B-Raf [1]
(Cell-free assay)
6.7 nM 13 nM 130 nM 160 nM
体外研究

PLX-4720高亲和力与活性B-RafV600E和c-Raf-1Y340D/Y341D结合,作用于野生型B-Raf选择性>10倍,作用于其他激酶如Frk, Src, Fak, FGFR, 和Aurora A 选择性>100倍,IC50为1.3-3.4 μM。与有效的选择性相一致, PLX-4720作用于携带B-RafV600E的细胞系,显著抑制ERK磷酸化,IC50为14-46 nM, 但是对携带野生型B-Raf的细胞没有作用效果。PLX-4720 作用于携带B-RafV600E致癌基因(如COLO205, A375, WM2664, 和 COLO829)的肿瘤细胞系,显著抑制细胞生长,GI50 分别为 0.31 μM, 0.50 μM, 1.5 μM, 和 1.7 μM。此外, 1 μM PLX-4720 只有作用于B-RafV600E-阳性1205Lu细胞, 诱导细胞周期停滞和凋亡,而作用于B-Raf 野生型C8161细胞则无此效果。[1]10 μM PLX-4720 处理PTEN+细胞,诱导BIM表达,比PTEN-细胞系(4倍-fold)高14倍,说明PTEN-细胞系抗PLX-4720诱导的凋亡。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DU-4475 NXy3[mpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLSTWM2OD1yLkC3OFU4KM7:TR?= NWP5fWw2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
EoL-1-cell NIH5OFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vHfmlEPTB;MD6xOFE3PiEQvF2= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
C32 NHPHOmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;NTWgzUUN3ME2wMlE2OTNzIN88US=> M3rPTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
M14 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmiwTWM2OD1yLkKxO|U4KM7:TR?= NVLDR|AxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
CP50-MEL-B MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDhVIFHUUN3ME2wMlI6Pzh2IN88US=> NVizflRuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
A101D NXXDZ3VlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4WzdGlEPTB;MD6zNlU5QSEQvF2= NFzyU|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
G-361 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGj0V25KSzVyPUCuN|Q3OzdizszN MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
HT-144 NF;GXZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn36TWM2OD1yLkO2N|I6KM7:TR?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
ACN NV;EW3FsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fO[GlEPTB;MD6zPFQ4PyEQvF2= M1vSblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
COLO-829 MmDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfrTWM2OD1yLkO4PVY5KM7:TR?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
MEL-HO NH3jSlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnCTWM2OD1yLkSxNVc6KM7:TR?= Mmr6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
SH-4 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwNEG0NlIh|ryP NHL3ZW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
SK-MEL-3 NIjVVnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPMVItYUUN3ME2wMlUyPTZ6IN88US=> NV3T[pU1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
A375 MkjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPpTWM2OD1yLk[3N|U6KM7:TR?= NV;aOmZzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
MMAC-SF MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYD2eJRHUUN3ME2wMlY5PjF2IN88US=> Mn7hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
BHT-101 MkO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTBwN{C3NFIh|ryP NFrTRm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
K5 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[5cWlEPTB;MD63OlE1QCEQvF2= NFnlPHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
BV-173 MlTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWGydlQ6UUN3ME2wMlc6PjR2IN88US=> NIDF[VU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
RVH-421 MkfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2S2fmlEPTB;MD64Olc6PiEQvF2= NVv0c2FxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
HCC2218 NX;XU3hYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjTdZV7UUN3ME2wMlg4QDR2IN88US=> NX\uN3BLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
WM-115 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\iTWM2OD1yLki4OlkzKM7:TR?= NWPMT3B5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
SK-MEL-28 M3nGUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvlZ2I{UUN3ME2xMlA1PTZ7IN88US=> NFnZUZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
COLO-679 Ml;pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvuTWM2OD1zLkGwOFY1KM7:TR?= NEjsTII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
MZ7-mel MlvRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2i2WWlEPTB;MT6xOFk3OyEQvF2= M1;OflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
SK-MEL-30 NInV[IhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFviR4pKSzVyPUGuN|M{QDZizszN NFfKSHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
NCI-H209 NHHMVHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfNW|FyUUN3ME2xMlYxQDZizszN NYXaZXE{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
HTC-C3 NFPXWGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mke3TWM2OD1zLk[2Nlk1KM7:TR?= Mom5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
KARPAS-45 NYTnU4tTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjEeopEUUN3ME2yMlA1QTd6IN88US=> NIKySpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
NCI-SNU-5 NGPxO|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnniTWM2OD1{LkGxPVY6KM7:TR?= NWXrNoRrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
KP-4 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXOwSoNLUUN3ME2yMlMxPzh5IN88US=> M{i5eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
PA-1 NV\BbIZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzqNJlEUUN3ME2yMlczPjd|IN88US=> MkDSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
HuO-3N1 MoLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jDVWlEPTB;Mj64O|k1PiEQvF2= NF;5TmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
NCI-H358 M{fQT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fOdGlEPTB;Mj65NlI{OiEQvF2= NYLrRVB{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
CTB-1 NXPz[XJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXYeJA3UUN3ME2zMlQxOTd4IN88US=> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
697 M2nJ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmG3TWM2OD1|LkW1NlY3KM7:TR?= M4HNfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
CP66-MEL M2DTOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HTe2lEPTB;ND6xOVkzPyEQvF2= MnjrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
NB13 MnnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nmVGlEPTB;ND60PVE4QSEQvF2= MlSwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
DBTRG-05MG NI\EbItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TyfWlEPTB;ND61N|MzPSEQvF2= NVjDUHhsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
A2058 NEPpTWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zvTmlEPTB;ND63NlE3PCEQvF2= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
KG-1 NYHne3BUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnSVmlHUUN3ME20Mlc{QTB6IN88US=> Mn76QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
8305C MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWq4N4U{UUN3ME21MlE5PzNizszN M{nTcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
RPMI-7951 NXTBbJB1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nOe2lEPTB;NT64NFI5OyEQvF2= NELXUVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
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GCT NELaNZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HlbGlEPTB;OD63OVMyPCEQvF2= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
KY821 NXP2XI12T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTlwMEWxO|gh|ryP MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
JVM-3 NH[0bZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXCUZBKSzVyPUmuOVY6QTlizszN MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
RS4-11 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jDdGlEPTB;OT62NFQ5KM7:TR?= NHXoUok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
VA-ES-BJ NI\RNoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkniTWM2OD1zMD6wNVQ6KM7:TR?= M2PxWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
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SK-MEL-24 M4HN[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXETIdKSzVyPUGwMlgzPzRizszN MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
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KNS-62 MlzXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfLTWM2OD1zMT6yOFA1KM7:TR?= NHuyOpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
SK-HEP-1 NXTsW2lZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljPTWM2OD1zMT6zOVI4KM7:TR?= NETYXZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
A3-KAW MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LTNWlEPTB;MUGuO|E4QCEQvF2= M4jrWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
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BB65-RCC M1n1UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTF{LkexOlkh|ryP NF6zPFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
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Daoy M1fUNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TjTmlEPTB;MUWuO|YyPiEQvF2= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
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MZ2-MEL NF;t[3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2faOGlEPTB;MU[uNFY1PiEQvF2= NXzq[W5oRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
CAL-12T Ml7jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1H6R2lEPTB;MU[uOFg3OiEQvF2= MnfzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
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A673 MmDidWhVWyCjc4PhfS=> NF7XUpJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= MnTFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 MVPxTHRUKGG|c3H5 NGPmXIRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz NWPtRZNVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD MYfxTHRUKGG|c3H5 NH\vRm9yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? Mk\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH NF:y[mtyUFSVIHHzd4F6 MVnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= MmK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 MkC1dWhVWyCjc4PhfS=> NXjlVmxseUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> Mn[2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 M3nqPZFJXFNiYYPzZZk> NWLuepd1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> NWLOO|E6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 NXPIeYdReUiWUzDhd5NigQ>? NU\l[ohveUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> NXXn[2lMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC NHnLN45yUFSVIHHzd4F6 M4\zNpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz NXnRZXl3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-MEK / MEK / p-ERK / ERK / p-FAK(S910); 

PubMed: 23076151     


WM793 and WM793-Res NRAS cells were seeded overnight in the absence of PLX4720 and then treated with 1 μm PLX4720 for times ranging from 0 to 24 h. Samples were analyzed by Western blotting for phospho-MEK, total MEK, phospho-ERK1/2, total ERK1/2, phospho-S910 FAK, and total FAK.

p-EGFR 1173 / EGFR / p-Akt / Akt; 

PubMed: 26023796     


Three BRAF(V600E) glioma cell lines, NMC-G1, AM38 and DBTRG-05MG were subjected to a 24 hour time course treatment with 5 μM PLX4720 in the presence or absence of 1 μM HKI-272. These cells were serum starved for 16 hours before being stimulated with 10% FBS and harvested for immunoblotting analysis. Cells treated with PLX4720 alone showed an initial suppression of MEK and ERK phosphorylation followed by a profound rebound of MAPK pathway activation as early as one hour post-PLX4720 treatment. Elevated levels of EGFR phosphorylation were also observed in the PLX4720 treated cells. The extent of Akt phosphorylation increased upon PLX4720 treatment, although the extent varies between cell lines. In contrast, no reactivation of EGFR, MEK, ERK or Akt was observed in cells pre-treated with HKI-272.

p27 / Cyclin D1 / pRb; 

PubMed: 21828154     


Immunoblot analysis revealed that PLX4720 (3 μM) decreased levels of phosphorylated ERK, decreased levels of cyclin D1, increased levels of p27, and decreased levels of phosphorylated Rb in BRAF-mutant (OCM3) cells. On the contrary, in Gα-mutant (OMM1.3) UM cells, PLX4720 induced a paradoxical increase in phosphorylated ERK and Rb levels and an early increase in cyclin D1 levels but did not stimulate p27 levels.

pAkt(Ser473) / pAkt(Thr308); 

PubMed: 21828154     


Immunoblot analysis revealed that both AZD6244 and PLX4720 induced an early (within 2–6 hours of exposure) increase in the levels of phosphorylated Akt (at residues Ser473 and Thr308) in both BRAF-mutant OCM3 and Gα-mutant OMM1.3 cells. Eventually, and with prolonged drug exposure, the phosphorylation of Akt returned to baseline in Gα-mutant OMM1.3 cells and decreased even below baseline levels in BRAF-mutant OCM3 cells.

23076151 26023796 21828154
Immunofluorescence
LAMP1; 

PubMed: 30979895     


Representative images of LysoTracker Red (red) and LAMP1 (green) immunostaining of PLX4720 (1 μM, 12 h-treated) A375 cells with depletion of the indicated genes. Note the reduced lysosome staining in PLX4720-treated cells upon TFEB depletion. 

ZKSCAN3 / TFEB ; 

PubMed: 30979895     


Representative confocal images of subcellular translocation of endogenous TFEB (green) and ZKSCAN3 (red) in A375 cells treated with PLX4720 (1 μM, 12 h). n = 3 independent experiments. 

30979895
Growth inhibition assay
Cell viability; 

PubMed: 27848137     


AM-38 and DBTRG-05MG cells were treated for 5 days. Media was changed once every 3 days. Cell viability was measured using WST-1 assay. Error bars indicate the variation between triplicate measurements. PLX4720 and PD0325901 alone or in combination reduced cell viability significantly. However, combined therapy led to the most significant cell viability reduction compared to either monotherapy in both AM-38 and DBTRG-05MG cell lines.

27848137
ELISA
mIFN-γ; 

PubMed: 23204132     


(C, D and E) IFN-γ secretion by pmel-1 T cells co-cultured with transduced melanoma cells (after cell sorting) that had been pre-treated with the indicated concentrations of PLX4720, as determined by ELISA. (*P<0.05, ** P<0.01) Data are representative of 3 independent experiments.

23204132
体内研究 PLX-4720每天按20 mg/kg剂量口服给药依赖B-RafV600E的COLO205移植瘤,显著延迟肿瘤生长,且引起肿瘤衰退, 即使按1 g/kg剂量处理也不会对小鼠造成明显的不利影响。PLX-4720按 100 mg/kg剂量处理 携带B-RafV600E的1205Lu 移植瘤,每天两次,几乎完全消除肿瘤, 而对携带野生型B-Raf的C8161 移植瘤则没有作用活性。PLX-4720 作用于含V600E突变细胞的抗癌效果与阻断MAPK通路相关。[1] PLX-4720每天按30 mg/kg剂量处理8505c肿瘤,显著抑制肿瘤生长,抑制达90%以上,也显著降低远处肺转移。[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]
- 合并

体外Raf激酶活性实验:

通过测量生物素-MEK蛋白,使用Perkin-Elmer's AlphaScreen 技术测定体外野生型和突变型Raf的激酶活性。在20 mM Hepes (pH 7.0), 10 mM MgCl2, 1 mM DTT, 0.01% Tween-20, 100 nM 生物素-MEK 蛋白,多种ATP浓度,及浓度不断增高的PLX-4720混合物中在室温下进行每组酶(0.1 ng)反应,反应体积为20-μL。 在 2, 5, 8, 10, 20,和 30分钟加入5 μL含20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, 和 0.3% BSA的溶液终止反应。终止液包括磷酸-MEK抗体, 链霉亲和素包被的供体珠,和AlphaScreen蛋白 A检测试剂盒中的蛋白A受体珠。抗体和小株在终止液中在室温下黑暗温育30分钟。抗体最终按 1:2,000稀释,每个小珠终浓度为 10 μg/mL。实验板在室温下温育1小时,然后在 PerkinElmer AlphaQuest 读数器上读数。
细胞实验:[1]
- 合并
  • Cell lines: COLO205, A375, WM2664, COLO829, HT716, SW620, H460, Calu-6, HCT116, SK-MEL2, SK-MEL3, Lovo, H1299, 1205Lu, 和C8161
  • Concentrations: 溶于DMSO, 终浓度为~1 mM
  • Incubation Time: 24, 48, 和 72小时
  • Method: 使用不同浓度PLX-4720 for处理细胞 24, 48,和72小时通过 CellTiter-GLO荧光细胞活性检测或MTT实验测定细胞增殖。为了分析细胞周期, 收集上清液和细胞, 制成颗粒,与70%乙醇混合。在使用碘化丙啶 (10 μg/mL)染色前,细胞在0.5 mg/mL RNase I 中37oC下温育1小时,除去残留RNA污染样本。使用EPICS XL仪分析样本。为了测定凋亡, 获得培养基和细胞,制成颗粒,然后使用膜联蛋白-FITC和碘化丙啶染色。然后再使用EPICS XL仪分析样本。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 皮下移植 COLO205 细胞的雌性无胸腺NCr nu/nu小鼠, 携带1205Lu或C8161 细胞的SCID小鼠
  • Dosages: 5, 20, 或100 mg/kg
  • Administration: 口服饲喂,每天一次或两次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 83 mg/mL (200.56 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):
2% DMSO+50% 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 413.83
化学式

C17H14ClF2N3O3S

CAS号 918505-84-7
储存条件 粉状
溶于溶剂
别名 N/A

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
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、MSDS / 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、MSDS / 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

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 would you recommend to make working solution for intraperitoneal injection into mice?

  • 回答:

    PLX4720 has very limited solubility in aqueous solution and for this reason, we recommend oral gavage to administer this compound as not fully dissolved suspension can be used in oral gavage feeding.

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

相关Raf产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID