PLX-4720

目录号:S1152

仅限科研使用

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。

PLX-4720 Chemical Structure

CAS: 918505-84-7

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 5496.89 现货
大包装 有超大折扣
大剂量询单有大折扣!

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PLX-4720发表文献167篇:

产品安全说明书

Raf抑制剂选择性比较

相关Raf产品

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 M4HxRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTBwMEe0OVch|ryP M1PzbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
EoL-1-cell M2XYUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PMe2lEPTB;MD6xOFE3PiEQvF2= NH3kSHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
C32 NED4OGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HYRWlEPTB;MD6xOVE{OSEQvF2= M3;zT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
M14 Ml\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33CdWlEPTB;MD6yNVc2PyEQvF2= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
CP50-MEL-B NU[1[4VJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTBwMkm3PFQh|ryP NYj0NIMzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
A101D M17Xbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTBwM{K1PFkh|ryP M3ntVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
G-361 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETOcotKSzVyPUCuN|Q3OzdizszN NIPCNm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
HT-144 M{O5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPKR5ZtUUN3ME2wMlM3OzJ7IN88US=> Mlf1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
ACN M3K0cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjVS4pkUUN3ME2wMlM5PDd5IN88US=> NGi1Wpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
COLO-829 M3T2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwM{i5Olgh|ryP MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
MEL-HO NW\tVGtyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjKTWM2OD1yLkSxNVc6KM7:TR?= NXu2cJN1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
SH-4 NYW1PFZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTBwNEG0NlIh|ryP NYnYZ|dCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
SK-MEL-3 NYL4XGoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnFNWdKSzVyPUCuOVE2PjhizszN MnKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
A375 M2X3d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fhWmlEPTB;MD62O|M2QSEQvF2= M2PqWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
MMAC-SF MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHuTWM2OD1yLk[4OlE1KM7:TR?= NXnlSHR[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
BHT-101 Mn7sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTBwN{C3NFIh|ryP NUjwSmZORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
K5 NYnlXIRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\PXVBRUUN3ME2wMlc3OTR6IN88US=> M33EelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
BV-173 NX\VdJJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HBSmlEPTB;MD63PVY1PCEQvF2= MoroQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
RVH-421 NWnNdo9nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTuTWM2OD1yLki2O|k3KM7:TR?= NYf4VXlmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
HCC2218 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnsTWM2OD1yLki3PFQ1KM7:TR?= NH3RUmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
WM-115 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTBwOEi2PVIh|ryP M373clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
SK-MEL-28 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTFwMES1Olkh|ryP NWTpWYtGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
COLO-679 MlPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILGS5RKSzVyPUGuNVA1PjRizszN Mk[zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
MZ7-mel NUPxUZgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3iTWM2OD1zLkG0PVY{KM7:TR?= MmnrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
SK-MEL-30 M37pfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfMTWM2OD1zLkOzN|g3KM7:TR?= NXHNXlRuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
NCI-H209 NWjQXoFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rXXmlEPTB;MT62NFg3KM7:TR?= NXHrUo8zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
HTC-C3 M1PYNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTFwNk[yPVQh|ryP MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
KARPAS-45 NIL1UYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrITWM2OD1{LkC0PVc5KM7:TR?= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
NCI-SNU-5 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXxTWM2OD1{LkGxPVY6KM7:TR?= NWHEeottRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
KP-4 MkL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIX4bnpKSzVyPUKuN|A4QDdizszN M2C5eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
PA-1 Mmn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XSTGlEPTB;Mj63NlY4OyEQvF2= NFHHc2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
HuO-3N1 MnvFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPuTWM2OD1{Lki3PVQ3KM7:TR?= M4nBSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
NCI-H358 NUCwVIp7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3z2cmlEPTB;Mj65NlI{OiEQvF2= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
CTB-1 M2rFbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTNwNECxO|Yh|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
697 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\vcnFKSzVyPUOuOVUzPjZizszN NFLzPXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
CP66-MEL NYXMPYN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37COGlEPTB;ND6xOVkzPyEQvF2= M4LQXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
NB13 NVzMO5NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFju[ZFKSzVyPUSuOFkyPzlizszN MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
DBTRG-05MG NV3YNYJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTRwNUOzNlUh|ryP NFXuUHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
A2058 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfRV5k2UUN3ME20MlczOTZ2IN88US=> NH;uOoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
KG-1 NELwOW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTRwN{O5NFgh|ryP NYD6Z3UzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
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RD NXL3NlVYeUiWUzDhd5NigQ>? M1W3VJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCURDDj[Yxtew>? MkDCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH NIfF[4NyUFSVIHHzd4F6 M3yzXpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz NHrWd|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 NV3xWGtteUiWUzDhd5NigQ>? MVHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| M{HmWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 MmqwdWhVWyCjc4PhfS=> MYnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| NYXXcYlLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 NWG4VG1xeUiWUzDhd5NigQ>? Mnv1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NVPOV|l5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC NV\tdIl5eUiWUzDhd5NigQ>? NWHrWmhTeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NELB[ZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Assay
Methods Test Index PMID
Western blot p-MEK / MEK / p-ERK / ERK / p-FAK(S910) p-EGFR 1173 / EGFR / p-Akt / Akt p27 / Cyclin D1 / pRb pAkt(Ser473) / pAkt(Thr308) 23076151 26023796 21828154
Immunofluorescence LAMP1 ZKSCAN3 / TFEB 30979895
Growth inhibition assay Cell viability 27848137
ELISA mIFN-γ 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]
  • 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]
  • 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。
动物实验:[1]
  • 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

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+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 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

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

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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.