PLX-4720

For research use only. Not for use in humans.

目录号:S1152

PLX-4720 Chemical Structure

Molecular Weight(MW): 413.83

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 5496.89 现货
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客户使用Selleck生产的PLX-4720发表文献110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 NHntXmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTBwMEe0OVch|ryP MX7TRW5ITVJ?
EoL-1-cell NFvOWGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnLXnhKSzVyPUCuNVQyPjZizszN NWTLUINEW0GQR1XS
C32 Ml\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TKSWlEPTB;MD6xOVE{OSEQvF2= M4rldnNCVkeHUh?=
M14 NF7oXnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\hTWM2OD1yLkKxO|U4KM7:TR?= NFLXRmlUSU6JRWK=
CP50-MEL-B NEPCPVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPTTWM2OD1yLkK5O|g1KM7:TR?= NWDUdI1qW0GQR1XS
A101D NFOxPZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ewZ2lEPTB;MD6zNlU5QSEQvF2= NVLUZ2NnW0GQR1XS
G-361 M1rETGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVK1ToNyUUN3ME2wMlM1PjN5IN88US=> MXXTRW5ITVJ?
HT-144 MonRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnmNmxbUUN3ME2wMlM3OzJ7IN88US=> NI\GWWxUSU6JRWK=
ACN NFPtSY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjTTWM2OD1yLkO4OFc4KM7:TR?= NX;DRVNEW0GQR1XS
COLO-829 NHnGfodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDhN2VMUUN3ME2wMlM5QTZ6IN88US=> Mkm0V2FPT0WU
MEL-HO MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHyTJVKSzVyPUCuOFEyPzlizszN MlvkV2FPT0WU
SH-4 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHPTWM2OD1yLkSxOFIzKM7:TR?= NHnDemZUSU6JRWK=
SK-MEL-3 MoWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PDb2lEPTB;MD61NVU3QCEQvF2= MnHDV2FPT0WU
A375 M1HqdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTBwNkezOVkh|ryP MWrTRW5ITVJ?
MMAC-SF MlW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\LRoxKSzVyPUCuOlg3OTRizszN MkmyV2FPT0WU
BHT-101 NWHqWmhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwN{C3NFIh|ryP NW\ZUXZWW0GQR1XS
K5 NWfI[GlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHm5SllKSzVyPUCuO|YyPDhizszN NH;xSplUSU6JRWK=
BV-173 NFjvbI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTWUnptUUN3ME2wMlc6PjR2IN88US=> MUPTRW5ITVJ?
RVH-421 NVPWVnVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTBwOE[3PVYh|ryP MXrTRW5ITVJ?
HCC2218 NUj5NVE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIi0fYxKSzVyPUCuPFc5PDRizszN M2XjcXNCVkeHUh?=
WM-115 NH3XbVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[zWmV6UUN3ME2wMlg5Pjl{IN88US=> MnL2V2FPT0WU
SK-MEL-28 M1\UVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHKxWW1KSzVyPUGuNFQ2PjlizszN M{H5NXNCVkeHUh?=
COLO-679 MnfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DpbmlEPTB;MT6xNFQ3PCEQvF2= MoHiV2FPT0WU
MZ7-mel MmW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLQTWM2OD1zLkG0PVY{KM7:TR?= MX3TRW5ITVJ?
SK-MEL-30 MmLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTFwM{OzPFYh|ryP M{e1XHNCVkeHUh?=
NCI-H209 M4nrUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLKO|dkUUN3ME2xMlYxQDZizszN NV3mbo85W0GQR1XS
HTC-C3 NF;FXY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jPNWlEPTB;MT62OlI6PCEQvF2= NWrpcnhGW0GQR1XS
KARPAS-45 NH;YNXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml64TWM2OD1{LkC0PVc5KM7:TR?= M4rKeHNCVkeHUh?=
NCI-SNU-5 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGm3OnVKSzVyPUKuNVE6PjlizszN NXfZVJI2W0GQR1XS
KP-4 M2XvTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkKyTWM2OD1{LkOwO|g4KM7:TR?= MVfTRW5ITVJ?
PA-1 NYq0cWxmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvxeGdVUUN3ME2yMlczPjd|IN88US=> M3zLcnNCVkeHUh?=
HuO-3N1 NWjNcnl5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnj5TWM2OD1{Lki3PVQ3KM7:TR?= MWDTRW5ITVJ?
NCI-H358 NInsbXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1[0bmlEPTB;Mj65NlI{OiEQvF2= NIjlOXZUSU6JRWK=
CTB-1 M4nOOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDaTWM2OD1|LkSwNVc3KM7:TR?= NHvUc4lUSU6JRWK=
697 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HHcWlEPTB;Mz61OVI3PiEQvF2= NWLq[YE6W0GQR1XS
CP66-MEL M1nzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXMco9KSzVyPUSuNVU6OjdizszN M4XKSHNCVkeHUh?=
NB13 NXvjZ|V[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PzfGlEPTB;ND60PVE4QSEQvF2= MoXyV2FPT0WU
DBTRG-05MG MoXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\TTWM2OD12LkWzN|I2KM7:TR?= MXzTRW5ITVJ?
A2058 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1e5VmlEPTB;ND63NlE3PCEQvF2= NWC5dZIzW0GQR1XS
KG-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjqVod6UUN3ME20Mlc{QTB6IN88US=> M1;uOXNCVkeHUh?=
8305C MmjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;qTWM2OD13LkG4O|Mh|ryP MWTTRW5ITVJ?
RPMI-7951 M2S0d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTVwOECyPFMh|ryP M{TiZnNCVkeHUh?=
CHL-1 M4PMdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7oSJJKSzVyPUWuPVc3ODNizszN NFXuPIVUSU6JRWK=
TI-73 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkj1TWM2OD14LkCwPVAzKM7:TR?= MVfTRW5ITVJ?
HT-1080 MkfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTZwMUC5OFYh|ryP Mn3CV2FPT0WU
ES5 NWHjfJdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1G0cmlEPTB;Nj6xOFkzPCEQvF2= NUnEUJVjW0GQR1XS
8-MG-BA MleyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rrOGlEPTB;Nj6xPFEzQSEQvF2= MoHVV2FPT0WU
NB7 Ml3YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPsdHdKSzVyPU[uNlE{PzNizszN NIjBXpVUSU6JRWK=
H4 NXjkVnNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHvTWM2OD14LkKyOFk{KM7:TR?= NVXWT2hDW0GQR1XS
CAL-72 NGrPcWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlT6TWM2OD14LkS1OFI{KM7:TR?= NV3LTZJMW0GQR1XS
HCC1806 M2\GUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTZwOEG5N|Eh|ryP MWLTRW5ITVJ?
BCPAP NIHSNnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\zdGk{UUN3ME23MlIyPzZ2IN88US=> MlTKV2FPT0WU
LB2241-RCC NW\tfo85T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3:1fGlEPTB;Nz6zOlkxPyEQvF2= MXXTRW5ITVJ?
COLO-741 Mo\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPCcFRNUUN3ME24MlAyPjd7IN88US=> NGjuVGFUSU6JRWK=
HSC-3 NHHxUpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUOyOFNKUUN3ME24MlA4ODZ6IN88US=> NGiyNFdUSU6JRWK=
SW982 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfVTWM2OD16LkSxOVE3KM7:TR?= MV\TRW5ITVJ?
GCT MlXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoWwTWM2OD16Lke1N|E1KM7:TR?= MmHTV2FPT0WU
KY821 Ml3yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWKxN4tEUUN3ME25MlA2OTd6IN88US=> NWX1V29GW0GQR1XS
JVM-3 M3;yRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTlwNU[5PVkh|ryP NFHseHpUSU6JRWK=
RS4-11 NEn3d3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT6RXprUUN3ME25MlYxPDhizszN NIrVWGpUSU6JRWK=
VA-ES-BJ NFmzN4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTFyLkCxOFkh|ryP NGHKT|FUSU6JRWK=
A431 M3jiO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TQbmlEPTB;MUCuOFIyOiEQvF2= MknQV2FPT0WU
LXF-289 MkK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXlTWM2OD1zMD60OVgh|ryP NXvHeXFIW0GQR1XS
SK-MEL-24 M2P3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XBPGlEPTB;MUCuPFI4PCEQvF2= NFTaWnpUSU6JRWK=
NOS-1 M2TxUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH73SGJKSzVyPUGwMlg1PzJizszN MVXTRW5ITVJ?
KNS-62 M4fSSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\xZVZZUUN3ME2xNU4zPDB2IN88US=> MWTTRW5ITVJ?
SK-HEP-1 MoHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PWPGlEPTB;MUGuN|UzPyEQvF2= MoH2V2FPT0WU
A3-KAW NF\xTpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LzSmlEPTB;MUGuO|E4QCEQvF2= NYrh[Yt5W0GQR1XS
SK-LU-1 M1TsOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\RbWlEPTB;MUKuNlY2PSEQvF2= MlLKV2FPT0WU
TYK-nu NXq2U2lKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\3VI9KSzVyPUGyMlM6OzJizszN MX7TRW5ITVJ?
NMC-G1 NGTlN21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2L4SmlEPTB;MUKuOlA3OiEQvF2= M{nv[3NCVkeHUh?=
BB65-RCC Mn3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;sb2lEPTB;MUKuO|E3QSEQvF2= NHTKWpBUSU6JRWK=
QIMR-WIL MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXSeJpvUUN3ME2xNk45QDN|IN88US=> M1S3VnNCVkeHUh?=
D-566MG MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTF|Lkm1O|Yh|ryP NGLoeFlUSU6JRWK=
KYSE-140 M2jrPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDKZ|VVUUN3ME2xOE4xPzV|IN88US=> NYjjSHdOW0GQR1XS
SCC-4 MoW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;NcGlKSzVyPUG0MlM{PTlizszN NFT0ZWlUSU6JRWK=
U251 NV7VOGZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTF2Lki0PVIh|ryP M{XLPHNCVkeHUh?=
D-542MG MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3mfVU5UUN3ME2xOE46OjJ{IN88US=> Mm\YV2FPT0WU
LAMA-84 NFezOZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjFSlQ4UUN3ME2xOE46QTN{IN88US=> Mly4V2FPT0WU
NCI-H720 Mli1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLaR25SUUN3ME2xOU4zPjh2IN88US=> MXTTRW5ITVJ?
DEL MnK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\XO4NKSzVyPUG1MlQzQTNizszN NGq5SoJUSU6JRWK=
SBC-1 NXfGPYpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnjTJJKSzVyPUG1MlQ{ODVizszN NYLtSHpIW0GQR1XS
ECC10 NV\JS5I2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrSRmZKSzVyPUG1MlQ1PThizszN MmHxV2FPT0WU
Daoy NWr2NVN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTF3Lke2NVYh|ryP NWTiNml2W0GQR1XS
SCH M4PsZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTF3Lke4N|Uh|ryP NFLMTZhUSU6JRWK=
MZ2-MEL NWL4bGZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTF4LkC2OFYh|ryP NHTPW29USU6JRWK=
CAL-12T MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTrO3RKSzVyPUG2MlQ5PjJizszN MlPoV2FPT0WU
KE-37 NHnkOHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\MTWM2OD1zNj64NVA4KM7:TR?= NXe2OolvW0GQR1XS
LS-411N MnnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUP6dGxCUUN3ME2xO{4yOThizszN MoWxV2FPT0WU
NCI-H2228 NU\TOodZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTF5LkOwO|Eh|ryP NIm4cWhUSU6JRWK=
SK-MEL-2 M1Hz[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTUTWM2OD1zNz60PVY2KM7:TR?= M3S4dXNCVkeHUh?=
HN NF\MdYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXXTWM2OD1zNz63NlQ5KM7:TR?= NEXKXolUSU6JRWK=
NCI-H1648 NIPiVJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTF5LkixPEDPxE1? NXHFd2JCW0GQR1XS
IA-LM NHHjZ2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTF6LkOxO|Ih|ryP MnnBV2FPT0WU
EW-13 Ml7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLZbpljUUN3ME2xPE42PzB6IN88US=> MUfTRW5ITVJ?
YKG-1 NHP0N|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3nVGNKSzVyPUG5MlU4OTFizszN M4LTWnNCVkeHUh?=
KNS-81-FD NUnLUGF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXqzdXVOUUN3ME2xPU42QDV6IN88US=> NVTZU5ZVW0GQR1XS
23132-87 NFXWblRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHZbpdKSzVyPUG5Mlc3PDJizszN NVrROI4zW0GQR1XS
NUGC-3 M4Lkcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTF7Lkm4PFch|ryP MUDTRW5ITVJ?
5637 M2nmVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\kW4tKSzVyPUKwMlA1PzhizszN M2TvbHNCVkeHUh?=
NCI-H1755 M3\VUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTJyLkS3OlQh|ryP NXOySI9DW0GQR1XS
RH-18 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrKTWM2OD1{MD61O|Q5KM7:TR?= MnPBV2FPT0WU
RXF393 NHXYTpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDTN3BKSzVyPUKwMlY4PTZizszN MYTTRW5ITVJ?
LU-134-A NF;MU4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLJPFhVUUN3ME2yNE44ODV4IN88US=> MWrTRW5ITVJ?
TE-12 M4GyZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NED1OFlKSzVyPUKwMlczODFizszN MWTTRW5ITVJ?
MOLT-4 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DYV2lEPTB;MkGuNVkyPSEQvF2= M4fjRnNCVkeHUh?=
IGR-1 M3zxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTJzLkO3PVYh|ryP MoX6V2FPT0WU
HOP-92 M3LwTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjwT2dKSzVyPUKxMlQ6QDdizszN NHf5N|RUSU6JRWK=
SK-MES-1 NFvtS2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\pRotKSzVyPUKxMlc{QDFizszN M{LaSHNCVkeHUh?=
LU-65 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTZXGlkUUN3ME2yNU45PjJ2IN88US=> NHvKcHpUSU6JRWK=
MS-1 M1njPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYriSJM6UUN3ME2yNk4yOjB|IN88US=> NY\VWY82W0GQR1XS
LoVo MnT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPKTHF3UUN3ME2yNk4zPDRizszN NYDNVYd4W0GQR1XS
A704 MnXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTJ{LkWxOVUh|ryP Mn;KV2FPT0WU
HT-1376 M{Lpcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTJ{Lk[wOVkh|ryP NHPHcYNUSU6JRWK=
IST-MEL1 M{PL[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\xOphDUUN3ME2yNk43PzVzIN88US=> NEnyWYtUSU6JRWK=
Ramos-2G6-4C10 MmPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTJ{LkezOlYh|ryP NVrubGE6W0GQR1XS
T47D NEKwS4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTJ{Lke5O|kh|ryP NEDGTZZUSU6JRWK=
HT-1197 M3LLUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXuTWM2OD1{Mz6wPFE4KM7:TR?= NVyyTIVWW0GQR1XS
LB2518-MEL NVXSXJV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTJ|Lk[0NVIh|ryP NXv1OXdXW0GQR1XS
J-RT3-T3-5 Mmf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkmwTWM2OD1{ND63OVk2KM7:TR?= MYnTRW5ITVJ?
SK-NEP-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJ2Lki3OFQh|ryP MWDTRW5ITVJ?
NCI-H526 NYnyXY1RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvGTWM2OD1{NT6wNFI{KM7:TR?= MX7TRW5ITVJ?
IST-SL1 MoPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHDdY1GUUN3ME2yOU4zPzVzIN88US=> NVjSWZBUW0GQR1XS
HH M1PrbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTJ3LkOxPVIh|ryP M4fIOHNCVkeHUh?=
NCI-H82 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTJ3LkmzPEDPxE1? MYDTRW5ITVJ?
SNU-449 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXKZlZoUUN3ME2yO{4zODF6IN88US=> MUnTRW5ITVJ?
COR-L23 M4S2N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nHU2lEPTB;MkeuNlgyOyEQvF2= NVvvRXo2W0GQR1XS
LOXIMVI NYfmcmR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfDPZJKSzVyPUK3MlM3QCEQvF2= NELJXFZUSU6JRWK=
GR-ST M4rsc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTJ5Lk[3NFYh|ryP NVvyRmdbW0GQR1XS
NCI-SNU-1 NVXxb4FpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13xc2lEPTB;MkeuPVQ1KM7:TR?= M{PFbHNCVkeHUh?=
ALL-PO M{\nTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmD4TWM2OD1{OD6xOlA1KM7:TR?= NF\YeFRUSU6JRWK=
ML-2 M4WwN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGntSYFKSzVyPUK4MlI5OTRizszN NEHvW4RUSU6JRWK=
HOP-62 NHjVUJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrNdGtKSzVyPUK4MlcyOyEQvF2= MUDTRW5ITVJ?
EGI-1 NX\5NmU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHm5V45KSzVyPUK4Mlg5PDVizszN MmLGV2FPT0WU
TCCSUP NUW3eWQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\MSWlEPTB;MkiuPVI4OiEQvF2= MY\TRW5ITVJ?
LB996-RCC NHXYc3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fIS2lEPTB;MkmuOVY5OiEQvF2= NW\FfHB{W0GQR1XS
LCLC-97TM1 MmXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\mNFR5UUN3ME2zNk4yQTZ2IN88US=> NF31cVlUSU6JRWK=
NCI-H1304 M17TdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPkRo9KSzVyPUOyMlM{ODFizszN NUi3ZWxNW0GQR1XS
KP-N-YS MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2S1cmlEPTB;M{KuOVk4OyEQvF2= NEXXVFFUSU6JRWK=
NCI-H1770 NU\EfINTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{f4cmlEPTB;M{OuNVY1QCEQvF2= MXjTRW5ITVJ?
EM-2 M1GzWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfUTWM2OD1|Mz62OVA1KM7:TR?= M3nrO3NCVkeHUh?=
ChaGo-K-1 M2O4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;VU4ZXUUN3ME2zN{44OjN4IN88US=> MoX5V2FPT0WU
ACHN NFzXVGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LqS2lEPTB;M{OuPFM5PSEQvF2= NEDTfIZUSU6JRWK=
MN-60 NEjnN|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH[zW|FKSzVyPUOzMlg2PDRizszN MmLSV2FPT0WU
EW-18 NEjzdZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4X2e2lEPTB;M{OuPFk4OSEQvF2= Mor5V2FPT0WU
KGN NI\jbVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPoNllKSzVyPUO1MlczQTJizszN MWjTRW5ITVJ?
U031 Mn[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LSWmlEPTB;M{WuPFE{OiEQvF2= NVjOZ4VrW0GQR1XS
HMV-II NHS5UIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofwTWM2OD1|Nj6wO|c1KM7:TR?= Mlm0V2FPT0WU
L-363 M{W3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrOTWM2OD1|Nz62OFU2KM7:TR?= M1rmOnNCVkeHUh?=
NCI-H1155 M3nKXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvhN4Z7UUN3ME2zPE4xODF3IN88US=> NXXJbo95W0GQR1XS
NCI-H1793 M3\icmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFWwT|VKSzVyPUO4MlExOjZizszN MYjTRW5ITVJ?
P30-OHK M2nIdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzyXGhKSzVyPUO4MlE{OzJizszN MnLXV2FPT0WU
AN3-CA NG[4cVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPxTWM2OD1|OD6xOlE2KM7:TR?= Mk\SV2FPT0WU
UACC-257 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zsXWlEPTB;M{iuO|kh|ryP NV6wW5FSW0GQR1XS
MCF7 NX33[pg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHlTWM2OD1|OT64OlI6KM7:TR?= NXvSZm1HW0GQR1XS
KP-N-YN MmH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTRyLkSyPFUh|ryP Mn\CV2FPT0WU
T98G NHPvbY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjnTmIyUUN3ME20NE41QTV5IN88US=> MlHPV2FPT0WU
HGC-27 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTR|LkK3OEDPxE1? NXjzR4lTW0GQR1XS
NCI-H1092 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPFNmVKSzVyPUSzMlI5QTVizszN M3\RdHNCVkeHUh?=
KARPAS-299 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1:wcGlEPTB;NEOuN|A4OSEQvF2= NH\CNoxUSU6JRWK=
LB1047-RCC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTR2Lkm5OVkh|ryP MVfTRW5ITVJ?
786-0 NGP0TFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFSyUopKSzVyPUS1MlY2KM7:TR?= NHfXO3FUSU6JRWK=
HCC2157 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTR4LkCzOVkh|ryP NVjad2RJW0GQR1XS
NY NYHWXY9zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfRRlJmUUN3ME20Ok4yPzd6IN88US=> MX\TRW5ITVJ?
EFM-19 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVj6e3VVUUN3ME20Ok44PTN|IN88US=> MXPTRW5ITVJ?
EW-16 NXTmSII2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjmT5lrUUN3ME20Ok44QDB4IN88US=> Ml3MV2FPT0WU
UM-UC-3 M2jONmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFK0Z4RKSzVyPUS2MlgxPTlizszN MlPVV2FPT0WU
HT-29 MlfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzkNINDUUN3ME20O{45Pzl{IN88US=> MV7TRW5ITVJ?
LN-405 M{jjOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XpdmlEPTB;NEiuNFgzPyEQvF2= MljDV2FPT0WU
NCI-H727 M4fvW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnz6TWM2OD12OD63O|I3KM7:TR?= M{jkdXNCVkeHUh?=
D-502MG NEezTFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUT1NmpSUUN3ME20PE46Pjd4IN88US=> NWPzZolDW0GQR1XS
GMS-10 NVuxZpFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[1TWM2OD12OT6yPVc1KM7:TR?= MkPvV2FPT0WU
MEL-JUSO NV3BUYxnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;vTWM2OD12OT6zOFch|ryP MkWyV2FPT0WU

... 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
  • Formulation: 悬浮于5% DMSO, 1% 甲基纤维素中
  • 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

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