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130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 M{nWU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTBwMEe0OVch|ryP NV\ScmR[W0GQR1XS
EoL-1-cell NFnrd2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPaTWM2OD1yLkG0NVY3KM7:TR?= MVTTRW5ITVJ?
C32 M3n6bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXZWVdKSzVyPUCuNVUyOzFizszN MofBV2FPT0WU
M14 NHHpbY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDuSmFKSzVyPUCuNlE4PTdizszN NWXO[4R6W0GQR1XS
CP50-MEL-B MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnTTWM2OD1yLkK5O|g1KM7:TR?= NFHoW|FUSU6JRWK=
A101D NYLqVIJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfESnhIUUN3ME2wMlMzPTh7IN88US=> NVLDTHg4W0GQR1XS
G-361 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTBwM{S2N|ch|ryP NY\tfm5JW0GQR1XS
HT-144 NYD5ZVVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlG0TWM2OD1yLkO2N|I6KM7:TR?= NFjKOohUSU6JRWK=
ACN NWDtU|E5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3GWnFKSzVyPUCuN|g1PzdizszN MX\TRW5ITVJ?
COLO-829 NYjvOok{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHtTWM2OD1yLkO4PVY5KM7:TR?= NEWx[JJUSU6JRWK=
MEL-HO MnvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkT3TWM2OD1yLkSxNVc6KM7:TR?= NUH5[YJbW0GQR1XS
SH-4 MkPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTBwNEG0NlIh|ryP NXG4OIh1W0GQR1XS
SK-MEL-3 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlG2TWM2OD1yLkWxOVY5KM7:TR?= M3zCUnNCVkeHUh?=
A375 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DZOWlEPTB;MD62O|M2QSEQvF2= NGnIW4pUSU6JRWK=
MMAC-SF M1jveGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1G5WGlEPTB;MD62PFYyPCEQvF2= M3vMd3NCVkeHUh?=
BHT-101 NGLadHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrZTWM2OD1yLkewO|AzKM7:TR?= M2nOdXNCVkeHUh?=
K5 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7FPZlOUUN3ME2wMlc3OTR6IN88US=> NHjIfJBUSU6JRWK=
BV-173 NF3zb|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXJTWM2OD1yLke5OlQ1KM7:TR?= MUPTRW5ITVJ?
RVH-421 M3nBXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XNe2lEPTB;MD64Olc6PiEQvF2= MUXTRW5ITVJ?
HCC2218 NWDMZYxkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnqzTWM2OD1yLki3PFQ1KM7:TR?= NWf4TohtW0GQR1XS
WM-115 M4fFXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnyTWM2OD1yLki4OlkzKM7:TR?= MkHCV2FPT0WU
SK-MEL-28 M37N[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mle4TWM2OD1zLkC0OVY6KM7:TR?= NVriSYdJW0GQR1XS
COLO-679 MlX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPjTWM2OD1zLkGwOFY1KM7:TR?= MlOyV2FPT0WU
MZ7-mel Ml3FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTFwMUS5OlMh|ryP M4joPHNCVkeHUh?=
SK-MEL-30 NUTZW|dDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[zTWM2OD1zLkOzN|g3KM7:TR?= MXfTRW5ITVJ?
NCI-H209 MnrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEKzTItKSzVyPUGuOlA5PiEQvF2= NXzS[ItqW0GQR1XS
HTC-C3 NIj4PYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmW2TWM2OD1zLk[2Nlk1KM7:TR?= M2TTXHNCVkeHUh?=
KARPAS-45 M{C1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXNTWM2OD1{LkC0PVc5KM7:TR?= NFfVc3dUSU6JRWK=
NCI-SNU-5 M2S5cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknUTWM2OD1{LkGxPVY6KM7:TR?= NXH5RWU{W0GQR1XS
KP-4 MlG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHhVY5KSzVyPUKuN|A4QDdizszN M1rHW3NCVkeHUh?=
PA-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLwTWM2OD1{LkeyOlc{KM7:TR?= MkLHV2FPT0WU
HuO-3N1 NIDDO|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTJwOEe5OFYh|ryP NVvCWm94W0GQR1XS
NCI-H358 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnWwTWM2OD1{LkmyNlMzKM7:TR?= NX;BbJRtW0GQR1XS
CTB-1 NUPCenN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3NTWM2OD1|LkSwNVc3KM7:TR?= M4rhbHNCVkeHUh?=
697 M2TQXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;zR3NVUUN3ME2zMlU2OjZ4IN88US=> M2X1RnNCVkeHUh?=
CP66-MEL MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHi5b21KSzVyPUSuNVU6OjdizszN MUDTRW5ITVJ?
NB13 NYHrR2Y1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;uT2lEPTB;ND60PVE4QSEQvF2= NV;DR2p1W0GQR1XS
DBTRG-05MG M2TBU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7CTWM2OD12LkWzN|I2KM7:TR?= MVTTRW5ITVJ?
A2058 MljLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXkTWM2OD12LkeyNVY1KM7:TR?= NWG0cnpXW0GQR1XS
KG-1 NV\VcZNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33veWlEPTB;ND63N|kxQCEQvF2= NELTcodUSU6JRWK=
8305C NUnKO2VxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPPWFJKSzVyPUWuNVg4OyEQvF2= M3T3[XNCVkeHUh?=
RPMI-7951 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTsVpVKSzVyPUWuPFAzQDNizszN NYTMfWpkW0GQR1XS
CHL-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTVwOUe2NFMh|ryP M2DkWXNCVkeHUh?=
TI-73 Mkf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vv[2lEPTB;Nj6wNFkxOiEQvF2= NFG4SZdUSU6JRWK=
HT-1080 MkjRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HIXmlEPTB;Nj6xNFk1PiEQvF2= NHvl[GVUSU6JRWK=
ES5 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTZwMUS5NlQh|ryP NE\FUI9USU6JRWK=
8-MG-BA NIfaXJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTZwMUixNlkh|ryP MoXYV2FPT0WU
NB7 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\DVHJKSzVyPU[uNlE{PzNizszN M1LVTXNCVkeHUh?=
H4 NGfhNYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfQWWVKSzVyPU[uNlI1QTNizszN M3fydXNCVkeHUh?=
CAL-72 MnPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLJTWM2OD14LkS1OFI{KM7:TR?= M3TlU3NCVkeHUh?=
HCC1806 NV\lcpRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHOTWM2OD14LkixPVMyKM7:TR?= NFTWVXpUSU6JRWK=
BCPAP Mne1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTdwMkG3OlQh|ryP NUjXNIFWW0GQR1XS
LB2241-RCC MlPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjWTpJlUUN3ME23MlM3QTB5IN88US=> M1vLRXNCVkeHUh?=
COLO-741 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3L0O2lEPTB;OD6wNVY4QSEQvF2= MVPTRW5ITVJ?
HSC-3 MljGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHryfVFKSzVyPUiuNFcxPjhizszN NGrJ[IhUSU6JRWK=
SW982 MnvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRThwNEG1NVYh|ryP M3jGUXNCVkeHUh?=
GCT NIewXFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHOO|VMUUN3ME24Mlc2OzF2IN88US=> MYTTRW5ITVJ?
KY821 M3f0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTlwMEWxO|gh|ryP MkXMV2FPT0WU
JVM-3 NXXab|N3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITHemhKSzVyPUmuOVY6QTlizszN MoXzV2FPT0WU
RS4-11 Ml3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTlwNkC0PEDPxE1? M4TEfnNCVkeHUh?=
VA-ES-BJ MoD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TENWlEPTB;MUCuNFE1QSEQvF2= NYP3cWNJW0GQR1XS
A431 Mlq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlG2TWM2OD1zMD60NlEzKM7:TR?= Mnn3V2FPT0WU
LXF-289 NHXLRYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3Deo9PUUN3ME2xNE41PThizszN NX7DZ4lQW0GQR1XS
SK-MEL-24 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXWTWM2OD1zMD64Nlc1KM7:TR?= NVXDNVhXW0GQR1XS
NOS-1 NWjGZ2hbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjVTWM2OD1zMD64OFczKM7:TR?= NGnDVohUSU6JRWK=
KNS-62 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXDTWM2OD1zMT6yOFA1KM7:TR?= NFzOfGtUSU6JRWK=
SK-HEP-1 NWqxSnpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPMSWE{UUN3ME2xNU4{PTJ5IN88US=> NUXhVI57W0GQR1XS
A3-KAW NIjTXnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjxTWM2OD1zMT63NVc5KM7:TR?= NVPWN4RSW0GQR1XS
SK-LU-1 MoLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4m3O2lEPTB;MUKuNlY2PSEQvF2= NHyyNJRUSU6JRWK=
TYK-nu MnzTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fBXGlEPTB;MUKuN|k{OiEQvF2= MmH4V2FPT0WU
NMC-G1 M2S4WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTF{Lk[wOlIh|ryP NVXnSpk6W0GQR1XS
BB65-RCC MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTF{LkexOlkh|ryP NIS2PI9USU6JRWK=
QIMR-WIL MnXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLvTWM2OD1zMj64PFM{KM7:TR?= NFTvcoZUSU6JRWK=
D-566MG NXX6NIs6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWGwcFJNUUN3ME2xN{46PTd4IN88US=> NX7HeoFbW0GQR1XS
KYSE-140 NYm2UHNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFSwVJVKSzVyPUG0MlA4PTNizszN NGO2foFUSU6JRWK=
SCC-4 NWTVSG9rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzpPIJKSzVyPUG0MlM{PTlizszN NWjONnZ[W0GQR1XS
U251 MlTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXG5TItEUUN3ME2xOE45PDl{IN88US=> NILVUIVUSU6JRWK=
D-542MG NWXtW2ZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjMc5BKSzVyPUG0MlkzOjJizszN NGqzPGhUSU6JRWK=
LAMA-84 NFnMPFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDvU295UUN3ME2xOE46QTN{IN88US=> MlfuV2FPT0WU
NCI-H720 NUC3Zmw4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTF3LkK2PFQh|ryP NIftb49USU6JRWK=
DEL NHfuSZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFL5[YRKSzVyPUG1MlQzQTNizszN NVXtOYJYW0GQR1XS
SBC-1 NILtZotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LtRWlEPTB;MUWuOFMxPSEQvF2= MmL4V2FPT0WU
ECC10 NHXDbIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoCxTWM2OD1zNT60OFU5KM7:TR?= MV\TRW5ITVJ?
Daoy M4DGbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzKeG5uUUN3ME2xOU44PjF4IN88US=> MoHxV2FPT0WU
SCH MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HKVWlEPTB;MUWuO|g{PSEQvF2= MkDiV2FPT0WU
MZ2-MEL M3LqU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzOOFVKSzVyPUG2MlA3PDZizszN M{DNOnNCVkeHUh?=
CAL-12T NFXHUI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDnN5VKSzVyPUG2MlQ5PjJizszN M2fMOnNCVkeHUh?=
KE-37 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;xbJRKSzVyPUG2MlgyODdizszN M{PMXHNCVkeHUh?=
LS-411N NW\ndXc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vmN2lEPTB;MUeuNVE5KM7:TR?= MnfoV2FPT0WU
NCI-H2228 NHLLU|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\Zd4hKSzVyPUG3MlMxPzFizszN NVG5VXFrW0GQR1XS
SK-MEL-2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWH2[VAyUUN3ME2xO{41QTZ3IN88US=> MWDTRW5ITVJ?
HN NF3nbJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLmPG9zUUN3ME2xO{44OjR6IN88US=> MU\TRW5ITVJ?
NCI-H1648 Mnn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTF5LkixPEDPxE1? NF7QRXhUSU6JRWK=
IA-LM MkewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nZdmlEPTB;MUiuN|E4OiEQvF2= Mn7mV2FPT0WU
EW-13 NHL5[odIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zTSmlEPTB;MUiuOVcxQCEQvF2= NXzETFk5W0GQR1XS
YKG-1 M3;Rbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYroPXpEUUN3ME2xPU42PzFzIN88US=> MlL3V2FPT0WU
KNS-81-FD NFrEfpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\hTWM2OD1zOT61PFU5KM7:TR?= MVHTRW5ITVJ?
23132-87 M2HBbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjq[IdKSzVyPUG5Mlc3PDJizszN Ml[2V2FPT0WU
NUGC-3 MoLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4f2XWlEPTB;MUmuPVg5PyEQvF2= MVzTRW5ITVJ?
5637 MkXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTJyLkC0O|gh|ryP Mmq1V2FPT0WU
NCI-H1755 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLiTWM2OD1{MD60O|Y1KM7:TR?= NHu4SmVUSU6JRWK=
RH-18 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF62WpdKSzVyPUKwMlU4PDhizszN M1jTVXNCVkeHUh?=
RXF393 Mn3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTJyLk[3OVYh|ryP NWKxWIZpW0GQR1XS
LU-134-A Mn7GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTKSFVKSzVyPUKwMlcxPTZizszN NH\oe|FUSU6JRWK=
TE-12 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnITWM2OD1{MD63NlAyKM7:TR?= MoTLV2FPT0WU
MOLT-4 M163UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTH[ZlPUUN3ME2yNU4yQTF3IN88US=> NFrTR5RUSU6JRWK=
IGR-1 NGSwcWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTJzLkO3PVYh|ryP MUnTRW5ITVJ?
HOP-92 MmjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEm4WmpKSzVyPUKxMlQ6QDdizszN NU\nO2tpW0GQR1XS
SK-MES-1 NYf0fG5bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLMe4NNUUN3ME2yNU44OzhzIN88US=> M3;sZ3NCVkeHUh?=
LU-65 M2LUemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrBXFJ4UUN3ME2yNU45PjJ2IN88US=> NH\BfphUSU6JRWK=
MS-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrTfJBKSzVyPUKyMlEzODNizszN NF\Nc2pUSU6JRWK=
LoVo M2[xbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\MOWt7UUN3ME2yNk4zPDRizszN NVjCXZNtW0GQR1XS
A704 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYS2UVJoUUN3ME2yNk42OTV3IN88US=> NVH3OIUzW0GQR1XS
HT-1376 M1HQOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPkTWM2OD1{Mj62NFU6KM7:TR?= M1S4OHNCVkeHUh?=
IST-MEL1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXHNJI1UUN3ME2yNk43PzVzIN88US=> MXnTRW5ITVJ?
Ramos-2G6-4C10 MkjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHv3S2lKSzVyPUKyMlc{PjZizszN MX7TRW5ITVJ?
T47D M3izN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjMdXdKSzVyPUKyMlc6PzlizszN MYjTRW5ITVJ?
HT-1197 NFXyUXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfPN|RKSzVyPUKzMlA5OTdizszN NEjyNJhUSU6JRWK=
LB2518-MEL M1HSR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHqTWM2OD1{Mz62OFEzKM7:TR?= NULifldpW0GQR1XS
J-RT3-T3-5 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3qyWGlEPTB;MkSuO|U6PSEQvF2= NUTrXVNMW0GQR1XS
SK-NEP-1 Mle5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTJ2Lki3OFQh|ryP M2f4bnNCVkeHUh?=
NCI-H526 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\ZcW5KSzVyPUK1MlAxOjNizszN NI\LbpdUSU6JRWK=
IST-SL1 M4m2[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmf6TWM2OD1{NT6yO|UyKM7:TR?= MnHjV2FPT0WU
HH MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1uydWlEPTB;MkWuN|E6OiEQvF2= M13iTXNCVkeHUh?=
NCI-H82 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIq2b21KSzVyPUK1Mlk{QCEQvF2= M2rEPHNCVkeHUh?=
SNU-449 NILlPYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoL1TWM2OD1{Nz6yNFE5KM7:TR?= M2LqTnNCVkeHUh?=
COR-L23 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofSTWM2OD1{Nz6yPFE{KM7:TR?= MULTRW5ITVJ?
LOXIMVI MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7YZ4NKSzVyPUK3MlM3QCEQvF2= Mk\UV2FPT0WU
GR-ST NILHdnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYH4WFRDUUN3ME2yO{43PzB4IN88US=> NUTRfVl1W0GQR1XS
NCI-SNU-1 Mn;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTJ5Lkm0OEDPxE1? M36zOnNCVkeHUh?=
ALL-PO M17NWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVywWVFFUUN3ME2yPE4yPjB2IN88US=> MnjnV2FPT0WU
ML-2 NU\GcoplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDCTWM2OD1{OD6yPFE1KM7:TR?= NXn4[3p{W0GQR1XS
HOP-62 M1LCcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPQVVZKSzVyPUK4MlcyOyEQvF2= NIKzV2ZUSU6JRWK=
EGI-1 M1Gzc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnqdVFKSzVyPUK4Mlg5PDVizszN MYDTRW5ITVJ?
TCCSUP MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFS0[oZKSzVyPUK4MlkzPzJizszN MXHTRW5ITVJ?
LB996-RCC M1G2[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fOe2lEPTB;MkmuOVY5OiEQvF2= NGXyS4tUSU6JRWK=
LCLC-97TM1 MkLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD4XHZ4UUN3ME2zNk4yQTZ2IN88US=> NYX3TmtxW0GQR1XS
NCI-H1304 M2LpfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrrTXA1UUN3ME2zNk4{OzBzIN88US=> MXPTRW5ITVJ?
KP-N-YS M1;qOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fwS2lEPTB;M{KuOVk4OyEQvF2= M1HLNnNCVkeHUh?=
NCI-H1770 NVf1XYpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37UfmlEPTB;M{OuNVY1QCEQvF2= MVHTRW5ITVJ?
EM-2 M325[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4j6O2lEPTB;M{OuOlUxPCEQvF2= NXTJVo56W0GQR1XS
ChaGo-K-1 NW\U[5ZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX:x[3ZHUUN3ME2zN{44OjN4IN88US=> NXnQOJJSW0GQR1XS
ACHN MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnn2TWM2OD1|Mz64N|g2KM7:TR?= NXP0R4lrW0GQR1XS
MN-60 M1PKTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjPTWM2OD1|Mz64OVQ1KM7:TR?= NYrrOZNqW0GQR1XS
EW-18 NYHEZolWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfOSGg6UUN3ME2zN{45QTdzIN88US=> Mon4V2FPT0WU
KGN NFG3TphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTN3LkeyPVIh|ryP NVnaT4pLW0GQR1XS
U031 M2nnc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zxdGlEPTB;M{WuPFE{OiEQvF2= M3zXWXNCVkeHUh?=
HMV-II NHjsU|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkD6TWM2OD1|Nj6wO|c1KM7:TR?= MkLQV2FPT0WU
L-363 M2KzPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jBcGlEPTB;M{euOlQ2PSEQvF2= NGnZbWJUSU6JRWK=
NCI-H1155 NXnnSHdKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\RcWlEPTB;M{iuNFAyPSEQvF2= MV3TRW5ITVJ?
NCI-H1793 NF3LU2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TZcGlEPTB;M{iuNVAzPiEQvF2= MoPCV2FPT0WU
P30-OHK M1LsS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLnPI1KSzVyPUO4MlE{OzJizszN MWfTRW5ITVJ?
AN3-CA Mm\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrw[ppCUUN3ME2zPE4yPjF3IN88US=> MV3TRW5ITVJ?
UACC-257 NILGSHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjJdY5YUUN3ME2zPE44QSEQvF2= MlTvV2FPT0WU
MCF7 NGTZRY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjsd|JKSzVyPUO5Mlg3OjlizszN MUPTRW5ITVJ?
KP-N-YN MkPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zpSGlEPTB;NECuOFI5PSEQvF2= NYfZSmtDW0GQR1XS
T98G MnrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrRRWNKSzVyPUSwMlQ6PTdizszN NXHWZlRPW0GQR1XS
HGC-27 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\JbGI6UUN3ME20N{4zPzRizszN NHToXJBUSU6JRWK=
NCI-H1092 MlfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTUfGE5UUN3ME20N{4zQDl3IN88US=> MlXlV2FPT0WU
KARPAS-299 NHjTfm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofaTWM2OD12Mz6zNFcyKM7:TR?= NXLIOopDW0GQR1XS
LB1047-RCC MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\iWGlEPTB;NESuPVk2QSEQvF2= NWPiO|lQW0GQR1XS
786-0 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUO4ZmRuUUN3ME20OU43PSEQvF2= M1jJbXNCVkeHUh?=
HCC2157 NIH3dmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVP5ZYJ[UUN3ME20Ok4xOzV7IN88US=> NVW2b|AyW0GQR1XS
NY NXv3NmhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M333XGlEPTB;NE[uNVc4QCEQvF2= M1Lx[HNCVkeHUh?=
EFM-19 NY[2RY1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2D5Z2lEPTB;NE[uO|U{OyEQvF2= MkHlV2FPT0WU
EW-16 Mon5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LBRmlEPTB;NE[uO|gxPiEQvF2= NYXrV|dyW0GQR1XS
UM-UC-3 M1\ROWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTR4LkiwOVkh|ryP NFrkSHhUSU6JRWK=
HT-29 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\DVo9KSzVyPUS3Mlg4QTJizszN MlPiV2FPT0WU
LN-405 NFH3WpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTR6LkC4Nlch|ryP NVq0VWh[W0GQR1XS
NCI-H727 Mn\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLL[I9KSzVyPUS4Mlc4OjZizszN Ml30V2FPT0WU
D-502MG M3HMXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;wUphKSzVyPUS4Mlk3PzZizszN NXi4cYJ4W0GQR1XS
GMS-10 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7qeoJKSzVyPUS5MlI6PzRizszN M3H2[3NCVkeHUh?=
MEL-JUSO NHv3eWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPHTWM2OD12OT6zOFch|ryP M1fufXNCVkeHUh?=

... 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

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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.

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID