PLX-4720

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  
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该产品发表文献49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 M1nTWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\LbGlEPTB;MD6wO|Q2PyEQvF2= NEC1XWhUSU6JRWK=
EoL-1-cell NWTx[mJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLXTWM2OD1yLkG0NVY3KM7:TR?= M2L0c3NCVkeHUh?=
C32 NHrYVnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\Qe|ZQUUN3ME2wMlE2OTNzIN88US=> MYDTRW5ITVJ?
M14 NIDPbI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPmTWM2OD1yLkKxO|U4KM7:TR?= NH\hSXlUSU6JRWK=
CP50-MEL-B MofkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIntUHJKSzVyPUCuNlk4QDRizszN MkX3V2FPT0WU
A101D M3zWfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwM{K1PFkh|ryP NITjfVhUSU6JRWK=
G-361 NHHWTZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHu2e2dKSzVyPUCuN|Q3OzdizszN M320OHNCVkeHUh?=
HT-144 NX;0W3F6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[1[pBZUUN3ME2wMlM3OzJ7IN88US=> NGLWclhUSU6JRWK=
ACN Mk\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHr6NVlKSzVyPUCuN|g1PzdizszN MXnTRW5ITVJ?
COLO-829 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7ZUJgyUUN3ME2wMlM5QTZ6IN88US=> MYPTRW5ITVJ?
MEL-HO M3TpXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoT3TWM2OD1yLkSxNVc6KM7:TR?= M{e4ZnNCVkeHUh?=
SH-4 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH[zdmJKSzVyPUCuOFE1OjJizszN NUjuSXI3W0GQR1XS
SK-MEL-3 NX7RO2tCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M360PWlEPTB;MD61NVU3QCEQvF2= M2PpVnNCVkeHUh?=
A375 M2T0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIf5OI5KSzVyPUCuOlc{PTlizszN MVTTRW5ITVJ?
MMAC-SF MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DKfmlEPTB;MD62PFYyPCEQvF2= MVXTRW5ITVJ?
BHT-101 MlK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHn5bIRKSzVyPUCuO|A4ODJizszN NH[xeHNUSU6JRWK=
K5 NVq1eopIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XGZWlEPTB;MD63OlE1QCEQvF2= MUDTRW5ITVJ?
BV-173 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTBwN{m2OFQh|ryP NUSwPY1DW0GQR1XS
RVH-421 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULWS5R2UUN3ME2wMlg3Pzl4IN88US=> NV\PXGszW0GQR1XS
HCC2218 NYXDN4JjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLnTWM2OD1yLki3PFQ1KM7:TR?= M1v1PXNCVkeHUh?=
WM-115 NIjpOHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7PcJZ2UUN3ME2wMlg5Pjl{IN88US=> NX76[VVGW0GQR1XS
SK-MEL-28 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\4R2lEPTB;MT6wOFU3QSEQvF2= MULTRW5ITVJ?
COLO-679 NXvpNIY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlGxTWM2OD1zLkGwOFY1KM7:TR?= MVPTRW5ITVJ?
MZ7-mel NVXzc5dQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWraV|hDUUN3ME2xMlE1QTZ|IN88US=> M4jOZ3NCVkeHUh?=
SK-MEL-30 M3nXOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfHTZI{UUN3ME2xMlM{Ozh4IN88US=> MorhV2FPT0WU
NCI-H209 Ml7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzlTWM2OD1zLk[wPFYh|ryP NYf4S4V3W0GQR1XS
HTC-C3 NYfEZYpHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfMVmFoUUN3ME2xMlY3Ojl2IN88US=> MVTTRW5ITVJ?
KARPAS-45 NUn0ZYNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTJwMES5O|gh|ryP MXnTRW5ITVJ?
NCI-SNU-5 M1OwcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTJwMUG5Olkh|ryP MYPTRW5ITVJ?
KP-4 NXjMUlh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULWOJZTUUN3ME2yMlMxPzh5IN88US=> MojvV2FPT0WU
PA-1 NYfQUlhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTJwN{K2O|Mh|ryP NXfXVVRsW0GQR1XS
HuO-3N1 NH3temNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTJwOEe5OFYh|ryP MU\TRW5ITVJ?
NCI-H358 M4XIOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWq5bnlIUUN3ME2yMlkzOjN{IN88US=> M1\KeXNCVkeHUh?=
CTB-1 M3ntTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjxTHpKSzVyPUOuOFAyPzZizszN NE[3SHNUSU6JRWK=
697 M4rQcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTNwNUWyOlYh|ryP MUDTRW5ITVJ?
CP66-MEL NVz2S3BMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXJfYFMUUN3ME20MlE2QTJ5IN88US=> NWjuTXdUW0GQR1XS
NB13 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3hSoVKSzVyPUSuOFkyPzlizszN MUfTRW5ITVJ?
DBTRG-05MG MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2q1XmlEPTB;ND61N|MzPSEQvF2= NVLwSI46W0GQR1XS
A2058 Mlj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLuN|hRUUN3ME20MlczOTZ2IN88US=> MlGzV2FPT0WU
KG-1 MlGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTRwN{O5NFgh|ryP MVPTRW5ITVJ?
8305C MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rENmlEPTB;NT6xPFc{KM7:TR?= MlfVV2FPT0WU
RPMI-7951 M3q0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVuy[GpDUUN3ME21MlgxOjh|IN88US=> NH3IUYVUSU6JRWK=
CHL-1 NGPhVopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTVwOUe2NFMh|ryP NETyVY5USU6JRWK=
TI-73 NXLEcoRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3hTWM2OD14LkCwPVAzKM7:TR?= NEf2PGFUSU6JRWK=
HT-1080 NEDPdolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nXcmlEPTB;Nj6xNFk1PiEQvF2= NXTHRlA2W0GQR1XS
ES5 NHjMTJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfIRWlKSzVyPU[uNVQ6OjRizszN NX3abWs{W0GQR1XS
8-MG-BA MnfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTZwMUixNlkh|ryP MXPTRW5ITVJ?
NB7 NFf6PFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HYeGlEPTB;Nj6yNVM4OyEQvF2= NFHHcZhUSU6JRWK=
H4 M1vwdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTZwMkK0PVMh|ryP M{D6dHNCVkeHUh?=
CAL-72 NUDZXnZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn:2TWM2OD14LkS1OFI{KM7:TR?= NGfZTFVUSU6JRWK=
HCC1806 MoDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnuTWM2OD14LkixPVMyKM7:TR?= M4Dhc3NCVkeHUh?=
BCPAP NHXaR3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfJTWM2OD15LkKxO|Y1KM7:TR?= MlHlV2FPT0WU
LB2241-RCC MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYe3W2VEUUN3ME23MlM3QTB5IN88US=> NVK1TWZ3W0GQR1XS
COLO-741 NFXzRW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfJR4pKSzVyPUiuNFE3PzlizszN NVjNXVlGW0GQR1XS
HSC-3 NW\peGVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFG2ZpdKSzVyPUiuNFcxPjhizszN NF7DUVlUSU6JRWK=
SW982 NGrnZ3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRThwNEG1NVYh|ryP M2rYVXNCVkeHUh?=
GCT NUPDZVZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRThwN{WzNVQh|ryP NEm2XpRUSU6JRWK=
KY821 NELHSWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PROGlEPTB;OT6wOVE4QCEQvF2= NUnyPVV6W0GQR1XS
JVM-3 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXkTWM2OD17LkW2PVk6KM7:TR?= MnTnV2FPT0WU
RS4-11 NX;KWGJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7sTWM2OD17Lk[wOFgh|ryP NG\CXGdUSU6JRWK=
VA-ES-BJ NYTrTJFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTFyLkCxOFkh|ryP NE\LOXBUSU6JRWK=
A431 NWP3bYROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkWzTWM2OD1zMD60NlEzKM7:TR?= NXLXXXRoW0GQR1XS
LXF-289 NUTZO3hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTFyLkS1PEDPxE1? MX7TRW5ITVJ?
SK-MEL-24 M{i4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvuSpFKSzVyPUGwMlgzPzRizszN M3PNdnNCVkeHUh?=
NOS-1 NXXXVXdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnDclg5UUN3ME2xNE45PDd{IN88US=> NIfMSmdUSU6JRWK=
KNS-62 NUTiUo1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTFzLkK0NFQh|ryP MXjTRW5ITVJ?
SK-HEP-1 NU\jR|VmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nPUGlEPTB;MUGuN|UzPyEQvF2= Mn:wV2FPT0WU
A3-KAW MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4WzZ2lEPTB;MUGuO|E4QCEQvF2= MmLMV2FPT0WU
SK-LU-1 M4XWPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYW5O4F{UUN3ME2xNk4zPjV3IN88US=> MnzPV2FPT0WU
TYK-nu MmXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\rUmlEPTB;MUKuN|k{OiEQvF2= MnHpV2FPT0WU
NMC-G1 NVjGSZNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPjTWM2OD1zMj62NFYzKM7:TR?= MXHTRW5ITVJ?
BB65-RCC MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXqV3dWUUN3ME2xNk44OTZ7IN88US=> NHLWTFZUSU6JRWK=
QIMR-WIL NUXC[GtpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rCfGlEPTB;MUKuPFg{OyEQvF2= NIfaXGlUSU6JRWK=
D-566MG MoXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTF|Lkm1O|Yh|ryP NHPoc5VUSU6JRWK=
KYSE-140 NXPC[293T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYqxc5RbUUN3ME2xOE4xPzV|IN88US=> MXvTRW5ITVJ?
SCC-4 M4DySGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPvTWM2OD1zND6zN|U6KM7:TR?= NVvT[Xp7W0GQR1XS
U251 MmD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTZTWM2OD1zND64OFkzKM7:TR?= M4TscXNCVkeHUh?=
D-542MG MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rDR2lEPTB;MUSuPVIzOiEQvF2= NH3qR|BUSU6JRWK=
LAMA-84 M3zN[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmr3TWM2OD1zND65PVMzKM7:TR?= NX7tPW45W0GQR1XS
NCI-H720 M2fwdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDjV4JKSzVyPUG1MlI3QDRizszN NYj2UFljW0GQR1XS
DEL M{Wxdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nlPWlEPTB;MUWuOFI6OyEQvF2= NUnmO|ZRW0GQR1XS
SBC-1 NYj1PYplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\sbmlEPTB;MUWuOFMxPSEQvF2= MkS5V2FPT0WU
ECC10 NXTtTJU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXjRm5KSzVyPUG1MlQ1PThizszN NWnqRnFFW0GQR1XS
Daoy MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HWVGlEPTB;MUWuO|YyPiEQvF2= M3zuTHNCVkeHUh?=
SCH NGf6THdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXRT|dOUUN3ME2xOU44QDN3IN88US=> NF\tR3lUSU6JRWK=
MZ2-MEL MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTF4LkC2OFYh|ryP NGmzRlJUSU6JRWK=
CAL-12T NGXS[|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjrZ2NKSzVyPUG2MlQ5PjJizszN Mn3UV2FPT0WU
KE-37 M2Hjemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPyfmVFUUN3ME2xOk45OTB5IN88US=> M3LXfnNCVkeHUh?=
LS-411N Ml;BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFyzTGpKSzVyPUG3MlEyQCEQvF2= NHz1UoxUSU6JRWK=
NCI-H2228 NV25XJF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXmTWM2OD1zNz6zNFcyKM7:TR?= Ml7aV2FPT0WU
SK-MEL-2 NXS4ZVR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7m[Yt{UUN3ME2xO{41QTZ3IN88US=> NV\pcnFFW0GQR1XS
HN M4jXemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTuTWM2OD1zNz63NlQ5KM7:TR?= NYrnOW97W0GQR1XS
NCI-H1648 M1HV[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTF5LkixPEDPxE1? M37v[XNCVkeHUh?=
IA-LM NIDYfnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mki0TWM2OD1zOD6zNVczKM7:TR?= NGfFT|hUSU6JRWK=
EW-13 M3P0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1yxNmlEPTB;MUiuOVcxQCEQvF2= NUjoTHF2W0GQR1XS
YKG-1 M1v0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTkU2VKSzVyPUG5MlU4OTFizszN M3\yeXNCVkeHUh?=
KNS-81-FD MlnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDyTWM2OD1zOT61PFU5KM7:TR?= M{L6Z3NCVkeHUh?=
23132-87 NGrISItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\qWIdKSzVyPUG5Mlc3PDJizszN NHewelhUSU6JRWK=
NUGC-3 NEO3OVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLuUnpSUUN3ME2xPU46QDh5IN88US=> MUTTRW5ITVJ?
5637 NH;HSVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJyLkC0O|gh|ryP NG\vWJhUSU6JRWK=
NCI-H1755 MnvXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDhO3NuUUN3ME2yNE41PzZ2IN88US=> MkfLV2FPT0WU
RH-18 M2Gy[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTJyLkW3OFgh|ryP M4fycXNCVkeHUh?=
RXF393 NYTNWVJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLKTWM2OD1{MD62O|U3KM7:TR?= NFjkR3JUSU6JRWK=
LU-134-A NVnmfXM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTQN|NsUUN3ME2yNE44ODV4IN88US=> M3;6W3NCVkeHUh?=
TE-12 Mk\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnzcVRKSzVyPUKwMlczODFizszN M3vzTnNCVkeHUh?=
MOLT-4 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTJzLkG5NVUh|ryP Ml3FV2FPT0WU
IGR-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zBV2lEPTB;MkGuN|c6PiEQvF2= MUjTRW5ITVJ?
HOP-92 NUTWdWZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jPSGlEPTB;MkGuOFk5PyEQvF2= MmH5V2FPT0WU
SK-MES-1 Mm[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrCTVBZUUN3ME2yNU44OzhzIN88US=> NVnQOGp4W0GQR1XS
LU-65 MknPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrLNW5KSzVyPUKxMlg3OjRizszN MkDGV2FPT0WU
MS-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjqRVN{UUN3ME2yNk4yOjB|IN88US=> NVjSbW0xW0GQR1XS
LoVo M4TFZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkn1TWM2OD1{Mj6yOFQh|ryP M37hXHNCVkeHUh?=
A704 NIjmSotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfnTWM2OD1{Mj61NVU2KM7:TR?= M4PxbHNCVkeHUh?=
HT-1376 Ml3OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDVS5NKSzVyPUKyMlYxPTlizszN M3fGWXNCVkeHUh?=
IST-MEL1 M1rnfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULmdG45UUN3ME2yNk43PzVzIN88US=> MYHTRW5ITVJ?
Ramos-2G6-4C10 NFGzcG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPVXoNKSzVyPUKyMlc{PjZizszN NEDlbG1USU6JRWK=
T47D NVz6TnVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;Be3JWUUN3ME2yNk44QTd7IN88US=> NEH2WVBUSU6JRWK=
HT-1197 NFj3UYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPYRmxKSzVyPUKzMlA5OTdizszN NWG0TW9ZW0GQR1XS
LB2518-MEL MmPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHaTWM2OD1{Mz62OFEzKM7:TR?= NWXwXFVzW0GQR1XS
J-RT3-T3-5 MljvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjHVnlmUUN3ME2yOE44PTl3IN88US=> MX3TRW5ITVJ?
SK-NEP-1 MoH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTJ2Lki3OFQh|ryP M1TWcnNCVkeHUh?=
NCI-H526 M{G0PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTJ3LkCwNlMh|ryP M4\2U3NCVkeHUh?=
IST-SL1 NIT2WpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTJ3LkK3OVEh|ryP NXHqUY1KW0GQR1XS
HH M2HYNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfaWHZoUUN3ME2yOU4{OTl{IN88US=> MonkV2FPT0WU
NCI-H82 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;wclhqUUN3ME2yOU46OzhizszN M4PET3NCVkeHUh?=
SNU-449 M4Drd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYCzd45FUUN3ME2yO{4zODF6IN88US=> MVvTRW5ITVJ?
COR-L23 NV:zbI96T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrQTWM2OD1{Nz6yPFE{KM7:TR?= MlvjV2FPT0WU
LOXIMVI NWTNN5lVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTJ5LkO2PEDPxE1? NInvR|FUSU6JRWK=
GR-ST MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\tfW5KSzVyPUK3MlY4ODZizszN NV3yW3Z{W0GQR1XS
NCI-SNU-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7T[INKSzVyPUK3Mlk1PCEQvF2= NGX1cFFUSU6JRWK=
ALL-PO MorHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn[1TWM2OD1{OD6xOlA1KM7:TR?= M1n1TXNCVkeHUh?=
ML-2 NELmS5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M322SGlEPTB;MkiuNlgyPCEQvF2= MXjTRW5ITVJ?
HOP-62 NX\1NXg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\XTWM2OD1{OD63NVMh|ryP NETyOWxUSU6JRWK=
EGI-1 NInEbIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;ReWlEPTB;MkiuPFg1PSEQvF2= NHzIem1USU6JRWK=
TCCSUP Mk[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYP5T4I4UUN3ME2yPE46Ojd{IN88US=> MoXsV2FPT0WU
LB996-RCC NFzmcGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\EbIQ6UUN3ME2yPU42Pjh{IN88US=> NUHCXFdQW0GQR1XS
LCLC-97TM1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPCTWM2OD1|Mj6xPVY1KM7:TR?= NYTodG1sW0GQR1XS
NCI-H1304 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjRU2pKSzVyPUOyMlM{ODFizszN MmXVV2FPT0WU
KP-N-YS MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;SSZI2UUN3ME2zNk42QTd|IN88US=> MUDTRW5ITVJ?
NCI-H1770 NWHoU2VtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmC3TWM2OD1|Mz6xOlQ5KM7:TR?= M2\1fHNCVkeHUh?=
EM-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjQTWM2OD1|Mz62OVA1KM7:TR?= MnzHV2FPT0WU
ChaGo-K-1 NHPpR2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfLcWVKSzVyPUOzMlczOzZizszN NU\V[FZOW0GQR1XS
ACHN NHKzRZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTN|LkizPFUh|ryP NXvLR4R4W0GQR1XS
MN-60 Mnu2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTN|Lki1OFQh|ryP NU\UNXUxW0GQR1XS
EW-18 M4TxfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTN|Lki5O|Eh|ryP MYTTRW5ITVJ?
KGN MlPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHCdVdqUUN3ME2zOU44Ojl{IN88US=> MYXTRW5ITVJ?
U031 MoHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjuPZE{UUN3ME2zOU45OTN{IN88US=> NFXSRplUSU6JRWK=
HMV-II MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUn5OXk4UUN3ME2zOk4xPzd2IN88US=> NX;HZpdyW0GQR1XS
L-363 MkO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2GxVmlEPTB;M{euOlQ2PSEQvF2= Mn\QV2FPT0WU
NCI-H1155 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3y0OGlEPTB;M{iuNFAyPSEQvF2= Ml7OV2FPT0WU
NCI-H1793 M2rTemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfqSFZmUUN3ME2zPE4yODJ4IN88US=> MXzTRW5ITVJ?
P30-OHK NVKx[XpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4noZWlEPTB;M{iuNVM{OiEQvF2= MVTTRW5ITVJ?
AN3-CA M1HpbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;tcWs2UUN3ME2zPE4yPjF3IN88US=> NVLDN4xQW0GQR1XS
UACC-257 NVS3NYxST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTN6Lke5JO69VQ>? MmDRV2FPT0WU
MCF7 NWHEXmE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTITWM2OD1|OT64OlI6KM7:TR?= MVnTRW5ITVJ?
KP-N-YN NV7Rb4tCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTRyLkSyPFUh|ryP MUXTRW5ITVJ?
T98G Mnf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7Hc2h1UUN3ME20NE41QTV5IN88US=> M3jVTHNCVkeHUh?=
HGC-27 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWi2c4lqUUN3ME20N{4zPzRizszN NYfDNZhJW0GQR1XS
NCI-H1092 NGnERnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTR|LkK4PVUh|ryP NILl[VdUSU6JRWK=
KARPAS-299 M4S4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXqXYlGUUN3ME20N{4{ODdzIN88US=> M4LYc3NCVkeHUh?=
LB1047-RCC NE\peXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPTTWM2OD12ND65PVU6KM7:TR?= MVLTRW5ITVJ?
786-0 M4fvNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\6NGlEPTB;NEWuOlUh|ryP NWDUPW5QW0GQR1XS
HCC2157 NFPYfoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPi[lBKUUN3ME20Ok4xOzV7IN88US=> MWjTRW5ITVJ?
NY NHTufoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jEVmlEPTB;NE[uNVc4QCEQvF2= MXnTRW5ITVJ?
EFM-19 NH;VfYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFv4eZNKSzVyPUS2Mlc2OzNizszN NYTIT5Q{W0GQR1XS
EW-16 MkPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;PUVhKSzVyPUS2Mlc5ODZizszN NV3IVnBJW0GQR1XS
UM-UC-3 NIPzZnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHmNFdXUUN3ME20Ok45ODV7IN88US=> MVfTRW5ITVJ?
HT-29 NUC0RpJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjDRYdKSzVyPUS3Mlg4QTJizszN M{n2d3NCVkeHUh?=
LN-405 MonqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vNfmlEPTB;NEiuNFgzPyEQvF2= NULWVoEyW0GQR1XS
NCI-H727 NVfuOFdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzkTWM2OD12OD63O|I3KM7:TR?= MYnTRW5ITVJ?
D-502MG MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jlXGlEPTB;NEiuPVY4PiEQvF2= MkHYV2FPT0WU
GMS-10 NVqyNlFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTR7LkK5O|Qh|ryP MVXTRW5ITVJ?
MEL-JUSO MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzkOYVKSzVyPUS5MlM1PyEQvF2= Mo\JV2FPT0WU

... 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]
+ 展开

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]
+ 展开
  • 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]
+ 展开
  • 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
稳定性 powder
in solvent
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 (g) = 浓度 (mol/L) x 体积 (L) 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