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  
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该产品发表文献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 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TBV2lEPTB;MD6wO|Q2PyEQvF2= NXHFOWtoW0GQR1XS
EoL-1-cell MkW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwMUSxOlYh|ryP NV;vRYFrW0GQR1XS
C32 MnjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPPNm1KSzVyPUCuNVUyOzFizszN MnXoV2FPT0WU
M14 NIDZbZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjRTWM2OD1yLkKxO|U4KM7:TR?= NH;idpZUSU6JRWK=
CP50-MEL-B MlfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLBZVdrUUN3ME2wMlI6Pzh2IN88US=> MnHrV2FPT0WU
A101D MmfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTBwM{K1PFkh|ryP NY\2PHpYW0GQR1XS
G-361 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTBwM{S2N|ch|ryP MljBV2FPT0WU
HT-144 NVjCUlZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmH5TWM2OD1yLkO2N|I6KM7:TR?= NEfRbohUSU6JRWK=
ACN M1nQfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTBwM{i0O|ch|ryP NWfUWoc2W0GQR1XS
COLO-829 M1LFXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvOXIlzUUN3ME2wMlM5QTZ6IN88US=> NVz3c4VbW0GQR1XS
MEL-HO NF2weppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3foTmlEPTB;MD60NVE4QSEQvF2= MlvRV2FPT0WU
SH-4 M3PJb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfGeVZJUUN3ME2wMlQyPDJ{IN88US=> NXXUd5B2W0GQR1XS
SK-MEL-3 NXjCXIN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnXTWM2OD1yLkWxOVY5KM7:TR?= MnHlV2FPT0WU
A375 M1fCfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PBPWlEPTB;MD62O|M2QSEQvF2= MnTmV2FPT0WU
MMAC-SF MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHGTWM2OD1yLk[4OlE1KM7:TR?= M4DhR3NCVkeHUh?=
BHT-101 NX32bpFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITFRZZKSzVyPUCuO|A4ODJizszN NVjQS4pRW0GQR1XS
K5 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\ySGlEPTB;MD63OlE1QCEQvF2= MlvSV2FPT0WU
BV-173 NWflOoprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILB[ZdKSzVyPUCuO|k3PDRizszN MlXvV2FPT0WU
RVH-421 NUfQWWFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;rOWJKSzVyPUCuPFY4QTZizszN NI[y[5JUSU6JRWK=
HCC2218 NUfVbWM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTrbW5WUUN3ME2wMlg4QDR2IN88US=> NV3hXXMyW0GQR1XS
WM-115 NFfCcolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nmUWlEPTB;MD64PFY6OiEQvF2= M1Pu[HNCVkeHUh?=
SK-MEL-28 NH;mUHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPhTWM2OD1zLkC0OVY6KM7:TR?= M2O3c3NCVkeHUh?=
COLO-679 NXn5XZR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzYTWM2OD1zLkGwOFY1KM7:TR?= MmHLV2FPT0WU
MZ7-mel NIfONlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjxUItWUUN3ME2xMlE1QTZ|IN88US=> NHXlVY5USU6JRWK=
SK-MEL-30 NXTVcGpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTFwM{OzPFYh|ryP NIrkXGpUSU6JRWK=
NCI-H209 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEH2eY5KSzVyPUGuOlA5PiEQvF2= M{fPcHNCVkeHUh?=
HTC-C3 M3fR[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnPTWM2OD1zLk[2Nlk1KM7:TR?= NIrSSYFUSU6JRWK=
KARPAS-45 MkOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnoTWM2OD1{LkC0PVc5KM7:TR?= NGnSUlZUSU6JRWK=
NCI-SNU-5 M4TXcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HNbGlEPTB;Mj6xNVk3QSEQvF2= NIrGT|hUSU6JRWK=
KP-4 NHTBV5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4X2bWlEPTB;Mj6zNFc5PyEQvF2= M2D4VHNCVkeHUh?=
PA-1 NFrj[pBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDzbHhXUUN3ME2yMlczPjd|IN88US=> M1PD[nNCVkeHUh?=
HuO-3N1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjx[m9KSzVyPUKuPFc6PDZizszN MX3TRW5ITVJ?
NCI-H358 NXH1TnBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\0SGMzUUN3ME2yMlkzOjN{IN88US=> MWLTRW5ITVJ?
CTB-1 NWHXcoNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorPTWM2OD1|LkSwNVc3KM7:TR?= MYDTRW5ITVJ?
697 M2TDZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTNwNUWyOlYh|ryP NUD0N|dDW0GQR1XS
CP66-MEL NVXtXJlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPTcFZYUUN3ME20MlE2QTJ5IN88US=> NXfJV4NlW0GQR1XS
NB13 NWDnXFRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILNXG9KSzVyPUSuOFkyPzlizszN MXjTRW5ITVJ?
DBTRG-05MG NVH5[phKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTRwNUOzNlUh|ryP NXPZZ3p7W0GQR1XS
A2058 MkK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PDV2lEPTB;ND63NlE3PCEQvF2= MmGwV2FPT0WU
KG-1 M3O0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfNbHhKSzVyPUSuO|M6ODhizszN M{LFdHNCVkeHUh?=
8305C NHvmW4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGL2V3pKSzVyPUWuNVg4OyEQvF2= NGWzNFlUSU6JRWK=
RPMI-7951 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXjPZRiUUN3ME21MlgxOjh|IN88US=> MorjV2FPT0WU
CHL-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[wTWM2OD13Lkm3OlA{KM7:TR?= MkTMV2FPT0WU
TI-73 NVLJd49uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vvNWlEPTB;Nj6wNFkxOiEQvF2= Mn70V2FPT0WU
HT-1080 M4O4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk[3TWM2OD14LkGwPVQ3KM7:TR?= M1;rSXNCVkeHUh?=
ES5 NXvmPYlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrJTWM2OD14LkG0PVI1KM7:TR?= MXnTRW5ITVJ?
8-MG-BA M3THTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTZwMUixNlkh|ryP M1[yRnNCVkeHUh?=
NB7 M1ezdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvjTWM2OD14LkKxN|c{KM7:TR?= M3HBWXNCVkeHUh?=
H4 Mmj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnO1TWM2OD14LkKyOFk{KM7:TR?= MWjTRW5ITVJ?
CAL-72 Mk\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HJ[WlEPTB;Nj60OVQzOyEQvF2= MYDTRW5ITVJ?
HCC1806 M2f5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnaXpVCUUN3ME22MlgyQTNzIN88US=> MXzTRW5ITVJ?
BCPAP NGjaS4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDvTWM2OD15LkKxO|Y1KM7:TR?= M1vneXNCVkeHUh?=
LB2241-RCC M2ThTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHETWM2OD15LkO2PVA4KM7:TR?= M{fTbnNCVkeHUh?=
COLO-741 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{W0SWlEPTB;OD6wNVY4QSEQvF2= NXq3b21wW0GQR1XS
HSC-3 NX\YSIY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;uTWlEPTB;OD6wO|A3QCEQvF2= MXTTRW5ITVJ?
SW982 MoPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHH2S5hKSzVyPUiuOFE2OTZizszN M1faW3NCVkeHUh?=
GCT MkHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\kbGtTUUN3ME24Mlc2OzF2IN88US=> MV;TRW5ITVJ?
KY821 NUf4TWtFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknUTWM2OD17LkC1NVc5KM7:TR?= NVPYZ4dZW0GQR1XS
JVM-3 Mkn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTlwNU[5PVkh|ryP NU\BTYZzW0GQR1XS
RS4-11 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\mTWM2OD17Lk[wOFgh|ryP NFThPGtUSU6JRWK=
VA-ES-BJ M3GzS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTFyLkCxOFkh|ryP M{XGTnNCVkeHUh?=
A431 NILON5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLl[ppKSzVyPUGwMlQzOTJizszN MVzTRW5ITVJ?
LXF-289 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnDTWM2OD1zMD60OVgh|ryP M2XhTXNCVkeHUh?=
SK-MEL-24 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljaTWM2OD1zMD64Nlc1KM7:TR?= M2i2NXNCVkeHUh?=
NOS-1 NF:1cG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonZTWM2OD1zMD64OFczKM7:TR?= MonqV2FPT0WU
KNS-62 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTFzLkK0NFQh|ryP NYH1cXJMW0GQR1XS
SK-HEP-1 M3j5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrkd|NKSzVyPUGxMlM2OjdizszN Mn\3V2FPT0WU
A3-KAW NYf2dGY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTFzLkexO|gh|ryP Mnz3V2FPT0WU
SK-LU-1 NWrHXWVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLDdZFOUUN3ME2xNk4zPjV3IN88US=> NULhcVdQW0GQR1XS
TYK-nu MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjUOWhTUUN3ME2xNk4{QTN{IN88US=> MXzTRW5ITVJ?
NMC-G1 NHLoUGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoL2TWM2OD1zMj62NFYzKM7:TR?= M1jzR3NCVkeHUh?=
BB65-RCC M1PwW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NES2e2hKSzVyPUGyMlcyPjlizszN NIfUPWdUSU6JRWK=
QIMR-WIL NYjWS|JnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYT6c3VkUUN3ME2xNk45QDN|IN88US=> MVHTRW5ITVJ?
D-566MG M3;jRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPqOGFKSzVyPUGzMlk2PzZizszN NEnpUWZUSU6JRWK=
KYSE-140 NF3BVIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHrZXBGUUN3ME2xOE4xPzV|IN88US=> M2jkXXNCVkeHUh?=
SCC-4 MnPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT6dpFKSzVyPUG0MlM{PTlizszN MlXBV2FPT0WU
U251 M2n0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLoTWM2OD1zND64OFkzKM7:TR?= MmrsV2FPT0WU
D-542MG NEnWU41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1uxPWlEPTB;MUSuPVIzOiEQvF2= M1Tu[nNCVkeHUh?=
LAMA-84 M2P1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXqc4tKSzVyPUG0Mlk6OzJizszN NYfLdIh5W0GQR1XS
NCI-H720 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LqXGlEPTB;MUWuNlY5PCEQvF2= NGmyU4dUSU6JRWK=
DEL NU\1ZYNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXLOppKSzVyPUG1MlQzQTNizszN NVfqc3JFW0GQR1XS
SBC-1 NHHG[4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGKwPJZKSzVyPUG1MlQ{ODVizszN M2iwPXNCVkeHUh?=
ECC10 M1nnbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDPTWM2OD1zNT60OFU5KM7:TR?= MWXTRW5ITVJ?
Daoy MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUThNm01UUN3ME2xOU44PjF4IN88US=> NEjFW2RUSU6JRWK=
SCH NXzSXpFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\iTWM2OD1zNT63PFM2KM7:TR?= NXXGdHduW0GQR1XS
MZ2-MEL NF;hZ3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnP0TWM2OD1zNj6wOlQ3KM7:TR?= MXTTRW5ITVJ?
CAL-12T MlPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rrOmlEPTB;MU[uOFg3OiEQvF2= MnTIV2FPT0WU
KE-37 MlTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTF4LkixNFch|ryP NGj3[3RUSU6JRWK=
LS-411N NW[2R5dOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37TdWlEPTB;MUeuNVE5KM7:TR?= NWTONmp2W0GQR1XS
NCI-H2228 NYqxc5hOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHGTWM2OD1zNz6zNFcyKM7:TR?= M2HSTnNCVkeHUh?=
SK-MEL-2 MlHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HHVGlEPTB;MUeuOFk3PSEQvF2= NX\4epFGW0GQR1XS
HN M{DvRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDnTWM2OD1zNz63NlQ5KM7:TR?= MX3TRW5ITVJ?
NCI-H1648 Mn3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUWxcJZWUUN3ME2xO{45OThizszN NU[2VoxwW0GQR1XS
IA-LM NF71ToRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jOe2lEPTB;MUiuN|E4OiEQvF2= MnnwV2FPT0WU
EW-13 NIXrTpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfGTWM2OD1zOD61O|A5KM7:TR?= M1vxVnNCVkeHUh?=
YKG-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2S3cGlEPTB;MUmuOVcyOSEQvF2= MkHUV2FPT0WU
KNS-81-FD MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PVfWlEPTB;MUmuOVg2QCEQvF2= M{\ZNnNCVkeHUh?=
23132-87 MkXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTSTWM2OD1zOT63OlQzKM7:TR?= NWWwTW5qW0GQR1XS
NUGC-3 M1TncWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTF7Lkm4PFch|ryP NYTWV2VpW0GQR1XS
5637 NVLZTIpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M336[2lEPTB;MkCuNFQ4QCEQvF2= MoCyV2FPT0WU
NCI-H1755 M3fnXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4O1d2lEPTB;MkCuOFc3PCEQvF2= NEXMS5ZUSU6JRWK=
RH-18 MorPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIizOohKSzVyPUKwMlU4PDhizszN MVrTRW5ITVJ?
RXF393 MojUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPPfnJWUUN3ME2yNE43PzV4IN88US=> MnHUV2FPT0WU
LU-134-A M37zXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGr3cGRKSzVyPUKwMlcxPTZizszN MULTRW5ITVJ?
TE-12 NWTCeHFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPzeIZuUUN3ME2yNE44OjBzIN88US=> NVvUWlBEW0GQR1XS
MOLT-4 M3vsdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoW1TWM2OD1{MT6xPVE2KM7:TR?= NUDFUm8yW0GQR1XS
IGR-1 NYWyW2FGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITHbotKSzVyPUKxMlM4QTZizszN MmnvV2FPT0WU
HOP-92 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfzOllKSzVyPUKxMlQ6QDdizszN Mo\LV2FPT0WU
SK-MES-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXuTWM2OD1{MT63N|gyKM7:TR?= NYf2W|VbW0GQR1XS
LU-65 MlSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTJzLki2NlQh|ryP NYezNHpmW0GQR1XS
MS-1 NYHOPIl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3uTWM2OD1{Mj6xNlA{KM7:TR?= M1nB[XNCVkeHUh?=
LoVo M3zIXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonOTWM2OD1{Mj6yOFQh|ryP M1nlb3NCVkeHUh?=
A704 NEjPcpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjHXHpRUUN3ME2yNk42OTV3IN88US=> MXfTRW5ITVJ?
HT-1376 M3[2fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nwVmlEPTB;MkKuOlA2QSEQvF2= M4LxW3NCVkeHUh?=
IST-MEL1 M1;MZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmP4TWM2OD1{Mj62O|UyKM7:TR?= MWrTRW5ITVJ?
Ramos-2G6-4C10 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\KTWM2OD1{Mj63N|Y3KM7:TR?= NEf6d4pUSU6JRWK=
T47D M3fPNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;CXVh{UUN3ME2yNk44QTd7IN88US=> NHvzeZNUSU6JRWK=
HT-1197 M2SyOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTJ|LkC4NVch|ryP M1;mb3NCVkeHUh?=
LB2518-MEL NVfjeXZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTJ|Lk[0NVIh|ryP MVjTRW5ITVJ?
J-RT3-T3-5 M{jyUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTJ2Lke1PVUh|ryP MVvTRW5ITVJ?
SK-NEP-1 MlK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHWTWM2OD1{ND64O|Q1KM7:TR?= NVvFVJc2W0GQR1XS
NCI-H526 MlnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\LVHE2UUN3ME2yOU4xODJ|IN88US=> M1nOWnNCVkeHUh?=
IST-SL1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\2T2lEPTB;MkWuNlc2OSEQvF2= MUTTRW5ITVJ?
HH NXi1T4lvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTJ3LkOxPVIh|ryP NYHrdZBtW0GQR1XS
NCI-H82 MmXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHRSJYyUUN3ME2yOU46OzhizszN M3X6WnNCVkeHUh?=
SNU-449 MlfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTUTWM2OD1{Nz6yNFE5KM7:TR?= NH3iUWhUSU6JRWK=
COR-L23 M4LxSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4D0UGlEPTB;MkeuNlgyOyEQvF2= NEezcWNUSU6JRWK=
LOXIMVI MoTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1y0S2lEPTB;MkeuN|Y5KM7:TR?= MoOxV2FPT0WU
GR-ST MkjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DHN2lEPTB;MkeuOlcxPiEQvF2= MkTiV2FPT0WU
NCI-SNU-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTJ5Lkm0OEDPxE1? MkTGV2FPT0WU
ALL-PO MlrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlS2TWM2OD1{OD6xOlA1KM7:TR?= M4jjWnNCVkeHUh?=
ML-2 NUexTo13T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrPXHZKSzVyPUK4MlI5OTRizszN M2fRSnNCVkeHUh?=
HOP-62 Mm\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEiydlJKSzVyPUK4MlcyOyEQvF2= MmWxV2FPT0WU
EGI-1 MmTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7PZWxKSzVyPUK4Mlg5PDVizszN M3fES3NCVkeHUh?=
TCCSUP MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVmwXod4UUN3ME2yPE46Ojd{IN88US=> NYTmV3V6W0GQR1XS
LB996-RCC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTJ7LkW2PFIh|ryP NXjWOYlSW0GQR1XS
LCLC-97TM1 M4nJZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTN{LkG5OlQh|ryP MUXTRW5ITVJ?
NCI-H1304 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPTOmtjUUN3ME2zNk4{OzBzIN88US=> Mn\FV2FPT0WU
KP-N-YS NEXYdVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XRcWlEPTB;M{KuOVk4OyEQvF2= MUDTRW5ITVJ?
NCI-H1770 NITPXoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvtTWM2OD1|Mz6xOlQ5KM7:TR?= M1LDU3NCVkeHUh?=
EM-2 MkLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFKwTmpKSzVyPUOzMlY2ODRizszN NEXPdGdUSU6JRWK=
ChaGo-K-1 M1nWWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M372WGlEPTB;M{OuO|I{PiEQvF2= M1rmc3NCVkeHUh?=
ACHN MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTN|LkizPFUh|ryP MoTpV2FPT0WU
MN-60 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HCSGlEPTB;M{OuPFU1PCEQvF2= Ml;6V2FPT0WU
EW-18 NGTrZWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTN|Lki5O|Eh|ryP M2DmdXNCVkeHUh?=
KGN NIfQ[WhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTN3LkeyPVIh|ryP NXuzUpd3W0GQR1XS
U031 NV7YVHF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fBXWlEPTB;M{WuPFE{OiEQvF2= NUjmSnRCW0GQR1XS
HMV-II NIWyRlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;0TWM2OD1|Nj6wO|c1KM7:TR?= NXPIZ5I4W0GQR1XS
L-363 M3TYfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPDc|RYUUN3ME2zO{43PDV3IN88US=> MnrsV2FPT0WU
NCI-H1155 NWrNOVlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTkTWM2OD1|OD6wNFE2KM7:TR?= NITjdIxUSU6JRWK=
NCI-H1793 NHHvNXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTN6LkGwNlYh|ryP MmPjV2FPT0WU
P30-OHK Mm\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTN6LkGzN|Ih|ryP M1\5UHNCVkeHUh?=
AN3-CA Mm[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HuT2lEPTB;M{iuNVYyPSEQvF2= MYfTRW5ITVJ?
UACC-257 NIDKTY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TvW2lEPTB;M{iuO|kh|ryP M1OxNnNCVkeHUh?=
MCF7 NIrGXpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Hv[GlEPTB;M{muPFYzQSEQvF2= M2TqfXNCVkeHUh?=
KP-N-YN NG\5PIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXwRoZKSzVyPUSwMlQzQDVizszN M4DJe3NCVkeHUh?=
T98G NGD3c3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rYVGlEPTB;NECuOFk2PyEQvF2= MmfMV2FPT0WU
HGC-27 NUPPXFVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HybWlEPTB;NEOuNlc1KM7:TR?= NVvZbZNjW0GQR1XS
NCI-H1092 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGGxNHRKSzVyPUSzMlI5QTVizszN NYLUOYZ7W0GQR1XS
KARPAS-299 NFnQb5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\ETldKSzVyPUSzMlMxPzFizszN Mon5V2FPT0WU
LB1047-RCC NFjB[IVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XVS2lEPTB;NESuPVk2QSEQvF2= MUjTRW5ITVJ?
786-0 MmHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTR3Lk[1JO69VQ>? M1fsdHNCVkeHUh?=
HCC2157 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3XTWM2OD12Nj6wN|U6KM7:TR?= NVjseZo1W0GQR1XS
NY M1fGSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HldGlEPTB;NE[uNVc4QCEQvF2= MV3TRW5ITVJ?
EFM-19 NGTEd5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPITWM2OD12Nj63OVM{KM7:TR?= M1XkOHNCVkeHUh?=
EW-16 M1Lnb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPPVIdKSzVyPUS2Mlc5ODZizszN NELhWIJUSU6JRWK=
UM-UC-3 MmDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorrTWM2OD12Nj64NFU6KM7:TR?= NYDJcGlbW0GQR1XS
HT-29 MmTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUT1SXhjUUN3ME20O{45Pzl{IN88US=> M1zGd3NCVkeHUh?=
LN-405 M3zrW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXoTWM2OD12OD6wPFI4KM7:TR?= MYHTRW5ITVJ?
NCI-H727 M1PH[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;qWJljUUN3ME20PE44PzJ4IN88US=> MYnTRW5ITVJ?
D-502MG M1KwfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrUV|ZEUUN3ME20PE46Pjd4IN88US=> NWjBW3I{W0GQR1XS
GMS-10 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTR7LkK5O|Qh|ryP M1vTd3NCVkeHUh?=
MEL-JUSO M1\TPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TuXWlEPTB;NEmuN|Q4KM7:TR?= NGH6[2xUSU6JRWK=

... 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID