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 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123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 NXzZPHlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXITWM2OD1yLkC3OFU4KM7:TR?= M172XnNCVkeHUh?=
EoL-1-cell NXPYbmpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nKd2lEPTB;MD6xOFE3PiEQvF2= MmCxV2FPT0WU
C32 NFGy[5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTBwMUWxN|Eh|ryP M3fW[3NCVkeHUh?=
M14 Mn\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3GwO2lEPTB;MD6yNVc2PyEQvF2= NIXtN5JUSU6JRWK=
CP50-MEL-B Mlf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXGU2VKSzVyPUCuNlk4QDRizszN NYDtU3VUW0GQR1XS
A101D MorWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonITWM2OD1yLkOyOVg6KM7:TR?= MWPTRW5ITVJ?
G-361 MmHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILORZJKSzVyPUCuN|Q3OzdizszN MX;TRW5ITVJ?
HT-144 MkT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jjTmlEPTB;MD6zOlMzQSEQvF2= NFnV[XhUSU6JRWK=
ACN M3G2cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXvfmQ{UUN3ME2wMlM5PDd5IN88US=> MkHDV2FPT0WU
COLO-829 MlfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIT6c2dKSzVyPUCuN|g6PjhizszN MnPvV2FPT0WU
MEL-HO NEjzZlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mof0TWM2OD1yLkSxNVc6KM7:TR?= NW\sdpFEW0GQR1XS
SH-4 M4q3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULyUmRqUUN3ME2wMlQyPDJ{IN88US=> M{O4bXNCVkeHUh?=
SK-MEL-3 NUi5RnQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLMTWM2OD1yLkWxOVY5KM7:TR?= M{[wS3NCVkeHUh?=
A375 NEn0WmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHuxSFdKSzVyPUCuOlc{PTlizszN NU\tUFNIW0GQR1XS
MMAC-SF MmLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\BRVlKSzVyPUCuOlg3OTRizszN M{DiOXNCVkeHUh?=
BHT-101 Mln2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mof1TWM2OD1yLkewO|AzKM7:TR?= MkDGV2FPT0WU
K5 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7oZZFKSzVyPUCuO|YyPDhizszN NFTCXIhUSU6JRWK=
BV-173 MnHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnsblJKSzVyPUCuO|k3PDRizszN MX3TRW5ITVJ?
RVH-421 NEXZZ5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XtW2lEPTB;MD64Olc6PiEQvF2= MoC2V2FPT0WU
HCC2218 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfxe3RvUUN3ME2wMlg4QDR2IN88US=> NUn1U2NMW0GQR1XS
WM-115 NYruR4RXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTBwOEi2PVIh|ryP M1;ZUHNCVkeHUh?=
SK-MEL-28 NWfmNllPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTFwMES1Olkh|ryP M{TndnNCVkeHUh?=
COLO-679 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2[1V2lEPTB;MT6xNFQ3PCEQvF2= MYjTRW5ITVJ?
MZ7-mel MlPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LRcWlEPTB;MT6xOFk3OyEQvF2= NELmd45USU6JRWK=
SK-MEL-30 Mk\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfUcIlKUUN3ME2xMlM{Ozh4IN88US=> NH;JfWZUSU6JRWK=
NCI-H209 M2\UfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\oTWM2OD1zLk[wPFYh|ryP M2K3cHNCVkeHUh?=
HTC-C3 MnvQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjJOVVrUUN3ME2xMlY3Ojl2IN88US=> MXzTRW5ITVJ?
KARPAS-45 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P2N2lEPTB;Mj6wOFk4QCEQvF2= Ml3lV2FPT0WU
NCI-SNU-5 NVfFUmcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTJwMUG5Olkh|ryP NWTQ[4JCW0GQR1XS
KP-4 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\0NolKSzVyPUKuN|A4QDdizszN NFn3VYNUSU6JRWK=
PA-1 NV\6Um1sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTJwN{K2O|Mh|ryP M{Prc3NCVkeHUh?=
HuO-3N1 Mo\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3jRWFoUUN3ME2yMlg4QTR4IN88US=> MX;TRW5ITVJ?
NCI-H358 Mn[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPhTWM2OD1{LkmyNlMzKM7:TR?= MX\TRW5ITVJ?
CTB-1 NYXiWVJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7oTWM2OD1|LkSwNVc3KM7:TR?= MofBV2FPT0WU
697 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;zeXhKSzVyPUOuOVUzPjZizszN MUHTRW5ITVJ?
CP66-MEL NE\adJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1i3NmlEPTB;ND6xOVkzPyEQvF2= M4[zbHNCVkeHUh?=
NB13 NUXTU4RCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTRwNEmxO|kh|ryP MkjsV2FPT0WU
DBTRG-05MG MlXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLOTWM2OD12LkWzN|I2KM7:TR?= NVqzbIpLW0GQR1XS
A2058 MlzwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTRwN{KxOlQh|ryP MonvV2FPT0WU
KG-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXwd2ZTUUN3ME20Mlc{QTB6IN88US=> M370VXNCVkeHUh?=
8305C NILIWYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTVwMUi3N{DPxE1? M2jwZXNCVkeHUh?=
RPMI-7951 M2nyfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTVwOECyPFMh|ryP MmT1V2FPT0WU
CHL-1 M4PCWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTVwOUe2NFMh|ryP MWfTRW5ITVJ?
TI-73 NIHDc4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGL1c3VKSzVyPU[uNFA6ODJizszN MYXTRW5ITVJ?
HT-1080 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHQTWM2OD14LkGwPVQ3KM7:TR?= NVjlW2xqW0GQR1XS
ES5 NFPkbJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHzPFd6UUN3ME22MlE1QTJ2IN88US=> MV3TRW5ITVJ?
8-MG-BA MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPEO2hrUUN3ME22MlE5OTJ7IN88US=> MmrNV2FPT0WU
NB7 M3\2WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nrU2lEPTB;Nj6yNVM4OyEQvF2= MkPpV2FPT0WU
H4 M{LjRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7xdJRnUUN3ME22MlIzPDl|IN88US=> NFG5fpRUSU6JRWK=
CAL-72 NUHIUYlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvBTWM2OD14LkS1OFI{KM7:TR?= M1vD[XNCVkeHUh?=
HCC1806 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTZwOEG5N|Eh|ryP M3vueXNCVkeHUh?=
BCPAP MkPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTdwMkG3OlQh|ryP NUO0UoVoW0GQR1XS
LB2241-RCC MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHacFd4UUN3ME23MlM3QTB5IN88US=> M4TDPXNCVkeHUh?=
COLO-741 M2jMR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfVRnFLUUN3ME24MlAyPjd7IN88US=> M2S4ZnNCVkeHUh?=
HSC-3 MofiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRThwMEewOlgh|ryP NVq1NWFTW0GQR1XS
SW982 NY\wXWUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRThwNEG1NVYh|ryP NEfiUXZUSU6JRWK=
GCT NX20S21[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRThwN{WzNVQh|ryP NGLZT2RUSU6JRWK=
KY821 MoHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTlwMEWxO|gh|ryP MkPNV2FPT0WU
JVM-3 NYnSfIF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXG1ZYw4UUN3ME25MlU3QTl7IN88US=> NVzMbIlHW0GQR1XS
RS4-11 NF24V21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYK3U5hsUUN3ME25MlYxPDhizszN M2X5cnNCVkeHUh?=
VA-ES-BJ M3XpRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7LTWM2OD1zMD6wNVQ6KM7:TR?= MX;TRW5ITVJ?
A431 Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULJ[Yc6UUN3ME2xNE41OjF{IN88US=> M1HhTHNCVkeHUh?=
LXF-289 Mn;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\xTJN6UUN3ME2xNE41PThizszN MUfTRW5ITVJ?
SK-MEL-24 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXETWM2OD1zMD64Nlc1KM7:TR?= MnHrV2FPT0WU
NOS-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTFyLki0O|Ih|ryP M4i5fHNCVkeHUh?=
KNS-62 M4XqTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjqTWM2OD1zMT6yOFA1KM7:TR?= NFPKXI5USU6JRWK=
SK-HEP-1 MkjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLhTWM2OD1zMT6zOVI4KM7:TR?= MULTRW5ITVJ?
A3-KAW NVTIOGZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHv6bHZKSzVyPUGxMlcyPzhizszN M4jRVHNCVkeHUh?=
SK-LU-1 M3K1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUW2cpVGUUN3ME2xNk4zPjV3IN88US=> NX;xcVlPW0GQR1XS
TYK-nu MoWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTF{LkO5N|Ih|ryP MknFV2FPT0WU
NMC-G1 NYnFZpdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTF{Lk[wOlIh|ryP NWLWO|VYW0GQR1XS
BB65-RCC NYPqbWZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoraTWM2OD1zMj63NVY6KM7:TR?= M2GxOHNCVkeHUh?=
QIMR-WIL NWPZclM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTF{Lki4N|Mh|ryP M2jnXnNCVkeHUh?=
D-566MG NIq4TG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfqcpJKSzVyPUGzMlk2PzZizszN NFzOcIVUSU6JRWK=
KYSE-140 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILpOFFKSzVyPUG0MlA4PTNizszN MXLTRW5ITVJ?
SCC-4 NHnkcGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{WzOGlEPTB;MUSuN|M2QSEQvF2= MUHTRW5ITVJ?
U251 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHFTWM2OD1zND64OFkzKM7:TR?= NYLJNlMxW0GQR1XS
D-542MG NVPFbpJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTF2LkmyNlIh|ryP NWHJU5BGW0GQR1XS
LAMA-84 NGDuTXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHn4XnhKSzVyPUG0Mlk6OzJizszN NXf5S|k{W0GQR1XS
NCI-H720 Ml;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfCV5V7UUN3ME2xOU4zPjh2IN88US=> NVy5bHFrW0GQR1XS
DEL M4XKOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfxTWM2OD1zNT60Nlk{KM7:TR?= MoOyV2FPT0WU
SBC-1 M3HhTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2r1VWlEPTB;MUWuOFMxPSEQvF2= M{fKeXNCVkeHUh?=
ECC10 NI\zVo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTF3LkS0OVgh|ryP MXfTRW5ITVJ?
Daoy M2Trdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPMS5dKSzVyPUG1Mlc3OTZizszN MoP5V2FPT0WU
SCH Ml;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPxTWM2OD1zNT63PFM2KM7:TR?= MormV2FPT0WU
MZ2-MEL NFrpcZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;tUmlEPTB;MU[uNFY1PiEQvF2= NHTRTWxUSU6JRWK=
CAL-12T MnjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\Jd2lEPTB;MU[uOFg3OiEQvF2= Ml;NV2FPT0WU
KE-37 MonPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTnc2RVUUN3ME2xOk45OTB5IN88US=> MYjTRW5ITVJ?
LS-411N MlfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoL2TWM2OD1zNz6xNVgh|ryP NHu4PFlUSU6JRWK=
NCI-H2228 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlG2TWM2OD1zNz6zNFcyKM7:TR?= MmnXV2FPT0WU
SK-MEL-2 M1n3Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHiwNI9KSzVyPUG3MlQ6PjVizszN M2jnfnNCVkeHUh?=
HN NGX3NYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXS1SnFXUUN3ME2xO{44OjR6IN88US=> MnLsV2FPT0WU
NCI-H1648 NH;4VppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzZTWM2OD1zNz64NVgh|ryP M1;afnNCVkeHUh?=
IA-LM NIXndYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfDdFVvUUN3ME2xPE4{OTd{IN88US=> NVHSblRJW0GQR1XS
EW-13 NHXpZ4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmf6TWM2OD1zOD61O|A5KM7:TR?= NHLDW4pUSU6JRWK=
YKG-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NISyV|JKSzVyPUG5MlU4OTFizszN NFPaeGhUSU6JRWK=
KNS-81-FD NWG0[GVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTF7LkW4OVgh|ryP NW\2SJZbW0GQR1XS
23132-87 NFriRmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;jTWM2OD1zOT63OlQzKM7:TR?= MmXNV2FPT0WU
NUGC-3 NEfPNndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{GzVmlEPTB;MUmuPVg5PyEQvF2= MYXTRW5ITVJ?
5637 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn6[WZKSzVyPUKwMlA1PzhizszN MXPTRW5ITVJ?
NCI-H1755 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2[5e2lEPTB;MkCuOFc3PCEQvF2= NF;tflBUSU6JRWK=
RH-18 NH\2Z|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJyLkW3OFgh|ryP MYDTRW5ITVJ?
RXF393 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTPcpJbUUN3ME2yNE43PzV4IN88US=> MlrJV2FPT0WU
LU-134-A MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzVbI5XUUN3ME2yNE44ODV4IN88US=> MV\TRW5ITVJ?
TE-12 M1vEWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTJyLkeyNFEh|ryP MUfTRW5ITVJ?
MOLT-4 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTJzLkG5NVUh|ryP NVK5fGxyW0GQR1XS
IGR-1 NF7DbVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjkell3UUN3ME2yNU4{Pzl4IN88US=> NXL2OZFxW0GQR1XS
HOP-92 NFrP[5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmK1TWM2OD1{MT60PVg4KM7:TR?= MU\TRW5ITVJ?
SK-MES-1 M3rKbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm[xTWM2OD1{MT63N|gyKM7:TR?= M{fwdHNCVkeHUh?=
LU-65 NV\2N5hIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\SR5NlUUN3ME2yNU45PjJ2IN88US=> NG[3T4VUSU6JRWK=
MS-1 NUXneYNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\0T5FKSzVyPUKyMlEzODNizszN M1jySnNCVkeHUh?=
LoVo NHvjS5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDt[W9KSzVyPUKyMlI1PCEQvF2= MX3TRW5ITVJ?
A704 MlvIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTJ{LkWxOVUh|ryP Mn7OV2FPT0WU
HT-1376 M3;POGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLLTWM2OD1{Mj62NFU6KM7:TR?= NXzLNHBPW0GQR1XS
IST-MEL1 NFTtemRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTJ{Lk[3OVEh|ryP M1HK[nNCVkeHUh?=
Ramos-2G6-4C10 M3nj[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\4W3JKSzVyPUKyMlc{PjZizszN NIfOSIpUSU6JRWK=
T47D MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWqycWk2UUN3ME2yNk44QTd7IN88US=> MnjOV2FPT0WU
HT-1197 NIHiToVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XFOWlEPTB;MkOuNFgyPyEQvF2= MWPTRW5ITVJ?
LB2518-MEL MlzuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnEb5RMUUN3ME2yN{43PDF{IN88US=> MkH6V2FPT0WU
J-RT3-T3-5 M{Hmb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH32bYdKSzVyPUK0Mlc2QTVizszN MYHTRW5ITVJ?
SK-NEP-1 MmTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnJTWM2OD1{ND64O|Q1KM7:TR?= M13qN3NCVkeHUh?=
NCI-H526 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HLbGlEPTB;MkWuNFAzOyEQvF2= MmH3V2FPT0WU
IST-SL1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTJ3LkK3OVEh|ryP MWPTRW5ITVJ?
HH MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TjUGlEPTB;MkWuN|E6OiEQvF2= NH3zXnNUSU6JRWK=
NCI-H82 MnuyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLGSZlKSzVyPUK1Mlk{QCEQvF2= M2XiXXNCVkeHUh?=
SNU-449 Mm\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nrb2lEPTB;MkeuNlAyQCEQvF2= M4XsdXNCVkeHUh?=
COR-L23 M4TRUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXnTWM2OD1{Nz6yPFE{KM7:TR?= NGfoS4lUSU6JRWK=
LOXIMVI MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHkZ4lKSzVyPUK3MlM3QCEQvF2= NYXLPWZLW0GQR1XS
GR-ST MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\YTWlEPTB;MkeuOlcxPiEQvF2= NFzZco9USU6JRWK=
NCI-SNU-1 NFjIUZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PjZWlEPTB;MkeuPVQ1KM7:TR?= MX7TRW5ITVJ?
ALL-PO MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTJ6LkG2NFQh|ryP M3u2SHNCVkeHUh?=
ML-2 M1;hNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjoOZE3UUN3ME2yPE4zQDF2IN88US=> Mln3V2FPT0WU
HOP-62 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rSdGlEPTB;MkiuO|E{KM7:TR?= NHvwWllUSU6JRWK=
EGI-1 NELLelRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfSTWM2OD1{OD64PFQ2KM7:TR?= NEn5bYhUSU6JRWK=
TCCSUP NWTIZ5JQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE[0clFKSzVyPUK4MlkzPzJizszN M1Ttc3NCVkeHUh?=
LB996-RCC M4PZR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zzeWlEPTB;MkmuOVY5OiEQvF2= NFuyb3FUSU6JRWK=
LCLC-97TM1 M3zBcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDFTWM2OD1|Mj6xPVY1KM7:TR?= MojmV2FPT0WU
NCI-H1304 MoTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPLc2RiUUN3ME2zNk4{OzBzIN88US=> NUn6N4pZW0GQR1XS
KP-N-YS MoLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nz[2lEPTB;M{KuOVk4OyEQvF2= M2\obnNCVkeHUh?=
NCI-H1770 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUf2b5RJUUN3ME2zN{4yPjR6IN88US=> NWH6fVA{W0GQR1XS
EM-2 M17lbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTN|Lk[1NFQh|ryP M3HkRXNCVkeHUh?=
ChaGo-K-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DXXGlEPTB;M{OuO|I{PiEQvF2= NHH4ZY1USU6JRWK=
ACHN NWXsSmNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPITWM2OD1|Mz64N|g2KM7:TR?= NHj0c|JUSU6JRWK=
MN-60 MorFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3YepdKSzVyPUOzMlg2PDRizszN NXnvW2h4W0GQR1XS
EW-18 Mo\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGf1OG1KSzVyPUOzMlg6PzFizszN NV;seWtOW0GQR1XS
KGN M3zPemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFT4eIdKSzVyPUO1MlczQTJizszN M{\qWXNCVkeHUh?=
U031 M1PCUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmKzTWM2OD1|NT64NVMzKM7:TR?= MoO4V2FPT0WU
HMV-II NIXuZo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjDTWM2OD1|Nj6wO|c1KM7:TR?= NX:zVIxVW0GQR1XS
L-363 NVXhdXFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;mWG54UUN3ME2zO{43PDV3IN88US=> MYrTRW5ITVJ?
NCI-H1155 NIHVTWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnLTWM2OD1|OD6wNFE2KM7:TR?= MY\TRW5ITVJ?
NCI-H1793 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmCyTWM2OD1|OD6xNFI3KM7:TR?= NHTYSZRUSU6JRWK=
P30-OHK MkPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjocnkzUUN3ME2zPE4yOzN{IN88US=> NGD6[GNUSU6JRWK=
AN3-CA MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3z2d2lEPTB;M{iuNVYyPSEQvF2= MV;TRW5ITVJ?
UACC-257 NVnBNYZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVn5OJFVUUN3ME2zPE44QSEQvF2= MnrDV2FPT0WU
MCF7 M1jHVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFL3cYtKSzVyPUO5Mlg3OjlizszN NF:5U5hUSU6JRWK=
KP-N-YN M1X5bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLITWM2OD12MD60Nlg2KM7:TR?= NIjFcGRUSU6JRWK=
T98G M3;pbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTRyLkS5OVch|ryP MYrTRW5ITVJ?
HGC-27 NUm4SGVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{KzNWlEPTB;NEOuNlc1KM7:TR?= MWXTRW5ITVJ?
NCI-H1092 MoTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PveWlEPTB;NEOuNlg6PSEQvF2= NHvMSIxUSU6JRWK=
KARPAS-299 MnPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1r4bWlEPTB;NEOuN|A4OSEQvF2= MoLhV2FPT0WU
LB1047-RCC NX\pd5ZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\ndWlEPTB;NESuPVk2QSEQvF2= NUXLSXg4W0GQR1XS
786-0 Ml\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jncGlEPTB;NEWuOlUh|ryP MU\TRW5ITVJ?
HCC2157 MoHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTR4LkCzOVkh|ryP M4\OO3NCVkeHUh?=
NY NGf6THJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEX6R5lKSzVyPUS2MlE4PzhizszN NET3WpVUSU6JRWK=
EFM-19 NF2yToVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHFbZZKSzVyPUS2Mlc2OzNizszN MXnTRW5ITVJ?
EW-16 M4OzXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTR4Lke4NFYh|ryP NVnpSm5CW0GQR1XS
UM-UC-3 Mo\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTR4LkiwOVkh|ryP Ml3rV2FPT0WU
HT-29 Mn\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXZSXhKSzVyPUS3Mlg4QTJizszN M33sZXNCVkeHUh?=
LN-405 NX3xTmpHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlf3TWM2OD12OD6wPFI4KM7:TR?= M{Lu[3NCVkeHUh?=
NCI-H727 M164VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYiwc|duUUN3ME20PE44PzJ4IN88US=> M1\We3NCVkeHUh?=
D-502MG M4T3Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;ZbWlEPTB;NEiuPVY4PiEQvF2= NVflfZhoW0GQR1XS
GMS-10 Moj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PlVWlEPTB;NEmuNlk4PCEQvF2= MXHTRW5ITVJ?
MEL-JUSO MmnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrpPYFKSzVyPUS5MlM1PyEQvF2= NFvWOWxUSU6JRWK=

... 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(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

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