PLX-4720 化学構造
分子量: 413.83

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Quality Control & MSDS

製品説明

  • Compare Raf Inhibitors
    Raf製品生物活性の比較
  • 研究分野
  • PLX-4720のメカニズム

製品の説明

生物活性

製品説明 PLX-4720は、B-Raf(V600E)とc-Raf-1(Y340D/Y341D)の「実行中の」形の強力で選択的な阻害剤で、IC50 がそれぞれ 13 nM と 6.7 nMです。
ターゲット B-RafV600E c-Raf-1Y340D/Y341D
IC50 13 nM 6.7 nM [1]
In vitro試験 PLX-4720 displays >10 times selectivity against wild type B-Raf, and >100 times selectivity over other kinases such as Frk, Src, Fak, FGFR, and Aurora A with IC50 of 1.3-3.4 μM. PLX-4720 significantly inhibits the ERK phosphorylation in cell lines bearing B-RafV600E with IC50 of 14-46 nM, but not the cells with wild-type B-Raf. PLX-4720 significantly inhibits the growth of tumor cell lines bearing the B-RafV600E oncogene, such as COLO205, A375, WM2664, and COLO829 with GI50 of 0.31 μM, 0.50 μM, 1.5 μM, and 1.7 μM, respectively. In addition, PLX-4720 treatment at 1 μM induces cell cycle arrest and apoptosis exclusively in the B-RafV600E-positive 1205Lu cells, but not in the B-Raf wild-type C8161 cells. [1] PLX-4720 treatment (10 μM) significantly induces >14-fold expression of BIM in the PTEN+ cells, compared with the PTEN- cell lines (4-fold), giving an explanation of the resistance of PTEN- cells to PLX-4720-induced apoptosis. [2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
DU-4475 M3zmTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzyTY1KSzVyPUCuNFc1PTdizszN NUjuR4p5W0GQR1XS
EoL-1-cell MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIGycYtKSzVyPUCuNVQyPjZizszN Ml\BV2FPT0WU
C32 NWX0V|g{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHLO2hKSzVyPUCuNVUyOzFizszN MVHTRW5ITVJ?
M14 NULKWm9vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTBwMkG3OVch|ryP M4LQR3NCVkeHUh?=
CP50-MEL-B NYLTN|RyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFL4OoRKSzVyPUCuNlk4QDRizszN NIjzbFBUSU6JRWK=
A101D MkLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXyTWM2OD1yLkOyOVg6KM7:TR?= MknRV2FPT0WU
G-361 NV[1dmNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwM{S2N|ch|ryP NIezcHRUSU6JRWK=
HT-144 MonTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXuTWM2OD1yLkO2N|I6KM7:TR?= NVLYSGhDW0GQR1XS
ACN MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPCN2ZKSzVyPUCuN|g1PzdizszN NIHrcXFUSU6JRWK=
COLO-829 NH2xR49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7lTWM2OD1yLkO4PVY5KM7:TR?= M4PKN3NCVkeHUh?=
MEL-HO NVXoWlNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnn3TWM2OD1yLkSxNVc6KM7:TR?= NFfwWHVUSU6JRWK=
SH-4 NWPGR4tbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPOTYZKSzVyPUCuOFE1OjJizszN NIfLR5hUSU6JRWK=
SK-MEL-3 MmjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTBwNUG1Olgh|ryP NXuzcGRzW0GQR1XS
A375 NXHiVIhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fneWlEPTB;MD62O|M2QSEQvF2= MkLTV2FPT0WU
MMAC-SF MonUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7oSXhKSzVyPUCuOlg3OTRizszN NILxWWJUSU6JRWK=
BHT-101 NIDtNXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHsZmJUUUN3ME2wMlcxPzB{IN88US=> NIHnfI1USU6JRWK=
K5 MnXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTBwN{[xOFgh|ryP MlzZV2FPT0WU
BV-173 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{C3SGlEPTB;MD63PVY1PCEQvF2= NWLjR|dFW0GQR1XS
RVH-421 M3\BZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\6VIpKSzVyPUCuPFY4QTZizszN NHfC[4pUSU6JRWK=
HCC2218 M4TYcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwOEe4OFQh|ryP NHPxWWhUSU6JRWK=
WM-115 MnezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\rSpBKSzVyPUCuPFg3QTJizszN NFzR[3dUSU6JRWK=
SK-MEL-28 NWLST29QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTTTWM2OD1zLkC0OVY6KM7:TR?= M4XLcXNCVkeHUh?=
COLO-679 MnHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DWVWlEPTB;MT6xNFQ3PCEQvF2= NEDaWFdUSU6JRWK=
MZ7-mel NU\JXFlDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV71dlVHUUN3ME2xMlE1QTZ|IN88US=> NV;LNIl[W0GQR1XS
SK-MEL-30 MmDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfmTWM2OD1zLkOzN|g3KM7:TR?= NHTme5pUSU6JRWK=
NCI-H209 NWfpPY1wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnjWnFyUUN3ME2xMlYxQDZizszN MlrkV2FPT0WU
HTC-C3 M1PTOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nuUWlEPTB;MT62OlI6PCEQvF2= NU\rSGdwW0GQR1XS
KARPAS-45 MnTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfXTWM2OD1{LkC0PVc5KM7:TR?= M4HF[nNCVkeHUh?=
NCI-SNU-5 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1GxV2lEPTB;Mj6xNVk3QSEQvF2= MkToV2FPT0WU
KP-4 NFH6NIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITrXHpKSzVyPUKuN|A4QDdizszN M13qPXNCVkeHUh?=
PA-1 M1zZN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTSTWM2OD1{LkeyOlc{KM7:TR?= MWTTRW5ITVJ?
HuO-3N1 MlHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEK0V2dKSzVyPUKuPFc6PDZizszN MXXTRW5ITVJ?
NCI-H358 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\WU2lEPTB;Mj65NlI{OiEQvF2= NUXtfZAyW0GQR1XS
CTB-1 NH3MdWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4j5U2lEPTB;Mz60NFE4PiEQvF2= Ml;UV2FPT0WU
697 NFL0[IVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTNwNUWyOlYh|ryP NW[zWWxyW0GQR1XS
CP66-MEL NYfSOZdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TQVWlEPTB;ND6xOVkzPyEQvF2= NHPZS|FUSU6JRWK=
NB13 M1LOOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTKZo5KSzVyPUSuOFkyPzlizszN M{niUXNCVkeHUh?=
DBTRG-05MG NX;Ndm5FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjCZXBKSzVyPUSuOVM{OjVizszN NVnFOJZ1W0GQR1XS
A2058 MoDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYj0OZVZUUN3ME20MlczOTZ2IN88US=> MkjhV2FPT0WU
KG-1 M4XqcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHDU2RKSzVyPUSuO|M6ODhizszN NVrXcVQ{W0GQR1XS
8305C NWnDZYU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXr0U3MzUUN3ME21MlE5PzNizszN NVvLRWoyW0GQR1XS
RPMI-7951 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4exZmlEPTB;NT64NFI5OyEQvF2= M3HITnNCVkeHUh?=
CHL-1 NHLPe2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vVcWlEPTB;NT65O|YxOyEQvF2= NFX3fWdUSU6JRWK=
TI-73 NHe1UlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXDTWM2OD14LkCwPVAzKM7:TR?= NEOxZo9USU6JRWK=
HT-1080 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vnRWlEPTB;Nj6xNFk1PiEQvF2= M{LjUnNCVkeHUh?=
ES5 M1fkTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfsOpBKSzVyPU[uNVQ6OjRizszN NV62[ZVvW0GQR1XS
8-MG-BA NWTmZ4Q4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoD0TWM2OD14LkG4NVI6KM7:TR?= MX7TRW5ITVJ?
NB7 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXQSZVZUUN3ME22MlIyOzd|IN88US=> NHXHVJVUSU6JRWK=
H4 NIWxcldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEW2[XNKSzVyPU[uNlI1QTNizszN NVrsXIs6W0GQR1XS
CAL-72 MoK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI[5dlJKSzVyPU[uOFU1OjNizszN MoPiV2FPT0WU
HCC1806 M1v6PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\heYlKSzVyPU[uPFE6OzFizszN MojsV2FPT0WU
BCPAP NVS0R3dOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:xc|duUUN3ME23MlIyPzZ2IN88US=> M{XK[3NCVkeHUh?=
LB2241-RCC MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTdwM{[5NFch|ryP MXnTRW5ITVJ?
COLO-741 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfCNHR4UUN3ME24MlAyPjd7IN88US=> NUHHdXdVW0GQR1XS
HSC-3 MkDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTpb2NKSzVyPUiuNFcxPjhizszN Ml\hV2FPT0WU
SW982 NH\UeotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\IcGlEPTB;OD60NVUyPiEQvF2= M{DHUHNCVkeHUh?=
GCT NHfuZm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRThwN{WzNVQh|ryP MmrNV2FPT0WU
KY821 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzTWoxkUUN3ME25MlA2OTd6IN88US=> NFH5bm9USU6JRWK=
JVM-3 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTlwNU[5PVkh|ryP M4L1VHNCVkeHUh?=
RS4-11 NXvMdGsyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHmTWM2OD17Lk[wOFgh|ryP NWfX[4FSW0GQR1XS
VA-ES-BJ MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfHTWM2OD1zMD6wNVQ6KM7:TR?= NEXvXlRUSU6JRWK=
A431 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXtTWM2OD1zMD60NlEzKM7:TR?= M2rVT3NCVkeHUh?=
LXF-289 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\L[Y1KSzVyPUGwMlQ2QCEQvF2= MU\TRW5ITVJ?
SK-MEL-24 NWLw[2FtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTFyLkiyO|Qh|ryP MlmwV2FPT0WU
NOS-1 NHrj[GFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfLTWM2OD1zMD64OFczKM7:TR?= NUfjU5Q3W0GQR1XS
KNS-62 Ml3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTFzLkK0NFQh|ryP NGnDdVNUSU6JRWK=
SK-HEP-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXrbFBKSzVyPUGxMlM2OjdizszN M1Hk[nNCVkeHUh?=
A3-KAW NHLaSJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jzdWlEPTB;MUGuO|E4QCEQvF2= MX;TRW5ITVJ?
SK-LU-1 NX3HflZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXR[INbUUN3ME2xNk4zPjV3IN88US=> NF;PdHJUSU6JRWK=
TYK-nu M3ztd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfYUoVEUUN3ME2xNk4{QTN{IN88US=> NYnmdYNiW0GQR1XS
NMC-G1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XlZWlEPTB;MUKuOlA3OiEQvF2= MoLYV2FPT0WU
BB65-RCC NE\ZNmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2j1RWlEPTB;MUKuO|E3QSEQvF2= NFjX[I1USU6JRWK=
QIMR-WIL M{TTXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTF{Lki4N|Mh|ryP M1S4SnNCVkeHUh?=
D-566MG NGW3T5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTF|Lkm1O|Yh|ryP M3LrWHNCVkeHUh?=
KYSE-140 MnjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIm5XmtKSzVyPUG0MlA4PTNizszN M2jqbXNCVkeHUh?=
SCC-4 M3\DfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYixfJh[UUN3ME2xOE4{OzV7IN88US=> M{\0XHNCVkeHUh?=
U251 MlXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkG5TWM2OD1zND64OFkzKM7:TR?= NFzYfZlUSU6JRWK=
D-542MG M1nQTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXJfIxKSzVyPUG0MlkzOjJizszN NGfOXYVUSU6JRWK=
LAMA-84 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rDdGlEPTB;MUSuPVk{OiEQvF2= NYTxXFloW0GQR1XS
NCI-H720 MlrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTF3LkK2PFQh|ryP M4HtXnNCVkeHUh?=
DEL NHqwXWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTq[25KSzVyPUG1MlQzQTNizszN M1myW3NCVkeHUh?=
SBC-1 NYT1flduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfYboRKSzVyPUG1MlQ{ODVizszN Ml75V2FPT0WU
ECC10 NX3DRW5tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPjXZJKSzVyPUG1MlQ1PThizszN MlfuV2FPT0WU
Daoy NVS0T4FbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTF3Lke2NVYh|ryP M2PUeXNCVkeHUh?=
SCH MknZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHS2SnFKSzVyPUG1Mlc5OzVizszN NWPIUJlpW0GQR1XS
MZ2-MEL MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\Ce5hKSzVyPUG2MlA3PDZizszN M1rrUXNCVkeHUh?=
CAL-12T Mlq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3z2VmlEPTB;MU[uOFg3OiEQvF2= NXrZSW1xW0GQR1XS
KE-37 NF\CSFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTF4LkixNFch|ryP MorWV2FPT0WU
LS-411N NIDpW41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXqU4JHUUN3ME2xO{4yOThizszN MnLRV2FPT0WU
NCI-H2228 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLx[HB4UUN3ME2xO{4{ODdzIN88US=> MYPTRW5ITVJ?
SK-MEL-2 NHnGNGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4K1OWlEPTB;MUeuOFk3PSEQvF2= M3XHdXNCVkeHUh?=
HN MojOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;uTWM2OD1zNz63NlQ5KM7:TR?= NV;QN|hEW0GQR1XS
NCI-H1648 NXTzenZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vzV2lEPTB;MUeuPFE5KM7:TR?= M4W3fnNCVkeHUh?=
IA-LM MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTF6LkOxO|Ih|ryP MWLTRW5ITVJ?
EW-13 NXPOWJg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVe5dlU4UUN3ME2xPE42PzB6IN88US=> NHPnbnNUSU6JRWK=
YKG-1 MnvaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13B[mlEPTB;MUmuOVcyOSEQvF2= NWXpWoh4W0GQR1XS
KNS-81-FD M1LhZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;FTWM2OD1zOT61PFU5KM7:TR?= MnvUV2FPT0WU
23132-87 M13ITmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1ywXGlEPTB;MUmuO|Y1OiEQvF2= MmDsV2FPT0WU
NUGC-3 M{O2[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PC[2lEPTB;MUmuPVg5PyEQvF2= M2nHdXNCVkeHUh?=
5637 NE\WcIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DDeGlEPTB;MkCuNFQ4QCEQvF2= MYPTRW5ITVJ?
NCI-H1755 NIHWUWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvuPYc6UUN3ME2yNE41PzZ2IN88US=> NUO4O3RGW0GQR1XS
RH-18 NV;Xe4YyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\wTWM2OD1{MD61O|Q5KM7:TR?= NVO3bFZMW0GQR1XS
RXF393 NV[2UlU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfsTWM2OD1{MD62O|U3KM7:TR?= M4CwT3NCVkeHUh?=
LU-134-A M{G5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLYXmxTUUN3ME2yNE44ODV4IN88US=> M3vOdHNCVkeHUh?=
TE-12 M1e5dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jCXWlEPTB;MkCuO|IxOSEQvF2= NXLiWnNWW0GQR1XS
MOLT-4 NXvZR|lZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILueINKSzVyPUKxMlE6OTVizszN MVrTRW5ITVJ?
IGR-1 MkWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHafHpzUUN3ME2yNU4{Pzl4IN88US=> NUHwNWdCW0GQR1XS
HOP-92 NYXydYFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHpOGJKSzVyPUKxMlQ6QDdizszN NEjm[|RUSU6JRWK=
SK-MES-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLSTJZKSzVyPUKxMlc{QDFizszN M2W1OHNCVkeHUh?=
LU-65 M{XnU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV33TVdTUUN3ME2yNU45PjJ2IN88US=> MV3TRW5ITVJ?
MS-1 MlXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13UXWlEPTB;MkKuNVIxOyEQvF2= NGfjdHZUSU6JRWK=
LoVo MnTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3nTWM2OD1{Mj6yOFQh|ryP M3q5bHNCVkeHUh?=
A704 NGLDN2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4KyW2lEPTB;MkKuOVE2PSEQvF2= NXfObItPW0GQR1XS
HT-1376 NUjiSXpCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHoTWM2OD1{Mj62NFU6KM7:TR?= MmXGV2FPT0WU
IST-MEL1 NVvmW4pWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjLOGlKSzVyPUKyMlY4PTFizszN NXPDd3ZCW0GQR1XS
Ramos-2G6-4C10 NYm5dpVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PDcWlEPTB;MkKuO|M3PiEQvF2= NHfYeZNUSU6JRWK=
T47D NVHqWWI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\WW4g{UUN3ME2yNk44QTd7IN88US=> NGjJNVdUSU6JRWK=
HT-1197 NHLrTItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTJ|LkC4NVch|ryP MUjTRW5ITVJ?
LB2518-MEL MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvwU2UxUUN3ME2yN{43PDF{IN88US=> NHvGcYFUSU6JRWK=
J-RT3-T3-5 NHfI[lJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnzXHVKSzVyPUK0Mlc2QTVizszN NVHSU4pmW0GQR1XS
SK-NEP-1 NWnBR2VqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTJ2Lki3OFQh|ryP MnjmV2FPT0WU
NCI-H526 NIT1bmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTJ3LkCwNlMh|ryP MkDjV2FPT0WU
IST-SL1 M4D4cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTuTWM2OD1{NT6yO|UyKM7:TR?= MVXTRW5ITVJ?
HH NUDPTFJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1za[2lEPTB;MkWuN|E6OiEQvF2= M1vZ[XNCVkeHUh?=
NCI-H82 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTJ3LkmzPEDPxE1? NIDxWJFUSU6JRWK=
SNU-449 M3TYfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nRT2lEPTB;MkeuNlAyQCEQvF2= NXjUZZRkW0GQR1XS
COR-L23 M1K3Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\IfZFKSzVyPUK3MlI5OTNizszN M{XIN3NCVkeHUh?=
LOXIMVI NULpR|VQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXW4bWJPUUN3ME2yO{4{PjhizszN NWPFO|dQW0GQR1XS
GR-ST Mo\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3K4VmlEPTB;MkeuOlcxPiEQvF2= NFrIUGNUSU6JRWK=
NCI-SNU-1 M1PDZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDpcHhKSzVyPUK3Mlk1PCEQvF2= NFK0U2NUSU6JRWK=
ALL-PO MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfaeXdKSzVyPUK4MlE3ODRizszN MXrTRW5ITVJ?
ML-2 MoqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrNTWM2OD1{OD6yPFE1KM7:TR?= Mkj3V2FPT0WU
HOP-62 NYXNTYpiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;5Z|JQUUN3ME2yPE44OTNizszN NFy1ZmVUSU6JRWK=
EGI-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnRU5NKSzVyPUK4Mlg5PDVizszN MnfmV2FPT0WU
TCCSUP MlTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTJ6LkmyO|Ih|ryP NVLObGQ2W0GQR1XS
LB996-RCC NF\HWpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\JTWM2OD1{OT61OlgzKM7:TR?= M4HLTXNCVkeHUh?=
LCLC-97TM1 NFKxNnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;nTWM2OD1|Mj6xPVY1KM7:TR?= MYDTRW5ITVJ?
NCI-H1304 M{\iZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTN{LkOzNFEh|ryP NEDLUllUSU6JRWK=
KP-N-YS Mnv0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7BTWM2OD1|Mj61PVc{KM7:TR?= NWrPfW9VW0GQR1XS
NCI-H1770 NGLHPXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HKbmlEPTB;M{OuNVY1QCEQvF2= NVSyeWdyW0GQR1XS
EM-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXWTWM2OD1|Mz62OVA1KM7:TR?= NI[ydWlUSU6JRWK=
ChaGo-K-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPJTWM2OD1|Mz63NlM3KM7:TR?= NUfXdmJZW0GQR1XS
ACHN M1vlT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTN|LkizPFUh|ryP NX;ofWNPW0GQR1XS
MN-60 MnTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfIS5FKSzVyPUOzMlg2PDRizszN NIjP[ZFUSU6JRWK=
EW-18 MmfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFL0SVVKSzVyPUOzMlg6PzFizszN NUnxbJNxW0GQR1XS
KGN NWHubmx1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlu0TWM2OD1|NT63NlkzKM7:TR?= MoPuV2FPT0WU
U031 NXTMWnV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\2TWM2OD1|NT64NVMzKM7:TR?= M{\rNnNCVkeHUh?=
HMV-II NIrkSlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLxUoZKSzVyPUO2MlA4PzRizszN NHq5UoNUSU6JRWK=
L-363 NVvnUW9MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTVTWM2OD1|Nz62OFU2KM7:TR?= M2TaUHNCVkeHUh?=
NCI-H1155 NXi5Z3JKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrQTpJKSzVyPUO4MlAxOTVizszN MmrGV2FPT0WU
NCI-H1793 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH34T5BKSzVyPUO4MlExOjZizszN M{\v[nNCVkeHUh?=
P30-OHK NGfadWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTN6LkGzN|Ih|ryP MXXTRW5ITVJ?
AN3-CA NWPQe2V{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\oN2lEPTB;M{iuNVYyPSEQvF2= NV7RTZdvW0GQR1XS
UACC-257 MkHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTHTWM2OD1|OD63PUDPxE1? MVTTRW5ITVJ?
MCF7 MmG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHMTWM2OD1|OT64OlI6KM7:TR?= MUDTRW5ITVJ?
KP-N-YN MnfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrZTWM2OD12MD60Nlg2KM7:TR?= M4KwOHNCVkeHUh?=
T98G NIrkR4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4mzbGlEPTB;NECuOFk2PyEQvF2= NW\5SpNiW0GQR1XS
HGC-27 NYLEWZRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{j5bWlEPTB;NEOuNlc1KM7:TR?= MWnTRW5ITVJ?
NCI-H1092 Mn7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnWwTWM2OD12Mz6yPFk2KM7:TR?= NUjVepZyW0GQR1XS
KARPAS-299 MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIO0dGlKSzVyPUSzMlMxPzFizszN NHPv[JRUSU6JRWK=
LB1047-RCC NEK2c45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\BfmtKSzVyPUS0Mlk6PTlizszN MX3TRW5ITVJ?
786-0 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1G5N2lEPTB;NEWuOlUh|ryP MU\TRW5ITVJ?
HCC2157 M2fYW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\zS3lmUUN3ME20Ok4xOzV7IN88US=> NUTTTJdUW0GQR1XS
NY NH\rfVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rVeWlEPTB;NE[uNVc4QCEQvF2= MkXBV2FPT0WU
EFM-19 MmHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTDeFNZUUN3ME20Ok44PTN|IN88US=> MoHmV2FPT0WU
EW-16 Mn7QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTR4Lke4NFYh|ryP NVXSSZJsW0GQR1XS
UM-UC-3 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHEUIhkUUN3ME20Ok45ODV7IN88US=> NH\HWopUSU6JRWK=
HT-29 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTR5Lki3PVIh|ryP NH\kflRUSU6JRWK=
LN-405 MoHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILheGFKSzVyPUS4MlA5OjdizszN MmrDV2FPT0WU
NCI-H727 NUO3O2htT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\mRmlEPTB;NEiuO|czPiEQvF2= M2O0V3NCVkeHUh?=
D-502MG NFnTWldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTR6Lkm2O|Yh|ryP MmD2V2FPT0WU
GMS-10 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzRVJVSUUN3ME20PU4zQTd2IN88US=> MUjTRW5ITVJ?
MEL-JUSO NIS2UJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTR7LkO0O{DPxE1? NYf5XpRxW0GQR1XS

... Click to View More Cell Line Experimental Data

In vivo試験 Oral administration of PLX-4720 at 20 mg/kg/day induces significant tumor growth delays and regressions in B-RafV600E-dependent COLO205 tumor xenografts, without obvious adverse effects in mice even at dose of 1 g/kg. PLX-4720 at 100 mg/kg twice daily almost completely eliminates the 1205Lu xenografts bearing B-RafV600E, while has no activity against C8161 xenografts bearing wild-type B-Raf. The anti-tumor effects of PLX-4720 correlate with the blockade of MAPK pathway in those cells harboring the V600E mutation. [1] PLX-4720 treatment at 30 mg/kg/day significant inhibits the tumor growth of 8505c xenografts by >90%, and dramatically decreases distant lung metastases. [3]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

In vitro Raf kinase activities The in vitro kinase activities of wild type Raf and mutants are determined by measuring phosphorylation of biotinylated-MEK protein using Perkin-Elmer's AlphaScreen Technology. For each enzyme (0.1 ng), 20-μL reactions are carried out in 20 mM Hepes (pH 7.0), 10 mM MgCl2, 1 mM DTT, 0.01% Tween-20, 100 nM biotin-MEK protein, various ATP concentrations, and increasing concentrations of PLX-4720 at room temperature. Reactions are stopped at 2, 5, 8, 10, 20, and 30 minutes with 5 μL of a solution containing 20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, and 0.3% BSA. The stop solution also includes phospho-MEK Antibody, Streptavidin-coated Donor beads and Protein A Acceptor beads from the AlphaScreen Protein A Detection Kit. The antibody and beads are preincubated in stop solution in the dark at room temperature for 30 minutes. The final dilution of antibody is 1/2,000, and the final concentration of each bead is 10 μg/mL. The assay plates are incubated at room temperature for one hour then are read on a PerkinElmer AlphaQuest reader.

細胞アッセイ: [1]

細胞株 COLO205, A375, WM2664, COLO829, HT716, SW620, H460, Calu-6, HCT116, SK-MEL2, SK-MEL3, Lovo, H1299, 1205Lu, and C8161 cells
濃度 Dissolved in DMSO, final concentrations ~1 mM
反応時間 24, 48, and 72 hours
実験の流れ Cells are treated with various concentrations PLX-4720 for 24, 48, and 72 hours. Cell proliferation is measured by using the CellTiter-Glo Luminescent Cell Viability Assay or MTT assay. For cell cycle analysis, supernatant and cells are collected, pelleted, and fixed with 70% ethanol. Before staining with propidium iodide (10 μg/mL), cells are incubated for 1 hour at 37 °C in 0.5 mg/mL RNase I to rid samples of residual RNA contamination. Samples are then analyzed by using the EPICS XL apparatus. For the assessment of apoptosis, media and cells are harvested and pelleted before staining with annexin-FITC and propidium iodide. Samples are subsequently analyzed by using the EPICS XL apparatus.

動物実験: [1]

動物モデル Female athymic mice (NCr nu/nu) implanted s.c. with COLO205 cells, and SCID mice with 1205Lu or C8161 cells
製剤 Suspended in vehicle (5% DMSO, 1% methylcellulose)
投薬量 5, 20, or 100 mg/kg
投与方法 Oral gavage once or twice daily

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download PLX-4720 SDF
分子量 413.83
化学式

C17H14ClF2N3O3S

CAS No. 918505-84-7
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 83 mg/mL (200.56 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 1% CMC/0.5% Tween-80 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 N-(3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide

カスタマーフィードバック (9)


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Rating
Source Cancer Discov, 2013, 3, 350-62. PLX-4720 purchased from Selleck
Method Western blot
Cell Lines A375 cells
Concentrations 1 uM
Incubation Time 16 h
Results Associated with the increased RAS-GTP, it's observed a concomitant increase in C-RAF activation, as measured by phosphorylation of Ser338. Under conditions of combined C-RAF/NF1 knockdown, ERK phosphorylation was inhibited more effectively compared to knockdown of NF1 alone. Moreover, whereas cyclin D1 levels were inhibited by PLX4720 in A375 cells, but NF1 silencing partially alleviated this effect.

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Rating
Source Genes Dev, 2012, 26, 1055-69. PLX-4720 purchased from Selleck
Method Western blot
Cell Lines Melanoma cell lines
Concentrations 1, 2, 3 uM
Incubation Time 4 h, 3 days
Results Treatment with Pi-103 and PLX4720 (a BRAFV600E inhibitor) inhibited the activity of AKT and ERK, respectively (D). More importantly, Pi-103 treatment profoundly cooperated with PLX4720 of inhibition in dose response curves(E).

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Source Proc Natl Acad Sci USA , 2011, 108, 6067-6072. PLX-4720 purchased from Selleck
Method Western blotting
Cell Lines Cells overexpressing myc-CRAF and BRAF
Concentrations 10/50 µM
Incubation Time 1/2 h
Results GDC0879 but not PLX4720 induced BRAF/CRAF dimer formation (Fig. A). However, both drugs induced complexes between KSR1 and CRAF and enhanced interactions between KSR1 and BRAF (Fig. B and C), which suggested that KSR1/RAF complexes induced by the drug might explain the effects ofthe type I BRAF specific inhibitors. As reported previously, treatment of wild-type cells with either drug strongly induced ERK activation at low to intermediate doses but inhibited ERK activation at higher doses (Fig. D and E). Similar results were obtained with cells expressing constitutively active RAS (Fig. D and E) or after serum treatment. Strikingly, in KSR deficient cells, ERK activation was significantly attenuated after PLX4720 or GDC0879 treatment (Fig. D and E), which demonstrates that the ability of PLX4720 and GDC0879 to activate ERK requires the presence of KSR1. We found that, when KSR1 was overexpressed withCRAF, MEK activation was induced by PLX4720 or GDC0879 treatment (Fig. F). this result suggested that induction of the CRAF/KSR1 complex might be important in the activation of MEK. In vitro kinase activity toward MEK was detected but only after drug treatment (Fig. G), which suggests KSR1/CRAF complex formation kinase activity toward MEK.

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Rating
Source Cancer Res , 2011, 71, 2750-2760. PLX-4720 purchased from Selleck
Method Western blotting, MTT assay, flow cytometry
Cell Lines PTEN+/ PTEN- melanoma cell lines
Concentrations 0.001-10 µmol/L
Incubation Time 48 h
Results The PTEN+ cell lines had lower constitutive levels of pAKT (Ser473) compared with the PTEN(Fig. A). Similar levels of pAKT (Thr308) were observed in the PTEN and PTEN þ cell lines. Analysis of the growth inhibitory effects of PLX4720 by the MTT and Alamar Blue assays (Fig. B) did not reveal any statistically significant differences in the GI 50 values between the PTEN+/ PTEN- cell lines. We observed that following PLX4720 treatment (3 and 10 µmol/L, 48 hours), the PTEN-melanoma cell lines showed significantly less apoptosis than the PTEN+ (P < 0.05: Fig. C)

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Rating
Source Cancer Res , 2011, 71, 2750-2760. PLX-4720 purchased from Selleck
Method Western blotting
Cell Lines PTEN+/ PTEN- melanoma cell lines
Concentrations 0.03-3 µmol/L
Incubation Time 24 h
Results Treatment of the PTEN+/ PTEN- cell line panels with PLX4720 increased pPDK1andpAKTsignaling only in the melanoma cell lines lacking PTEN expression (Fig. A). Addition of PLX4720 also led to the inhibition of mTOR activity in the PTEN+ cell lines only (Fig. A). The requirement for PTEN in the increased AKT signaling was confirmed by studies showing that PLX4720 stimulated pAKT in WM35 cells (PTEN+) when PTEN was knocked down by siRNA (Fig. B). The effects of PLX4720 upon pAKT signaling were BRAF specific, with BRAF siRNA knockdown found to increase pAKT in PTEN- cells only (Fig. C).

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Rating
Source Cancer Res, 2011, 71, 2750-2760. PLX-4720 purchased from Selleck
Method Western blot, Immunofluorescence staining, flow cytometry
Cell Lines 1205Lu cells
Concentrations 3 µmol/L
Incubation Time 48 h
Results Combined PI3K and BRAF inhibition increased the level of BIM expression in both Western blot and immunofluorescence studies (Fig. A). Consistent with a role for increased AKT signaling suppressing BIM expression in PTEN- cells, dual BRAF and PI3K inhibition increased nuclear FOXO3a localization in the PTEN- cell lines (Fig. B) and enhanced the level of BIM mRNA (Fig. B). the combination of PLX4720 with the PI3K inhibitor GDC-0941 significantly enhanced the levels of apoptosis observed in PTEN melanoma cell lines compared to either the BRAF or PI3K inhibitor alone (Fig. C). Similar results were also observed in a 3D spheroid assay, where combined PLX4720 (3 µmol/L) and LY294002 (10 µmol/L) treatment prevented the recovery of cell growth observed when melanoma spheroids were treated with either drug alone (Fig. D).

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Rating
Source Cancer Res , 2011, 71, 2750-2760. PLX-4720 purchased from Selleck
Method LC-MRM analysis, Western blotting, immunofluorescence staining
Cell Lines PTEN+/ PTEN- melanoma cell lines
Concentrations 3/10 µmol/L
Incubation Time 0-48 h
Results We next used LC-MRM to quantify the PLX4720-induced changes in the expression of 17 members of the Bcl-2 protein family (Fig. A shows results for 9 proteins). The only proapoptotic protein to demonstrate significant differences between the PTEN+/ PTEN- cell lines was BIM (Fig. A). Western blots and immunofluorescence staining confirmed the LC-MRM data and showed a greater degree of PLX4720-induced BIM expression in the PTEN+ cell lines compared to PTEN- cell lines (Fig. B,C). In parallel, we observed that PLX4720 also increased the inactivation of BAD (as shown by increased phospho-BAD) in the PTEN- cells (Fig. D) and that overexpression of BAD in the PTEN- cells enhanced PLX4720-mediated apoptosis (Fig. D).

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Rating
Source Dr. Jong-In Park of Medical College of Wisconsin. PLX-4720 purchased from Selleck
Method Western blot
Cell Lines SK-MEL-28 cell line
Concentrations 0-1 µM
Incubation Time 4/22 h
Results B-RafV600E mutated melanoma line, SK-MEL-28, was treated with different doses of PLX-4720 for 4 h or 22 h. Cell lysates were analyzed by Western blotting to determine the levels of phosphorylated MEK1/2 (pMEK1/2) and phosphorylated ERK1/2 (pERK1/2). MEK1/2 is the substrate of B-Raf while ERK1/2 is the substrate of MEK1/2. Data show that phosphorylation of MEK1/2 and ERK1/2 was significantly inhibited by PLX-4720 treatment although total MEK1/2 or ERK1/2 protein levels were not affected. No pMEK1/2 or pERK1/2 signal was detected even after prolonged exposure, indicating that the inhibitor at 1 μM is very effective in blocking the constitutive kinase activity of B-RafV600E. This data is consistent with the previous result demonstrating the effect of PLX-4720 in the B-RafV600E mutated melanoma line, A375-Fig. 2A

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Rating
Source Dr. Daniel C.Cho of Harvard Medical School. PLX-4720 purchased from Selleck
Method MTT assay, Western blotting
Cell Lines A375 melanoma cells
Concentrations 0-1000 nM
Incubation Time
Results A dose titration of PLX-4720 in A375 melanoma cells which possess a V600E B-Raf mutation.Effects of increasing PLX-4720 dose on Erk phosphorylation and on tumor cell proliferation as determined by MTT assay are shown.

文献中の引用 (44)

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    Sorafenib Tosylateは、Raf-1、B-RafとVEGFR-2のマルチキナーゼ阻害剤で、IC50 がそれぞれ 6 nM、 22 nM、90 nMです。

  • TAK-632

    TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf, respectively, showing less or no inhibition against other tested kinases.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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