PLX-4720

For research use only.

Catalog No.S1152

137 publications

PLX-4720 Chemical Structure

CAS No. 918505-84-7

PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.

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Selleck's PLX-4720 has been cited by 137 publications

Purity & Quality Control

Choose Selective Raf Inhibitors

Biological Activity

Description PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.
Targets
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
In vitro

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DU-4475 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTBwMEe0OVch|ryP MknVV2FPT0WU
EoL-1-cell NWXZXGttT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nJXmlEPTB;MD6xOFE3PiEQvF2= MlS4V2FPT0WU
C32 NIDtb3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmqwTWM2OD1yLkG1NVMyKM7:TR?= MlHiV2FPT0WU
M14 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwMkG3OVch|ryP NUK3SW5GW0GQR1XS
CP50-MEL-B NI\sXnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzy[npKSzVyPUCuNlk4QDRizszN MkDWV2FPT0WU
A101D NWD4SWVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ewdmlEPTB;MD6zNlU5QSEQvF2= MmniV2FPT0WU
G-361 NWnoS|lKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTBwM{S2N|ch|ryP MVfTRW5ITVJ?
HT-144 M2jhc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPLfmVKSzVyPUCuN|Y{OjlizszN M1TFNXNCVkeHUh?=
ACN M3nNZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnf4TWM2OD1yLkO4OFc4KM7:TR?= MmmxV2FPT0WU
COLO-829 NF62e2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYO0SZVmUUN3ME2wMlM5QTZ6IN88US=> MWTTRW5ITVJ?
MEL-HO MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzCTWM2OD1yLkSxNVc6KM7:TR?= Mm\LV2FPT0WU
SH-4 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\ySlRKSzVyPUCuOFE1OjJizszN NGT3PXNUSU6JRWK=
SK-MEL-3 MkfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnrN|NKSzVyPUCuOVE2PjhizszN MV3TRW5ITVJ?
A375 MmfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLydFlKSzVyPUCuOlc{PTlizszN NWrGOJFtW0GQR1XS
MMAC-SF M1HZWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfF[I5WUUN3ME2wMlY5PjF2IN88US=> MWPTRW5ITVJ?
BHT-101 MnG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnh[3VOUUN3ME2wMlcxPzB{IN88US=> MlfiV2FPT0WU
K5 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUe0b4RYUUN3ME2wMlc3OTR6IN88US=> MWfTRW5ITVJ?
BV-173 NFfzc3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorWTWM2OD1yLke5OlQ1KM7:TR?= M4PwRXNCVkeHUh?=
RVH-421 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPwcXZKSzVyPUCuPFY4QTZizszN MmnlV2FPT0WU
HCC2218 NEHnS3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;2fWlEPTB;MD64O|g1PCEQvF2= MnvBV2FPT0WU
WM-115 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTESHdyUUN3ME2wMlg5Pjl{IN88US=> MknIV2FPT0WU
SK-MEL-28 NVfvWoxTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfUTWM2OD1zLkC0OVY6KM7:TR?= NEW0TINUSU6JRWK=
COLO-679 M1;WPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWO2dox7UUN3ME2xMlExPDZ2IN88US=> NWDYV3U3W0GQR1XS
MZ7-mel NFzD[HZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXNR2R3UUN3ME2xMlE1QTZ|IN88US=> M2j0WHNCVkeHUh?=
SK-MEL-30 NW[2UZljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrLbWFKSzVyPUGuN|M{QDZizszN NX\TTo1XW0GQR1XS
NCI-H209 NYPLTmhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTFwNkC4OkDPxE1? MnuyV2FPT0WU
HTC-C3 NXvy[4hTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;iVJBIUUN3ME2xMlY3Ojl2IN88US=> NHnITnBUSU6JRWK=
KARPAS-45 NX\jfW9NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPNTWM2OD1{LkC0PVc5KM7:TR?= MmLZV2FPT0WU
NCI-SNU-5 NWjZNYJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XiUmlEPTB;Mj6xNVk3QSEQvF2= MYHTRW5ITVJ?
KP-4 M2PQO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrwfIhKSzVyPUKuN|A4QDdizszN M3rGcXNCVkeHUh?=
PA-1 NW\QbHNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrjRWdKSzVyPUKuO|I3PzNizszN NHLnXXlUSU6JRWK=
HuO-3N1 M33TPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHG5UmxKSzVyPUKuPFc6PDZizszN MnT3V2FPT0WU
NCI-H358 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrwWmpKSzVyPUKuPVIzOzJizszN NY\kNZl{W0GQR1XS
CTB-1 MnP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo[wTWM2OD1|LkSwNVc3KM7:TR?= MofvV2FPT0WU
697 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HXdWlEPTB;Mz61OVI3PiEQvF2= M2DU[3NCVkeHUh?=
CP66-MEL NH;Gb4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjR[XhKSzVyPUSuNVU6OjdizszN M1jvfXNCVkeHUh?=
NB13 NFz5OlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTRwNEmxO|kh|ryP M1LEcXNCVkeHUh?=
DBTRG-05MG MnXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTRwNUOzNlUh|ryP MUHTRW5ITVJ?
A2058 M2XaTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTRwN{KxOlQh|ryP MkfaV2FPT0WU
KG-1 NGjJcWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1O3eWlEPTB;ND63N|kxQCEQvF2= NIr1TJpUSU6JRWK=
8305C M1;zUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILKUlhKSzVyPUWuNVg4OyEQvF2= MknhV2FPT0WU
RPMI-7951 MnTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPHTWM2OD13LkiwNlg{KM7:TR?= Mlr5V2FPT0WU
CHL-1 NYjORVVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{WyOWlEPTB;NT65O|YxOyEQvF2= MkLoV2FPT0WU
TI-73 M{PMdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfNTWM2OD14LkCwPVAzKM7:TR?= MVHTRW5ITVJ?
HT-1080 NHzEZ5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnTU|M5UUN3ME22MlExQTR4IN88US=> M4XRUXNCVkeHUh?=
ES5 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHJTWM2OD14LkG0PVI1KM7:TR?= NGDJcZlUSU6JRWK=
8-MG-BA MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTZwMUixNlkh|ryP MoPuV2FPT0WU
NB7 M{LaSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVK1PFQxUUN3ME22MlIyOzd|IN88US=> MWPTRW5ITVJ?
H4 MnLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PVOGlEPTB;Nj6yNlQ6OyEQvF2= NVziW25NW0GQR1XS
CAL-72 NHzYcIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnj0TWM2OD14LkS1OFI{KM7:TR?= NW[xNXdWW0GQR1XS
HCC1806 NHvIdWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjCNm8zUUN3ME22MlgyQTNzIN88US=> NGXzT4tUSU6JRWK=
BCPAP NF7Bb4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTdwMkG3OlQh|ryP Mn3sV2FPT0WU
LB2241-RCC MoTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XLSGlEPTB;Nz6zOlkxPyEQvF2= M4f3PXNCVkeHUh?=
COLO-741 NUPhbWhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmf2TWM2OD16LkCxOlc6KM7:TR?= MYPTRW5ITVJ?
HSC-3 NFTKZnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fldWlEPTB;OD6wO|A3QCEQvF2= MYLTRW5ITVJ?
SW982 NFHQT4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHHO2VKSzVyPUiuOFE2OTZizszN NE\2eYhUSU6JRWK=
GCT NVPqZoFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;VNnlKSzVyPUiuO|U{OTRizszN MY\TRW5ITVJ?
KY821 M3;COmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTlwMEWxO|gh|ryP MUHTRW5ITVJ?
JVM-3 NF7ke4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTlwNU[5PVkh|ryP NVXGWVByW0GQR1XS
RS4-11 NHzaXW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLBTWM2OD17Lk[wOFgh|ryP NIS5cJhUSU6JRWK=
VA-ES-BJ NGHMNVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFyLkCxOFkh|ryP NYTPdHJQW0GQR1XS
A431 MoHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHQTWM2OD1zMD60NlEzKM7:TR?= MnHBV2FPT0WU
LXF-289 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH63[otKSzVyPUGwMlQ2QCEQvF2= MWrTRW5ITVJ?
SK-MEL-24 NX\oXYZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFOyUmNKSzVyPUGwMlgzPzRizszN M4XicXNCVkeHUh?=
NOS-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILEVIFKSzVyPUGwMlg1PzJizszN NH7Je3dUSU6JRWK=
KNS-62 MlnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLKTWM2OD1zMT6yOFA1KM7:TR?= MVfTRW5ITVJ?
SK-HEP-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1yw[GlEPTB;MUGuN|UzPyEQvF2= MnK5V2FPT0WU
A3-KAW MoDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v2TGlEPTB;MUGuO|E4QCEQvF2= Ml7VV2FPT0WU
SK-LU-1 NX[2[|hnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDaTohxUUN3ME2xNk4zPjV3IN88US=> NXPETHc3W0GQR1XS
TYK-nu NYT5dlRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXNTWM2OD1zMj6zPVMzKM7:TR?= NXT3epVwW0GQR1XS
NMC-G1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTF{Lk[wOlIh|ryP MXXTRW5ITVJ?
BB65-RCC NYfG[5ZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWqyRW9uUUN3ME2xNk44OTZ7IN88US=> MoHqV2FPT0WU
QIMR-WIL NIjVPWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fpPGlEPTB;MUKuPFg{OyEQvF2= NYDGbpM5W0GQR1XS
D-566MG NG\0Z5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrnWmJKSzVyPUGzMlk2PzZizszN NEjEWpJUSU6JRWK=
KYSE-140 NHjGXGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjYe5JjUUN3ME2xOE4xPzV|IN88US=> NHLDfJBUSU6JRWK=
SCC-4 Mn:1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkGxTWM2OD1zND6zN|U6KM7:TR?= NUDmT5hyW0GQR1XS
U251 NGfydpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTF2Lki0PVIh|ryP NYm1e2o5W0GQR1XS
D-542MG MlSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\wPWlEPTB;MUSuPVIzOiEQvF2= NGj4NZdUSU6JRWK=
LAMA-84 NHu2bIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmf2TWM2OD1zND65PVMzKM7:TR?= MXjTRW5ITVJ?
NCI-H720 NWXieY5PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHDem5XUUN3ME2xOU4zPjh2IN88US=> MlHRV2FPT0WU
DEL NFvhTYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTF3LkSyPVMh|ryP M{js[3NCVkeHUh?=
SBC-1 M4jtT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jWeGlEPTB;MUWuOFMxPSEQvF2= MYTTRW5ITVJ?
ECC10 Mnr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrDW5VKSzVyPUG1MlQ1PThizszN NIHsR2hUSU6JRWK=
Daoy Ml;jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzGTWM2OD1zNT63OlE3KM7:TR?= MkXuV2FPT0WU
SCH MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPJZlhKSzVyPUG1Mlc5OzVizszN NYTkWYw{W0GQR1XS
MZ2-MEL NXzOO4N6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTF4LkC2OFYh|ryP MUnTRW5ITVJ?
CAL-12T MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrFTWM2OD1zNj60PFYzKM7:TR?= M2jaWXNCVkeHUh?=
KE-37 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\xR2lEPTB;MU[uPFExPyEQvF2= Mnv0V2FPT0WU
LS-411N NGrYV5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jaSWlEPTB;MUeuNVE5KM7:TR?= MYHTRW5ITVJ?
NCI-H2228 MmH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfQPW4{UUN3ME2xO{4{ODdzIN88US=> MWnTRW5ITVJ?
SK-MEL-2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTF5LkS5OlUh|ryP MnfIV2FPT0WU
HN MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjtcnhGUUN3ME2xO{44OjR6IN88US=> MmfDV2FPT0WU
NCI-H1648 NGnGT|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLyTWM2OD1zNz64NVgh|ryP MUXTRW5ITVJ?
IA-LM M3ftUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jidmlEPTB;MUiuN|E4OiEQvF2= M3XxenNCVkeHUh?=
EW-13 Ml\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3UTHZKSzVyPUG4MlU4ODhizszN MYXTRW5ITVJ?
YKG-1 M1TxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInZO|ZKSzVyPUG5MlU4OTFizszN MXTTRW5ITVJ?
KNS-81-FD MkLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHlTWM2OD1zOT61PFU5KM7:TR?= MWnTRW5ITVJ?
23132-87 NYrSeJc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Lh[GlEPTB;MUmuO|Y1OiEQvF2= NVHVT5RzW0GQR1XS
NUGC-3 NG\LeIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HnXWlEPTB;MUmuPVg5PyEQvF2= MofkV2FPT0WU
5637 NILoOXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rWcWlEPTB;MkCuNFQ4QCEQvF2= NYDlTpZsW0GQR1XS
NCI-H1755 Mli1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjlTWM2OD1{MD60O|Y1KM7:TR?= Mm\QV2FPT0WU
RH-18 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXzTWM2OD1{MD61O|Q5KM7:TR?= NIThTZlUSU6JRWK=
RXF393 MofjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXKTWM2OD1{MD62O|U3KM7:TR?= MWXTRW5ITVJ?
LU-134-A MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrSSY1KSzVyPUKwMlcxPTZizszN M4TBWXNCVkeHUh?=
TE-12 MlfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTJyLkeyNFEh|ryP NY\6VoVuW0GQR1XS
MOLT-4 NV;yT2YxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TVTWlEPTB;MkGuNVkyPSEQvF2= NGLNVHpUSU6JRWK=
IGR-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1WzNmlEPTB;MkGuN|c6PiEQvF2= MX\TRW5ITVJ?
HOP-92 MkDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTJzLkS5PFch|ryP NITnSY1USU6JRWK=
SK-MES-1 M2jIZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXIWJhSUUN3ME2yNU44OzhzIN88US=> MVjTRW5ITVJ?
LU-65 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXoTIVxUUN3ME2yNU45PjJ2IN88US=> MXLTRW5ITVJ?
MS-1 NE\VdVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTJ{LkGyNFMh|ryP NILqVXhUSU6JRWK=
LoVo MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTJ{LkK0OEDPxE1? M4jWT3NCVkeHUh?=
A704 NFTzOWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3MO2ZwUUN3ME2yNk42OTV3IN88US=> NFGzNpZUSU6JRWK=
HT-1376 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXiTWM2OD1{Mj62NFU6KM7:TR?= NGPpfmVUSU6JRWK=
IST-MEL1 NYT6V49RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13oVGlEPTB;MkKuOlc2OSEQvF2= NEjVe2NUSU6JRWK=
Ramos-2G6-4C10 NHHZVGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTJ{LkezOlYh|ryP NVLvO4dsW0GQR1XS
T47D MoHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmT3TWM2OD1{Mj63PVc6KM7:TR?= NYOyTmN3W0GQR1XS
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LB2518-MEL MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{G5T2lEPTB;MkOuOlQyOiEQvF2= Mlv5V2FPT0WU
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SK-NEP-1 NGTLUIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTJ2Lki3OFQh|ryP MXrTRW5ITVJ?
NCI-H526 M3j6SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTJ3LkCwNlMh|ryP NICwS|JUSU6JRWK=
IST-SL1 M17JT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTJ3LkK3OVEh|ryP MofuV2FPT0WU
HH NEfYTmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXUTWM2OD1{NT6zNVkzKM7:TR?= MUjTRW5ITVJ?
NCI-H82 Ml;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPj[|ZMUUN3ME2yOU46OzhizszN M1;SNHNCVkeHUh?=
SNU-449 MlPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;iWWlEPTB;MkeuNlAyQCEQvF2= NHL0SWJUSU6JRWK=
COR-L23 NVzFZZBbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLve|ZKSzVyPUK3MlI5OTNizszN NWr6NJRiW0GQR1XS
LOXIMVI M2nEfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXj3OnZUUUN3ME2yO{4{PjhizszN MYHTRW5ITVJ?
GR-ST NWLiZow5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnENWJwUUN3ME2yO{43PzB4IN88US=> MUXTRW5ITVJ?
NCI-SNU-1 M4j0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonOTWM2OD1{Nz65OFQh|ryP MkjUV2FPT0WU
ALL-PO NHnWdGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG[5T29KSzVyPUK4MlE3ODRizszN NEfTbVBUSU6JRWK=
ML-2 M{TtS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLMN4VpUUN3ME2yPE4zQDF2IN88US=> NX21No1HW0GQR1XS
HOP-62 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3i5NWlEPTB;MkiuO|E{KM7:TR?= Mmj2V2FPT0WU
EGI-1 MlL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfvelRKSzVyPUK4Mlg5PDVizszN NVmwfXQxW0GQR1XS
TCCSUP MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUS3R3d3UUN3ME2yPE46Ojd{IN88US=> M1POXHNCVkeHUh?=
LB996-RCC MoDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoH4TWM2OD1{OT61OlgzKM7:TR?= NIDNN|RUSU6JRWK=
LCLC-97TM1 MkfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;5OGlEPTB;M{KuNVk3PCEQvF2= MoLTV2FPT0WU
NCI-H1304 MnOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTITWM2OD1|Mj6zN|AyKM7:TR?= MXnTRW5ITVJ?
KP-N-YS MnvFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\0eWlEPTB;M{KuOVk4OyEQvF2= NHG3Zm5USU6JRWK=
NCI-H1770 MnnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULzT2pbUUN3ME2zN{4yPjR6IN88US=> M1jWTHNCVkeHUh?=
EM-2 M{HYd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HrcmlEPTB;M{OuOlUxPCEQvF2= MnPFV2FPT0WU
ChaGo-K-1 Mki5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvLOnJPUUN3ME2zN{44OjN4IN88US=> NFfTUmhUSU6JRWK=
ACHN M3K4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLrTWM2OD1|Mz64N|g2KM7:TR?= NHG1TZdUSU6JRWK=
MN-60 M4nqfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLUTWM2OD1|Mz64OVQ1KM7:TR?= MVXTRW5ITVJ?
EW-18 NF[z[|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PyU2lEPTB;M{OuPFk4OSEQvF2= NFfkSJFUSU6JRWK=
KGN NVi0ZmV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTN3LkeyPVIh|ryP M3z2S3NCVkeHUh?=
U031 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXnToxKSzVyPUO1MlgyOzJizszN MoLKV2FPT0WU
HMV-II MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTN4LkC3O|Qh|ryP M{TWfHNCVkeHUh?=
L-363 NWPud4ZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLFTWM2OD1|Nz62OFU2KM7:TR?= NIrobW9USU6JRWK=
NCI-H1155 Ml[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG[1N|NKSzVyPUO4MlAxOTVizszN MUTTRW5ITVJ?
NCI-H1793 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXL2S|BbUUN3ME2zPE4yODJ4IN88US=> MXLTRW5ITVJ?
P30-OHK Ml;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXMTWM2OD1|OD6xN|MzKM7:TR?= NV\aOlh4W0GQR1XS
AN3-CA NWTYTW55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTN6LkG2NVUh|ryP NI\DRolUSU6JRWK=
UACC-257 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjJUJc6UUN3ME2zPE44QSEQvF2= NITCW2JUSU6JRWK=
MCF7 M325W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\WTWM2OD1|OT64OlI6KM7:TR?= MkjuV2FPT0WU
KP-N-YN NFrBVnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\YdmlEPTB;NECuOFI5PSEQvF2= MnHNV2FPT0WU
T98G MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LvR2lEPTB;NECuOFk2PyEQvF2= NF7zeFRUSU6JRWK=
HGC-27 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLSTWM2OD12Mz6yO|Qh|ryP NUL5PW03W0GQR1XS
NCI-H1092 NHXCd3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjOU2VXUUN3ME20N{4zQDl3IN88US=> M4nORnNCVkeHUh?=
KARPAS-299 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVH6fGNoUUN3ME20N{4{ODdzIN88US=> M{HWfnNCVkeHUh?=
LB1047-RCC M4Sxc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7ubnVKSzVyPUS0Mlk6PTlizszN NFXOTVBUSU6JRWK=
786-0 NIDmU3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXBT4hKSzVyPUS1MlY2KM7:TR?= MXvTRW5ITVJ?
HCC2157 NYTwS401T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTR4LkCzOVkh|ryP NXfVNVdHW0GQR1XS
NY NIq0VGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrzNVlKSzVyPUS2MlE4PzhizszN NIrZZ5pUSU6JRWK=
EFM-19 M13ZbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zO[WlEPTB;NE[uO|U{OyEQvF2= NVPucohDW0GQR1XS
EW-16 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vWVmlEPTB;NE[uO|gxPiEQvF2= MonsV2FPT0WU
UM-UC-3 MlT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYe1cJpYUUN3ME20Ok45ODV7IN88US=> NV;TW|NQW0GQR1XS
HT-29 NUfCZZk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTR5Lki3PVIh|ryP NF\6PVBUSU6JRWK=
LN-405 NYX0d2hPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWWyNXhzUUN3ME20PE4xQDJ5IN88US=> NHjnc2xUSU6JRWK=
NCI-H727 M4LIVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnRTWM2OD12OD63O|I3KM7:TR?= M2j0U3NCVkeHUh?=
D-502MG MkH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PiU2lEPTB;NEiuPVY4PiEQvF2= M1;WenNCVkeHUh?=
GMS-10 NYHLOWpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTR7LkK5O|Qh|ryP M3jDPXNCVkeHUh?=
MEL-JUSO Ml3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rRNmlEPTB;NEmuN|Q4KM7:TR?= M2iwTHNCVkeHUh?=

... 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
In vivo 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]

Protocol

Kinase Assay:[1]
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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.
Cell Research:[1]
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  • Cell lines: COLO205, A375, WM2664, COLO829, HT716, SW620, H460, Calu-6, HCT116, SK-MEL2, SK-MEL3, Lovo, H1299, 1205Lu, and C8161 cells
  • Concentrations: Dissolved in DMSO, final concentrations ~1 mM
  • Incubation Time: 24, 48, and 72 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Female athymic mice (NCr nu/nu) implanted s.c. with COLO205 cells, and SCID mice with 1205Lu or C8161 cells
  • Dosages: 5, 20, or 100 mg/kg
  • Administration: Oral gavage once or twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL (200.56 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+50% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/mL

* 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.

Chemical Information

Molecular Weight 413.83
Formula

C17H14ClF2N3O3S

CAS No. 918505-84-7
Storage powder
in solvent
Synonyms N/A
Smiles CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=C2C=C(C=N3)Cl)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    What would you recommend to make working solution for intraperitoneal injection into mice?

  • Answer:

    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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID