PLX-4720

Catalog No.S1152

PLX-4720 Chemical Structure

Molecular Weight(MW): 413.83

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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In DMSO USD 156 In stock
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USD 270 In stock
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Cited by 63 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 MnXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTBwMEe0OVch|ryP MUDTRW5ITVJ?
EoL-1-cell NIWzflBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPzTWM2OD1yLkG0NVY3KM7:TR?= M2myRXNCVkeHUh?=
C32 NVO5XGJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M165eGlEPTB;MD6xOVE{OSEQvF2= NUO3Sm8yW0GQR1XS
M14 NFzGd|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfjV4N6UUN3ME2wMlIyPzV5IN88US=> NIPITXVUSU6JRWK=
CP50-MEL-B NGDBPWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LOZmlEPTB;MD6yPVc5PCEQvF2= MVjTRW5ITVJ?
A101D MlT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPYTWM2OD1yLkOyOVg6KM7:TR?= NF\4PJNUSU6JRWK=
G-361 M2f4UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvYTWM2OD1yLkO0OlM4KM7:TR?= MkTlV2FPT0WU
HT-144 NH3vdYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnGUYdiUUN3ME2wMlM3OzJ7IN88US=> NYXibnNMW0GQR1XS
ACN MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzHd4xUUUN3ME2wMlM5PDd5IN88US=> MX3TRW5ITVJ?
COLO-829 M2GwfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX3ZWJiUUN3ME2wMlM5QTZ6IN88US=> M3X0ZnNCVkeHUh?=
MEL-HO MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rSNWlEPTB;MD60NVE4QSEQvF2= M4\OWHNCVkeHUh?=
SH-4 M4\ZZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXX4eoJbUUN3ME2wMlQyPDJ{IN88US=> MUHTRW5ITVJ?
SK-MEL-3 NFnsfWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXnTnRKSzVyPUCuOVE2PjhizszN MnnKV2FPT0WU
A375 NI[3fWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrKfo1KSzVyPUCuOlc{PTlizszN NHv0SnVUSU6JRWK=
MMAC-SF NIDkdZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{X3XWlEPTB;MD62PFYyPCEQvF2= MYTTRW5ITVJ?
BHT-101 NGXoWYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDzOXlmUUN3ME2wMlcxPzB{IN88US=> M2PXbnNCVkeHUh?=
K5 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M365fGlEPTB;MD63OlE1QCEQvF2= MWrTRW5ITVJ?
BV-173 MnLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HIOGlEPTB;MD63PVY1PCEQvF2= MnPCV2FPT0WU
RVH-421 NXzIUHpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLGbm9EUUN3ME2wMlg3Pzl4IN88US=> M2rufnNCVkeHUh?=
HCC2218 Ml;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnQcYNKSzVyPUCuPFc5PDRizszN M2H2TXNCVkeHUh?=
WM-115 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTBwOEi2PVIh|ryP M{LHWnNCVkeHUh?=
SK-MEL-28 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPYZ2FYUUN3ME2xMlA1PTZ7IN88US=> NIX1NY9USU6JRWK=
COLO-679 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7jbHN[UUN3ME2xMlExPDZ2IN88US=> MnzkV2FPT0WU
MZ7-mel NVrVVWhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWW1c4R2UUN3ME2xMlE1QTZ|IN88US=> NUnsTZE6W0GQR1XS
SK-MEL-30 NHjlZWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTFwM{OzPFYh|ryP NInkOo5USU6JRWK=
NCI-H209 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHraR5VKSzVyPUGuOlA5PiEQvF2= M12wTnNCVkeHUh?=
HTC-C3 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzZTWM2OD1zLk[2Nlk1KM7:TR?= M1\HVHNCVkeHUh?=
KARPAS-45 M3K3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLIZ5dQUUN3ME2yMlA1QTd6IN88US=> NIf6SmRUSU6JRWK=
NCI-SNU-5 NUnyRot6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTJwMUG5Olkh|ryP NXS2cFJ1W0GQR1XS
KP-4 MlPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVP4[4x5UUN3ME2yMlMxPzh5IN88US=> NIXUSoZUSU6JRWK=
PA-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrVWpN1UUN3ME2yMlczPjd|IN88US=> M4HtPXNCVkeHUh?=
HuO-3N1 MmfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTXTWM2OD1{Lki3PVQ3KM7:TR?= NYW3XmI4W0GQR1XS
NCI-H358 NYK5eVd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\PTWM2OD1{LkmyNlMzKM7:TR?= NY\VRXZrW0GQR1XS
CTB-1 MmLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\VdGlEPTB;Mz60NFE4PiEQvF2= Moe0V2FPT0WU
697 MnfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnQcG5KSzVyPUOuOVUzPjZizszN MXvTRW5ITVJ?
CP66-MEL MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2C1XWlEPTB;ND6xOVkzPyEQvF2= M2nBbXNCVkeHUh?=
NB13 NIfsU5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\QbIpnUUN3ME20MlQ6OTd7IN88US=> M3LycHNCVkeHUh?=
DBTRG-05MG NILnR4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fBdWlEPTB;ND61N|MzPSEQvF2= M3;RXnNCVkeHUh?=
A2058 MmDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\XTWhKSzVyPUSuO|IyPjRizszN MXLTRW5ITVJ?
KG-1 M2jVbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jVVGlEPTB;ND63N|kxQCEQvF2= Moi0V2FPT0WU
8305C Mon0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXnTWM2OD13LkG4O|Mh|ryP MkK5V2FPT0WU
RPMI-7951 M4fDe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M361VGlEPTB;NT64NFI5OyEQvF2= NX;pc|diW0GQR1XS
CHL-1 NHHaV41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTVwOUe2NFMh|ryP MV3TRW5ITVJ?
TI-73 NVrDcFNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHTUZVKSzVyPU[uNFA6ODJizszN M1S2VXNCVkeHUh?=
HT-1080 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTZwMUC5OFYh|ryP NV7zOmtZW0GQR1XS
ES5 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXzTFhlUUN3ME22MlE1QTJ2IN88US=> NH:0NGdUSU6JRWK=
8-MG-BA M4DwVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTZwMUixNlkh|ryP MU\TRW5ITVJ?
NB7 M2jBXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3GPZFrUUN3ME22MlIyOzd|IN88US=> NX74VVdmW0GQR1XS
H4 NFfkcmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXUTWM2OD14LkKyOFk{KM7:TR?= NGXIRoRUSU6JRWK=
CAL-72 NYPCUY52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;ITWM2OD14LkS1OFI{KM7:TR?= MW\TRW5ITVJ?
HCC1806 M1XJOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XNR2lEPTB;Nj64NVk{OSEQvF2= NWPvPGZuW0GQR1XS
BCPAP NUPKOJRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzMU2RKSzVyPUeuNlE4PjRizszN MYfTRW5ITVJ?
LB2241-RCC MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fvNGlEPTB;Nz6zOlkxPyEQvF2= MV3TRW5ITVJ?
COLO-741 NVnpcWF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRThwMEG2O|kh|ryP NVnUSXdNW0GQR1XS
HSC-3 M1GxdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLvTWM2OD16LkC3NFY5KM7:TR?= NWKzRpI{W0GQR1XS
SW982 NVjCR|NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDmbZdKSzVyPUiuOFE2OTZizszN M{SwUHNCVkeHUh?=
GCT M1nhOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRThwN{WzNVQh|ryP NFXYR2xUSU6JRWK=
KY821 NWrQcoFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHWzZ|dKSzVyPUmuNFUyPzhizszN M1\PU3NCVkeHUh?=
JVM-3 NXzxeJhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTsPFdoUUN3ME25MlU3QTl7IN88US=> NV3JTWFuW0GQR1XS
RS4-11 MkGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPrTWM2OD17Lk[wOFgh|ryP M2WxV3NCVkeHUh?=
VA-ES-BJ NUD6OYVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Tzc2lEPTB;MUCuNFE1QSEQvF2= M3zHcHNCVkeHUh?=
A431 M{XTcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HqWGlEPTB;MUCuOFIyOiEQvF2= MWrTRW5ITVJ?
LXF-289 M1HPbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTFyLkS1PEDPxE1? M{TJRnNCVkeHUh?=
SK-MEL-24 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTFyLkiyO|Qh|ryP MVTTRW5ITVJ?
NOS-1 M17wbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTFyLki0O|Ih|ryP NXHKN5pzW0GQR1XS
KNS-62 M4X0Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1faWGlEPTB;MUGuNlQxPCEQvF2= MWjTRW5ITVJ?
SK-HEP-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfk[4NKSzVyPUGxMlM2OjdizszN MmjlV2FPT0WU
A3-KAW M{nvUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTFzLkexO|gh|ryP MUTTRW5ITVJ?
SK-LU-1 NGLPR4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTF{LkK2OVUh|ryP Mn;3V2FPT0WU
TYK-nu NHzx[ZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfoR45KSzVyPUGyMlM6OzJizszN NGe3XWNUSU6JRWK=
NMC-G1 NFjhbmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXMTWM2OD1zMj62NFYzKM7:TR?= NXm5SZBJW0GQR1XS
BB65-RCC MkXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnKS2F7UUN3ME2xNk44OTZ7IN88US=> NYD2OJoxW0GQR1XS
QIMR-WIL MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTF{Lki4N|Mh|ryP MV\TRW5ITVJ?
D-566MG NIPhTHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnxTYxuUUN3ME2xN{46PTd4IN88US=> M3\OW3NCVkeHUh?=
KYSE-140 NGjBb5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\uTWM2OD1zND6wO|U{KM7:TR?= M2LJNXNCVkeHUh?=
SCC-4 NWXjU3o2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzITWM2OD1zND6zN|U6KM7:TR?= NIPqSWlUSU6JRWK=
U251 NFHoSmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTF2Lki0PVIh|ryP NVjufHpQW0GQR1XS
D-542MG MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nXSGlEPTB;MUSuPVIzOiEQvF2= M3[wWnNCVkeHUh?=
LAMA-84 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPQZm14UUN3ME2xOE46QTN{IN88US=> NXj0b|F{W0GQR1XS
NCI-H720 Mn60S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTF3LkK2PFQh|ryP NHTzPVdUSU6JRWK=
DEL M3zUbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknnTWM2OD1zNT60Nlk{KM7:TR?= M3PWdHNCVkeHUh?=
SBC-1 NY\TZ2xpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnmwTWM2OD1zNT60N|A2KM7:TR?= MUnTRW5ITVJ?
ECC10 M4DRV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLuTWM2OD1zNT60OFU5KM7:TR?= MlLiV2FPT0WU
Daoy NEDqc2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlm0TWM2OD1zNT63OlE3KM7:TR?= MoHEV2FPT0WU
SCH NFOxbnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTF3Lke4N|Uh|ryP MkfWV2FPT0WU
MZ2-MEL MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTF4LkC2OFYh|ryP NVjYd2l{W0GQR1XS
CAL-12T NWruS|Z5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTF4LkS4OlIh|ryP MULTRW5ITVJ?
KE-37 MoPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYGxVVZjUUN3ME2xOk45OTB5IN88US=> M2rKSXNCVkeHUh?=
LS-411N NY\HTlc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTF5LkGxPEDPxE1? M1z3NnNCVkeHUh?=
NCI-H2228 M1S3Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTF5LkOwO|Eh|ryP NFvXd3pUSU6JRWK=
SK-MEL-2 Mn3rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHOdIVKSzVyPUG3MlQ6PjVizszN M13jV3NCVkeHUh?=
HN MljaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWm4OGJxUUN3ME2xO{44OjR6IN88US=> M1TCfXNCVkeHUh?=
NCI-H1648 NHzOOIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTF5LkixPEDPxE1? M4j6ZnNCVkeHUh?=
IA-LM M4ftb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTF6LkOxO|Ih|ryP M{LacHNCVkeHUh?=
EW-13 M4i2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LsXGlEPTB;MUiuOVcxQCEQvF2= NGHxfHZUSU6JRWK=
YKG-1 MkfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjGZlhKSzVyPUG5MlU4OTFizszN M4XkPXNCVkeHUh?=
KNS-81-FD NUO5OY9XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrrUJlKSzVyPUG5MlU5PThizszN MWPTRW5ITVJ?
23132-87 NH2wSWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PvW2lEPTB;MUmuO|Y1OiEQvF2= NYTRVW1PW0GQR1XS
NUGC-3 NG\aVFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ry[WlEPTB;MUmuPVg5PyEQvF2= MVfTRW5ITVJ?
5637 NEnwSHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTJyLkC0O|gh|ryP NXrsXVl7W0GQR1XS
NCI-H1755 M{\SNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTJyLkS3OlQh|ryP NVfURnV4W0GQR1XS
RH-18 NWDCXYtoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1L6ZmlEPTB;MkCuOVc1QCEQvF2= NV3vUXE1W0GQR1XS
RXF393 NH3xVolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvhTWM2OD1{MD62O|U3KM7:TR?= NEnkPJNUSU6JRWK=
LU-134-A M1[0b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTJyLkewOVYh|ryP M17QUXNCVkeHUh?=
TE-12 Mk\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIK1dHNKSzVyPUKwMlczODFizszN NF\ZS3hUSU6JRWK=
MOLT-4 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLPTWM2OD1{MT6xPVE2KM7:TR?= M3vRPHNCVkeHUh?=
IGR-1 MmXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTJzLkO3PVYh|ryP NEfPRYRUSU6JRWK=
HOP-92 MnjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjLeVl1UUN3ME2yNU41QTh5IN88US=> NF7j[21USU6JRWK=
SK-MES-1 NXvX[WhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nQTmlEPTB;MkGuO|M5OSEQvF2= M4S1eXNCVkeHUh?=
LU-65 NXLWS3NsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPDdGxLUUN3ME2yNU45PjJ2IN88US=> NWDkcVY2W0GQR1XS
MS-1 M1fPeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{j0cWlEPTB;MkKuNVIxOyEQvF2= MkX2V2FPT0WU
LoVo MlfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTJ{LkK0OEDPxE1? M1[wVnNCVkeHUh?=
A704 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nOVmlEPTB;MkKuOVE2PSEQvF2= M3uxSHNCVkeHUh?=
HT-1376 NEfSeGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTJ{Lk[wOVkh|ryP M2LrPXNCVkeHUh?=
IST-MEL1 NIDodYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmq2TWM2OD1{Mj62O|UyKM7:TR?= NVPVeYVEW0GQR1XS
Ramos-2G6-4C10 M{jvW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTJ{LkezOlYh|ryP NGC5cpdUSU6JRWK=
T47D NEL4W5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLOfnZKSzVyPUKyMlc6PzlizszN MVTTRW5ITVJ?
HT-1197 NEO2eVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zKZ2lEPTB;MkOuNFgyPyEQvF2= MV\TRW5ITVJ?
LB2518-MEL MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfJVVlKSzVyPUKzMlY1OTJizszN NHL5OlZUSU6JRWK=
J-RT3-T3-5 MkjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPnSVJKSzVyPUK0Mlc2QTVizszN MoDMV2FPT0WU
SK-NEP-1 MorqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTJ2Lki3OFQh|ryP NIXHbGRUSU6JRWK=
NCI-H526 NXTSdYhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPER2pKSzVyPUK1MlAxOjNizszN Mo\iV2FPT0WU
IST-SL1 NELZNYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkH5TWM2OD1{NT6yO|UyKM7:TR?= MnjUV2FPT0WU
HH NWLqWGNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTJ3LkOxPVIh|ryP NIK1[WRUSU6JRWK=
NCI-H82 MoXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HHdmlEPTB;MkWuPVM5KM7:TR?= M17JUHNCVkeHUh?=
SNU-449 Mk\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfhZYZqUUN3ME2yO{4zODF6IN88US=> Mn33V2FPT0WU
COR-L23 M{XPeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTJ5LkK4NVMh|ryP MnHhV2FPT0WU
LOXIMVI NUP6Z4xVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTJ5LkO2PEDPxE1? NGfROY5USU6JRWK=
GR-ST M2XGU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPOZ|hJUUN3ME2yO{43PzB4IN88US=> NWDW[Vg5W0GQR1XS
NCI-SNU-1 MnrJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDIWWlKSzVyPUK3Mlk1PCEQvF2= M1zGNHNCVkeHUh?=
ALL-PO MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEi2WoxKSzVyPUK4MlE3ODRizszN NHHNVmNUSU6JRWK=
ML-2 NFrSOnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTJ6LkK4NVQh|ryP MWfTRW5ITVJ?
HOP-62 NIf5SoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Prb2lEPTB;MkiuO|E{KM7:TR?= M4nDSXNCVkeHUh?=
EGI-1 M2nv[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJ6Lki4OFUh|ryP MVLTRW5ITVJ?
TCCSUP MlzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{m4RmlEPTB;MkiuPVI4OiEQvF2= NFHCR2VUSU6JRWK=
LB996-RCC NHrv[WRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TwWmlEPTB;MkmuOVY5OiEQvF2= MoP0V2FPT0WU
LCLC-97TM1 NELvOohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLtTWM2OD1|Mj6xPVY1KM7:TR?= MWLTRW5ITVJ?
NCI-H1304 M{jBWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{e0NGlEPTB;M{KuN|MxOSEQvF2= NEjndGdUSU6JRWK=
KP-N-YS MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXHRVhVUUN3ME2zNk42QTd|IN88US=> MWDTRW5ITVJ?
NCI-H1770 NVXyNVg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGH6XWdKSzVyPUOzMlE3PDhizszN NHHLXGFUSU6JRWK=
EM-2 NInqWmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEH6ZmtKSzVyPUOzMlY2ODRizszN NFXx[JJUSU6JRWK=
ChaGo-K-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjYdXNKSzVyPUOzMlczOzZizszN MmDWV2FPT0WU
ACHN MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn74TWM2OD1|Mz64N|g2KM7:TR?= M2HhVnNCVkeHUh?=
MN-60 NWj4bJpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDUeIU6UUN3ME2zN{45PTR2IN88US=> M{nlbXNCVkeHUh?=
EW-18 Mne3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrJTWM2OD1|Mz64PVcyKM7:TR?= NX3PZ4c1W0GQR1XS
KGN MlfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnHTWM2OD1|NT63NlkzKM7:TR?= NHvwXYdUSU6JRWK=
U031 NH3Y[VJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEH6XYpKSzVyPUO1MlgyOzJizszN NYrUOlVvW0GQR1XS
HMV-II NXTwdpA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTN4LkC3O|Qh|ryP NX;ZRpFiW0GQR1XS
L-363 MmLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\mSVRKSzVyPUO3MlY1PTVizszN NF3XRXVUSU6JRWK=
NCI-H1155 MoHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfKTWM2OD1|OD6wNFE2KM7:TR?= Mn\nV2FPT0WU
NCI-H1793 M3m0Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TNe2lEPTB;M{iuNVAzPiEQvF2= NEj4[lhUSU6JRWK=
P30-OHK M2LK[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PUcWlEPTB;M{iuNVM{OiEQvF2= MU\TRW5ITVJ?
AN3-CA M4DRcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTN6LkG2NVUh|ryP M4[wUHNCVkeHUh?=
UACC-257 NYHSWZJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjiTII1UUN3ME2zPE44QSEQvF2= M3HXUHNCVkeHUh?=
MCF7 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPuN3g6UUN3ME2zPU45PjJ7IN88US=> M1TZWHNCVkeHUh?=
KP-N-YN MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIf4XZRKSzVyPUSwMlQzQDVizszN MYTTRW5ITVJ?
T98G Ml7GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTRyLkS5OVch|ryP MnG5V2FPT0WU
HGC-27 NIG2foRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHWTWM2OD12Mz6yO|Qh|ryP NYDHSYFSW0GQR1XS
NCI-H1092 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1W5SmlEPTB;NEOuNlg6PSEQvF2= MWrTRW5ITVJ?
KARPAS-299 M1PIWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPyT45KSzVyPUSzMlMxPzFizszN NWTl[HhUW0GQR1XS
LB1047-RCC MojQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTR2Lkm5OVkh|ryP NIDKSHlUSU6JRWK=
786-0 M1S0V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XBW2lEPTB;NEWuOlUh|ryP NGSwNlFUSU6JRWK=
HCC2157 NEXZcWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HHe2lEPTB;NE[uNFM2QSEQvF2= MXLTRW5ITVJ?
NY MknpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYn5WFRHUUN3ME20Ok4yPzd6IN88US=> NYDoPVl{W0GQR1XS
EFM-19 M1rKXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfiW5lsUUN3ME20Ok44PTN|IN88US=> NH7xdlJUSU6JRWK=
EW-16 MkTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTR4Lke4NFYh|ryP MoX3V2FPT0WU
UM-UC-3 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTR4LkiwOVkh|ryP M4DaUnNCVkeHUh?=
HT-29 NVP3SppIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTR5Lki3PVIh|ryP Mk[yV2FPT0WU
LN-405 MmDhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXsZWRKSzVyPUS4MlA5OjdizszN NXH6UJJuW0GQR1XS
NCI-H727 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYCzO25VUUN3ME20PE44PzJ4IN88US=> NGqwbVlUSU6JRWK=
D-502MG M1\lW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13vd2lEPTB;NEiuPVY4PiEQvF2= NWH6XZZTW0GQR1XS
GMS-10 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnKWXFvUUN3ME20PU4zQTd2IN88US=> MlHuV2FPT0WU
MEL-JUSO M3vydWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17oUmlEPTB;NEmuN|Q4KM7:TR?= MY\TRW5ITVJ?

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Female athymic mice (NCr nu/nu) implanted s.c. with COLO205 cells, and SCID mice with 1205Lu or C8161 cells
  • Formulation: Suspended in vehicle (5% DMSO, 1% methylcellulose)
  • 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

Bio Calculators

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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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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.

Raf Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID