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 97 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 NFTlb5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NESwOVVKSzVyPUCuNFc1PTdizszN Mnr4V2FPT0WU
EoL-1-cell MljBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTNTWM2OD1yLkG0NVY3KM7:TR?= NV3RNnNTW0GQR1XS
C32 NIDj[4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTBwMUWxN|Eh|ryP NHfQVXBUSU6JRWK=
M14 M4HlRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGi5VJRKSzVyPUCuNlE4PTdizszN MoDtV2FPT0WU
CP50-MEL-B NUj2U2RjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;nTWM2OD1yLkK5O|g1KM7:TR?= NHuyNYtUSU6JRWK=
A101D NILmdZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3wN4RCUUN3ME2wMlMzPTh7IN88US=> M36xV3NCVkeHUh?=
G-361 MmDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFT3No1KSzVyPUCuN|Q3OzdizszN NHW1[nVUSU6JRWK=
HT-144 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTBwM{[zNlkh|ryP M4HP[nNCVkeHUh?=
ACN M4jx[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwM{i0O|ch|ryP MVnTRW5ITVJ?
COLO-829 Mn6zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\vS3ZKSzVyPUCuN|g6PjhizszN NI[5cVVUSU6JRWK=
MEL-HO NUfIWmpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTBwNEGxO|kh|ryP NVnx[pU1W0GQR1XS
SH-4 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnMTWM2OD1yLkSxOFIzKM7:TR?= MWXTRW5ITVJ?
SK-MEL-3 M1nNc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fsRWlEPTB;MD61NVU3QCEQvF2= NEHqV4pUSU6JRWK=
A375 NH\xeHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTBwNkezOVkh|ryP M4m2PHNCVkeHUh?=
MMAC-SF MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\IS2xKSzVyPUCuOlg3OTRizszN NX;XSohRW0GQR1XS
BHT-101 MmDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlS1TWM2OD1yLkewO|AzKM7:TR?= NXrW[Y5SW0GQR1XS
K5 M13RXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DlVmlEPTB;MD63OlE1QCEQvF2= MlvxV2FPT0WU
BV-173 M3LI[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTzbmdYUUN3ME2wMlc6PjR2IN88US=> NHe5TlZUSU6JRWK=
RVH-421 NXTZb2ZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\POXdjUUN3ME2wMlg3Pzl4IN88US=> NIewW2lUSU6JRWK=
HCC2218 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7VS|VKSzVyPUCuPFc5PDRizszN M2ruenNCVkeHUh?=
WM-115 M1fq[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1u2PWlEPTB;MD64PFY6OiEQvF2= M{TieXNCVkeHUh?=
SK-MEL-28 Mm[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFGzZXhKSzVyPUGuNFQ2PjlizszN NYXnb|drW0GQR1XS
COLO-679 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXwXFFKSzVyPUGuNVA1PjRizszN NFj1eXJUSU6JRWK=
MZ7-mel NYrseWdUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\GOZhKSzVyPUGuNVQ6PjNizszN NWHsUHlDW0GQR1XS
SK-MEL-30 M2\zU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2m2b2lEPTB;MT6zN|M5PiEQvF2= MlfTV2FPT0WU
NCI-H209 NFHJdGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HFRWlEPTB;MT62NFg3KM7:TR?= NVzVZ4FFW0GQR1XS
HTC-C3 Ml;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LIe2lEPTB;MT62OlI6PCEQvF2= Mnu2V2FPT0WU
KARPAS-45 M{fFW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTJwMES5O|gh|ryP NYXpeW9sW0GQR1XS
NCI-SNU-5 M1jCb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4O4PGlEPTB;Mj6xNVk3QSEQvF2= MoDMV2FPT0WU
KP-4 NX3SdGJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3lTWM2OD1{LkOwO|g4KM7:TR?= M13rVHNCVkeHUh?=
PA-1 MnPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWT3VYF[UUN3ME2yMlczPjd|IN88US=> M{Dp[3NCVkeHUh?=
HuO-3N1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTJwOEe5OFYh|ryP NXrLWZNLW0GQR1XS
NCI-H358 NVHIT2RPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\zeY9KSzVyPUKuPVIzOzJizszN MVLTRW5ITVJ?
CTB-1 NEXHWWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LYW2lEPTB;Mz60NFE4PiEQvF2= MnPVV2FPT0WU
697 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vGemlEPTB;Mz61OVI3PiEQvF2= NXjtbWFTW0GQR1XS
CP66-MEL MkXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTRwMUW5Nlch|ryP MkX4V2FPT0WU
NB13 NVLBRXN5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTRwNEmxO|kh|ryP NX;6PYlbW0GQR1XS
DBTRG-05MG NIfNUYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXLV29uUUN3ME20MlU{OzJ3IN88US=> MoTnV2FPT0WU
A2058 M2P3Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;Ud4FmUUN3ME20MlczOTZ2IN88US=> NFW4bIxUSU6JRWK=
KG-1 NXnGcmhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\nWWlEPTB;ND63N|kxQCEQvF2= M{PxUnNCVkeHUh?=
8305C NWHFNG9ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljiTWM2OD13LkG4O|Mh|ryP MlfjV2FPT0WU
RPMI-7951 MlfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrUeIxuUUN3ME21MlgxOjh|IN88US=> NIH5enVUSU6JRWK=
CHL-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;i[2lKSzVyPUWuPVc3ODNizszN NH;KXXNUSU6JRWK=
TI-73 NILmU45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTZwMEC5NFIh|ryP MWDTRW5ITVJ?
HT-1080 NHPmfYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTZwMUC5OFYh|ryP NV;yXINvW0GQR1XS
ES5 M3TNcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HVN2lEPTB;Nj6xOFkzPCEQvF2= M4[4THNCVkeHUh?=
8-MG-BA M2TIRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDkPGdKSzVyPU[uNVgyOjlizszN MneyV2FPT0WU
NB7 M2j3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rtZmlEPTB;Nj6yNVM4OyEQvF2= MYDTRW5ITVJ?
H4 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTZwMkK0PVMh|ryP Mk\BV2FPT0WU
CAL-72 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zJcWlEPTB;Nj60OVQzOyEQvF2= NWnuVYRFW0GQR1XS
HCC1806 M2LJNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LrN2lEPTB;Nj64NVk{OSEQvF2= MYjTRW5ITVJ?
BCPAP NHrzVHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DLOmlEPTB;Nz6yNVc3PCEQvF2= M4DlN3NCVkeHUh?=
LB2241-RCC MkO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTdwM{[5NFch|ryP MkftV2FPT0WU
COLO-741 MnTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HKZWlEPTB;OD6wNVY4QSEQvF2= M1[3UHNCVkeHUh?=
HSC-3 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfmOnNKSzVyPUiuNFcxPjhizszN NHvudXJUSU6JRWK=
SW982 Mo\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4r5NmlEPTB;OD60NVUyPiEQvF2= NFuzNGJUSU6JRWK=
GCT NYW5WJY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXMTFJKSzVyPUiuO|U{OTRizszN NUXHOlJpW0GQR1XS
KY821 M{\qbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYq1W2RLUUN3ME25MlA2OTd6IN88US=> M3H1dHNCVkeHUh?=
JVM-3 MlrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTlwNU[5PVkh|ryP NFfiUVJUSU6JRWK=
RS4-11 MoOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFH5foFKSzVyPUmuOlA1QCEQvF2= NVO4cnJ1W0GQR1XS
VA-ES-BJ NYfWd29[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TSb2lEPTB;MUCuNFE1QSEQvF2= M4TO[HNCVkeHUh?=
A431 Mne5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV20eoFxUUN3ME2xNE41OjF{IN88US=> M2D5XHNCVkeHUh?=
LXF-289 NX6ydoZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTFyLkS1PEDPxE1? MkO3V2FPT0WU
SK-MEL-24 M4nqb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTFyLkiyO|Qh|ryP NX3MVXptW0GQR1XS
NOS-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTOTWM2OD1zMD64OFczKM7:TR?= NGXKXVhUSU6JRWK=
KNS-62 MkfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrhXG9nUUN3ME2xNU4zPDB2IN88US=> MmK3V2FPT0WU
SK-HEP-1 MlLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPBTWM2OD1zMT6zOVI4KM7:TR?= NHfYfmJUSU6JRWK=
A3-KAW NVm2O2N6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvSTWM2OD1zMT63NVc5KM7:TR?= NV\Ge2I4W0GQR1XS
SK-LU-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rmPWlEPTB;MUKuNlY2PSEQvF2= NV;TNYhrW0GQR1XS
TYK-nu NGXLbJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXL6SFF4UUN3ME2xNk4{QTN{IN88US=> MmS1V2FPT0WU
NMC-G1 MlzYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTF{Lk[wOlIh|ryP MWrTRW5ITVJ?
BB65-RCC NWrITnZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rtVWlEPTB;MUKuO|E3QSEQvF2= M37QeXNCVkeHUh?=
QIMR-WIL M2rNfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTF{Lki4N|Mh|ryP M1\tU3NCVkeHUh?=
D-566MG MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1S3bWlEPTB;MUOuPVU4PiEQvF2= MUjTRW5ITVJ?
KYSE-140 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;xUJlKSzVyPUG0MlA4PTNizszN NGjyRotUSU6JRWK=
SCC-4 M3XwXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDBUFJKSzVyPUG0MlM{PTlizszN NHi1[nFUSU6JRWK=
U251 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLUVI9pUUN3ME2xOE45PDl{IN88US=> M17acnNCVkeHUh?=
D-542MG M1HxcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHNTWM2OD1zND65NlIzKM7:TR?= NFrpT25USU6JRWK=
LAMA-84 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7ZTWM2OD1zND65PVMzKM7:TR?= MlK3V2FPT0WU
NCI-H720 NX\qcWkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHPV|NsUUN3ME2xOU4zPjh2IN88US=> M3W5cHNCVkeHUh?=
DEL M3PnVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvmRmFKSzVyPUG1MlQzQTNizszN NF7wUFBUSU6JRWK=
SBC-1 NUHGd4l7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfQ[FZKSzVyPUG1MlQ{ODVizszN NHzxe5FUSU6JRWK=
ECC10 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTF3LkS0OVgh|ryP MmW0V2FPT0WU
Daoy NU\YcXJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjTTWM2OD1zNT63OlE3KM7:TR?= NF7BTHBUSU6JRWK=
SCH Mn32S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfUTWM2OD1zNT63PFM2KM7:TR?= MlTpV2FPT0WU
MZ2-MEL M1LYfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrkTWM2OD1zNj6wOlQ3KM7:TR?= M4HFcXNCVkeHUh?=
CAL-12T MkXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml6xTWM2OD1zNj60PFYzKM7:TR?= MYjTRW5ITVJ?
KE-37 NFz0V4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDWTWM2OD1zNj64NVA4KM7:TR?= MVvTRW5ITVJ?
LS-411N MoXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTF5LkGxPEDPxE1? NF7jcVlUSU6JRWK=
NCI-H2228 M1Tkemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\TNWpKSzVyPUG3MlMxPzFizszN MUfTRW5ITVJ?
SK-MEL-2 NGG2ZnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33wSmlEPTB;MUeuOFk3PSEQvF2= M4WxNXNCVkeHUh?=
HN MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TuW2lEPTB;MUeuO|I1QCEQvF2= M3fZbHNCVkeHUh?=
NCI-H1648 NXnlVGNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnHV5BDUUN3ME2xO{45OThizszN MkP5V2FPT0WU
IA-LM Mn74S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUS2VYgyUUN3ME2xPE4{OTd{IN88US=> NE\UNXRUSU6JRWK=
EW-13 NUT6UYVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zuXWlEPTB;MUiuOVcxQCEQvF2= NHPrcpBUSU6JRWK=
YKG-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\mVWlEPTB;MUmuOVcyOSEQvF2= M4LzWXNCVkeHUh?=
KNS-81-FD MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmWzTWM2OD1zOT61PFU5KM7:TR?= NWPvN2N5W0GQR1XS
23132-87 M{Hkdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXz0e3JOUUN3ME2xPU44PjR{IN88US=> M4XXWHNCVkeHUh?=
NUGC-3 MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3OelJKSzVyPUG5Mlk5QDdizszN M4W4VnNCVkeHUh?=
5637 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELU[4pKSzVyPUKwMlA1PzhizszN NEjwSIFUSU6JRWK=
NCI-H1755 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXiU|FwUUN3ME2yNE41PzZ2IN88US=> NXTtSm9kW0GQR1XS
RH-18 M1H6b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XhdWlEPTB;MkCuOVc1QCEQvF2= MUnTRW5ITVJ?
RXF393 Mnv4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LOUWlEPTB;MkCuOlc2PiEQvF2= MkHCV2FPT0WU
LU-134-A MljlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJyLkewOVYh|ryP MX7TRW5ITVJ?
TE-12 MmPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrtSI5KSzVyPUKwMlczODFizszN MoXpV2FPT0WU
MOLT-4 NGTMfWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTrZ4Y4UUN3ME2yNU4yQTF3IN88US=> NFHLUJpUSU6JRWK=
IGR-1 MnizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\JNIpKSzVyPUKxMlM4QTZizszN M1THWHNCVkeHUh?=
HOP-92 NHTPfI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnhWZZLUUN3ME2yNU41QTh5IN88US=> NY\oN|VxW0GQR1XS
SK-MES-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfhO2t4UUN3ME2yNU44OzhzIN88US=> MX;TRW5ITVJ?
LU-65 Mlz0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTnRpFXUUN3ME2yNU45PjJ2IN88US=> MmPnV2FPT0WU
MS-1 NID5XZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDsSHo1UUN3ME2yNk4yOjB|IN88US=> M3vMdnNCVkeHUh?=
LoVo NIGwcFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTJ{LkK0OEDPxE1? NY\UNWN6W0GQR1XS
A704 NFy2eHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJ{LkWxOVUh|ryP MXTTRW5ITVJ?
HT-1376 M13lRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfPV4VbUUN3ME2yNk43ODV7IN88US=> NVX5R|FwW0GQR1XS
IST-MEL1 MmXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PDdGlEPTB;MkKuOlc2OSEQvF2= M2CxW3NCVkeHUh?=
Ramos-2G6-4C10 NWrZbIhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTaTWM2OD1{Mj63N|Y3KM7:TR?= NYfkPGhpW0GQR1XS
T47D NV65T5FkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTZOHFKSzVyPUKyMlc6PzlizszN NI\acI9USU6JRWK=
HT-1197 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXWRVA4UUN3ME2yN{4xQDF5IN88US=> MW\TRW5ITVJ?
LB2518-MEL NYixcXh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGP5eJJKSzVyPUKzMlY1OTJizszN NHLYTVBUSU6JRWK=
J-RT3-T3-5 M2LPWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPwTWM2OD1{ND63OVk2KM7:TR?= MnzsV2FPT0WU
SK-NEP-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTvXXJKSzVyPUK0Mlg4PDRizszN M2\2U3NCVkeHUh?=
NCI-H526 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHJTWM2OD1{NT6wNFI{KM7:TR?= MlTDV2FPT0WU
IST-SL1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfjTWM2OD1{NT6yO|UyKM7:TR?= M3S5fnNCVkeHUh?=
HH MkX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJ3LkOxPVIh|ryP M2f6[3NCVkeHUh?=
NCI-H82 M4XCd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[0fopKSzVyPUK1Mlk{QCEQvF2= NFXHSJhUSU6JRWK=
SNU-449 M4Xwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPV[W9KSzVyPUK3MlIxOThizszN NX7j[m01W0GQR1XS
COR-L23 NIXvWodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\sTWM2OD1{Nz6yPFE{KM7:TR?= NXi2ZZBpW0GQR1XS
LOXIMVI MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTJ5LkO2PEDPxE1? M1vocHNCVkeHUh?=
GR-ST NVfscVU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXtUGRKSzVyPUK3MlY4ODZizszN NF;DdoxUSU6JRWK=
NCI-SNU-1 M2S4OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnZSmhKSzVyPUK3Mlk1PCEQvF2= MlztV2FPT0WU
ALL-PO M2rnfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrX[nhiUUN3ME2yPE4yPjB2IN88US=> NXTwZ2V7W0GQR1XS
ML-2 MkLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTLTWM2OD1{OD6yPFE1KM7:TR?= M17NTnNCVkeHUh?=
HOP-62 NFjWbWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XkXWlEPTB;MkiuO|E{KM7:TR?= MmfKV2FPT0WU
EGI-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLHcJM3UUN3ME2yPE45QDR3IN88US=> NGjKOGNUSU6JRWK=
TCCSUP MoLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XJO2lEPTB;MkiuPVI4OiEQvF2= NGnYSmdUSU6JRWK=
LB996-RCC NHrtNWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTJ7LkW2PFIh|ryP M1HsPHNCVkeHUh?=
LCLC-97TM1 NG\IWGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTN{LkG5OlQh|ryP MWrTRW5ITVJ?
NCI-H1304 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fvWWlEPTB;M{KuN|MxOSEQvF2= MYPTRW5ITVJ?
KP-N-YS NXH6NnpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTN{LkW5O|Mh|ryP NGDVSWZUSU6JRWK=
NCI-H1770 NYP5XVhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfXTWM2OD1|Mz6xOlQ5KM7:TR?= M1jJZXNCVkeHUh?=
EM-2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4r0RWlEPTB;M{OuOlUxPCEQvF2= NH\rS5NUSU6JRWK=
ChaGo-K-1 M3XqcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TMXmlEPTB;M{OuO|I{PiEQvF2= Mo\1V2FPT0WU
ACHN NVXFXGdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHpT3JKSzVyPUOzMlg{QDVizszN NYK5PWdLW0GQR1XS
MN-60 M1GyUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HiTWlEPTB;M{OuPFU1PCEQvF2= MVTTRW5ITVJ?
EW-18 M1rMUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLTTWM2OD1|Mz64PVcyKM7:TR?= MoPlV2FPT0WU
KGN MlzFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTN3LkeyPVIh|ryP NXzmd|NUW0GQR1XS
U031 NHHNTGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfM[pdKSzVyPUO1MlgyOzJizszN NV7afpp5W0GQR1XS
HMV-II NWDNbVVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moe2TWM2OD1|Nj6wO|c1KM7:TR?= MXHTRW5ITVJ?
L-363 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4e5fGlEPTB;M{euOlQ2PSEQvF2= M1fa[nNCVkeHUh?=
NCI-H1155 NIXxdINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTN6LkCwNVUh|ryP NYDxRoVmW0GQR1XS
NCI-H1793 M3;VO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDQdmVKSzVyPUO4MlExOjZizszN NH7RXW9USU6JRWK=
P30-OHK M3LT[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;wTWM2OD1|OD6xN|MzKM7:TR?= MYrTRW5ITVJ?
AN3-CA NGjBcW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\rfmlEPTB;M{iuNVYyPSEQvF2= NWn6SpdLW0GQR1XS
UACC-257 NH3qdVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;jVWFKSzVyPUO4Mlc6KM7:TR?= M4npN3NCVkeHUh?=
MCF7 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvGTWM2OD1|OT64OlI6KM7:TR?= M3ryXnNCVkeHUh?=
KP-N-YN NI\TeFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTRyLkSyPFUh|ryP NVHTTm93W0GQR1XS
T98G MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnaUXNzUUN3ME20NE41QTV5IN88US=> MUPTRW5ITVJ?
HGC-27 Moq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjjTWM2OD12Mz6yO|Qh|ryP MnTRV2FPT0WU
NCI-H1092 MmK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTR|LkK4PVUh|ryP MonNV2FPT0WU
KARPAS-299 NUnJdphPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzFNWtMUUN3ME20N{4{ODdzIN88US=> NYLUWGc6W0GQR1XS
LB1047-RCC NXnxOJI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHGOJFKSzVyPUS0Mlk6PTlizszN NELo[|VUSU6JRWK=
786-0 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVywc|VXUUN3ME20OU43PSEQvF2= NUfue5lJW0GQR1XS
HCC2157 NXrwV|FIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHIPYwyUUN3ME20Ok4xOzV7IN88US=> NEXQeW9USU6JRWK=
NY NF\vNVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPLTWM2OD12Nj6xO|c5KM7:TR?= NEC5dI5USU6JRWK=
EFM-19 NIjTZ4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYj4UGRzUUN3ME20Ok44PTN|IN88US=> MUDTRW5ITVJ?
EW-16 NFnNTlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mme5TWM2OD12Nj63PFA3KM7:TR?= NWT1XHBZW0GQR1XS
UM-UC-3 NGPke3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTR4LkiwOVkh|ryP NHO0SWxUSU6JRWK=
HT-29 NXPQSGFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2i2XGlEPTB;NEeuPFc6OiEQvF2= NXnyboo6W0GQR1XS
LN-405 NETVVGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\KOJFKSzVyPUS4MlA5OjdizszN NWrqd2FGW0GQR1XS
NCI-H727 NYrQb|JnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHWXI5KSzVyPUS4Mlc4OjZizszN NFvIc3hUSU6JRWK=
D-502MG M2P4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NESwNYNKSzVyPUS4Mlk3PzZizszN MX;TRW5ITVJ?
GMS-10 NIDVe29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HES2lEPTB;NEmuNlk4PCEQvF2= MnTmV2FPT0WU
MEL-JUSO NHjX[FJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\OSWlEPTB;NEmuN|Q4KM7:TR?= NWLwTmxvW0GQR1XS

... 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
  • 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

Molarity Calculator

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID