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
USD 120 In stock
USD 270 In stock
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Cited by 110 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 NEDsRYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnVTWM2OD1yLkC3OFU4KM7:TR?= MkmyV2FPT0WU
EoL-1-cell NYeyO|FtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDqTWM2OD1yLkG0NVY3KM7:TR?= M3v1PHNCVkeHUh?=
C32 NUHxfWdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX:ycVRtUUN3ME2wMlE2OTNzIN88US=> MXfTRW5ITVJ?
M14 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXHPZJKSzVyPUCuNlE4PTdizszN M3vFWHNCVkeHUh?=
CP50-MEL-B M1fJNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfnbXFKSzVyPUCuNlk4QDRizszN M{LCOXNCVkeHUh?=
A101D MkDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjVW25KSzVyPUCuN|I2QDlizszN M1f6[nNCVkeHUh?=
G-361 MlTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjsPIRKSzVyPUCuN|Q3OzdizszN NYfVWHd6W0GQR1XS
HT-144 M3XaTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;xfIVYUUN3ME2wMlM3OzJ7IN88US=> MWXTRW5ITVJ?
ACN NHrWO|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rT[mlEPTB;MD6zPFQ4PyEQvF2= M3K3[3NCVkeHUh?=
COLO-829 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTBwM{i5Olgh|ryP MWPTRW5ITVJ?
MEL-HO NVHCcY9iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUO5Z|dkUUN3ME2wMlQyOTd7IN88US=> MV3TRW5ITVJ?
SH-4 MnTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWe2RlZbUUN3ME2wMlQyPDJ{IN88US=> M1zkc3NCVkeHUh?=
SK-MEL-3 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXqTWM2OD1yLkWxOVY5KM7:TR?= M4OxXHNCVkeHUh?=
A375 NIjvWlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\2bWJkUUN3ME2wMlY4OzV7IN88US=> NFf6[YlUSU6JRWK=
MMAC-SF NYjtT5llT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEOxcmtKSzVyPUCuOlg3OTRizszN NH\jW2NUSU6JRWK=
BHT-101 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljyTWM2OD1yLkewO|AzKM7:TR?= M{PI[HNCVkeHUh?=
K5 M{\qbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7hTWM2OD1yLke2NVQ5KM7:TR?= M2L5SHNCVkeHUh?=
BV-173 NInCO5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPHTWM2OD1yLke5OlQ1KM7:TR?= NWHjcYtyW0GQR1XS
RVH-421 NUnNUpptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3X1R2lEPTB;MD64Olc6PiEQvF2= NVm5cXZNW0GQR1XS
HCC2218 NHPKRlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nPZmlEPTB;MD64O|g1PCEQvF2= NVT0XFJ3W0GQR1XS
WM-115 MlzGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3OU|hKSzVyPUCuPFg3QTJizszN MnXZV2FPT0WU
SK-MEL-28 NGnhPY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLLbXVjUUN3ME2xMlA1PTZ7IN88US=> MnXXV2FPT0WU
COLO-679 M1LwTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7zOoVKSzVyPUGuNVA1PjRizszN NILvZWNUSU6JRWK=
MZ7-mel M4PVb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFwMUS5OlMh|ryP M1PBT3NCVkeHUh?=
SK-MEL-30 NHvFVFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYX3cGMzUUN3ME2xMlM{Ozh4IN88US=> NGPvZ4JUSU6JRWK=
NCI-H209 NHnNfVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljsTWM2OD1zLk[wPFYh|ryP M3HPSXNCVkeHUh?=
HTC-C3 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrX[5pKSzVyPUGuOlYzQTRizszN NG\BbmNUSU6JRWK=
KARPAS-45 NX7UfGhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XueWlEPTB;Mj6wOFk4QCEQvF2= M4O5e3NCVkeHUh?=
NCI-SNU-5 NFrldVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDZcI5KSzVyPUKuNVE6PjlizszN NIKxe3BUSU6JRWK=
KP-4 MlXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vCR2lEPTB;Mj6zNFc5PyEQvF2= MmLVV2FPT0WU
PA-1 MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTJwN{K2O|Mh|ryP Ml7OV2FPT0WU
HuO-3N1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX76WW5VUUN3ME2yMlg4QTR4IN88US=> M{fVWnNCVkeHUh?=
NCI-H358 MmfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XvVWlEPTB;Mj65NlI{OiEQvF2= MYrTRW5ITVJ?
CTB-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\pTWM2OD1|LkSwNVc3KM7:TR?= NXKxPVdCW0GQR1XS
697 M2KxXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7TUIJ7UUN3ME2zMlU2OjZ4IN88US=> MXXTRW5ITVJ?
CP66-MEL NX\rcJdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\ZTWM2OD12LkG1PVI4KM7:TR?= NX\TNGJFW0GQR1XS
NB13 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\lO|lIUUN3ME20MlQ6OTd7IN88US=> MnTKV2FPT0WU
DBTRG-05MG M3fjS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorlTWM2OD12LkWzN|I2KM7:TR?= MX\TRW5ITVJ?
A2058 NIDPelFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvRTXV1UUN3ME20MlczOTZ2IN88US=> NH7lUlFUSU6JRWK=
KG-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITqZ5RKSzVyPUSuO|M6ODhizszN NYfYXXQyW0GQR1XS
8305C MmLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTVwMUi3N{DPxE1? MVjTRW5ITVJ?
RPMI-7951 NXzIUW5VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrlZ4VMUUN3ME21MlgxOjh|IN88US=> MYXTRW5ITVJ?
CHL-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHES4R1UUN3ME21Mlk4PjB|IN88US=> NUfuPYFCW0GQR1XS
TI-73 MoKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIS5NZZKSzVyPU[uNFA6ODJizszN M2LF[XNCVkeHUh?=
HT-1080 M{XGd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULhbnBkUUN3ME22MlExQTR4IN88US=> MVLTRW5ITVJ?
ES5 NGC4UGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnoTWM2OD14LkG0PVI1KM7:TR?= NWHDVoJNW0GQR1XS
8-MG-BA NG[4bJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzFTWM2OD14LkG4NVI6KM7:TR?= M2q1fnNCVkeHUh?=
NB7 MkTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXGO5p2UUN3ME22MlIyOzd|IN88US=> NF24e41USU6JRWK=
H4 M4jvOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHxc|dHUUN3ME22MlIzPDl|IN88US=> NXL6fZpHW0GQR1XS
CAL-72 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\CNWlEPTB;Nj60OVQzOyEQvF2= M2nwTHNCVkeHUh?=
HCC1806 NVTpNYxmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\MTWM2OD14LkixPVMyKM7:TR?= MkfvV2FPT0WU
BCPAP MoDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\OeFNqUUN3ME23MlIyPzZ2IN88US=> MYLTRW5ITVJ?
LB2241-RCC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofBTWM2OD15LkO2PVA4KM7:TR?= MYfTRW5ITVJ?
COLO-741 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\tPJJKSzVyPUiuNFE3PzlizszN NHTD[IJUSU6JRWK=
HSC-3 NWnXPYxjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nQUmlEPTB;OD6wO|A3QCEQvF2= NFTBb4FUSU6JRWK=
SW982 NEfjZ4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\0c25qUUN3ME24MlQyPTF4IN88US=> NY\oPZdRW0GQR1XS
GCT MkHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3aTWM2OD16Lke1N|E1KM7:TR?= MmPqV2FPT0WU
KY821 NXLoSIVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEi4T2tKSzVyPUmuNFUyPzhizszN MWLTRW5ITVJ?
JVM-3 MnixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYX6UnR7UUN3ME25MlU3QTl7IN88US=> NEDse4NUSU6JRWK=
RS4-11 NHPvc|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfidoxKSzVyPUmuOlA1QCEQvF2= NVXLfolTW0GQR1XS
VA-ES-BJ MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTFyLkCxOFkh|ryP NH\C[XFUSU6JRWK=
A431 MlrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT2R|lKSzVyPUGwMlQzOTJizszN NFviU|hUSU6JRWK=
LXF-289 Mn7HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nSb2lEPTB;MUCuOFU5KM7:TR?= M17LeHNCVkeHUh?=
SK-MEL-24 NF\vZY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7lTWM2OD1zMD64Nlc1KM7:TR?= NEH5W3dUSU6JRWK=
NOS-1 Mo\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoriTWM2OD1zMD64OFczKM7:TR?= NFPKdY5USU6JRWK=
KNS-62 MmTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jvT2lEPTB;MUGuNlQxPCEQvF2= NXnTc5UzW0GQR1XS
SK-HEP-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTSUJNKSzVyPUGxMlM2OjdizszN NUjTdFlVW0GQR1XS
A3-KAW NFy1UJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTFzLkexO|gh|ryP MUnTRW5ITVJ?
SK-LU-1 NWPkTIliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTF{LkK2OVUh|ryP NFL2ZlBUSU6JRWK=
TYK-nu Ml3TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrTO2w4UUN3ME2xNk4{QTN{IN88US=> NH;BfI9USU6JRWK=
NMC-G1 MnnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XycWlEPTB;MUKuOlA3OiEQvF2= NIOzfoFUSU6JRWK=
BB65-RCC NYPXOldIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHySlRKSzVyPUGyMlcyPjlizszN MUHTRW5ITVJ?
QIMR-WIL MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVK2TohTUUN3ME2xNk45QDN|IN88US=> NFHkOXhUSU6JRWK=
D-566MG MkDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFqwR5BKSzVyPUGzMlk2PzZizszN NWS4dodNW0GQR1XS
KYSE-140 MlPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXuS4p1UUN3ME2xOE4xPzV|IN88US=> NHrlUYVUSU6JRWK=
SCC-4 NV3mO2xnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPWTWM2OD1zND6zN|U6KM7:TR?= MoPDV2FPT0WU
U251 NVLCWo9yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{j2NWlEPTB;MUSuPFQ6OiEQvF2= MXzTRW5ITVJ?
D-542MG M1TXWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmP1TWM2OD1zND65NlIzKM7:TR?= M172NnNCVkeHUh?=
LAMA-84 NEDXUJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTBVoJuUUN3ME2xOE46QTN{IN88US=> MnzYV2FPT0WU
NCI-H720 NEfOTGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOxTWM2OD1zNT6yOlg1KM7:TR?= MWLTRW5ITVJ?
DEL M3W2VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDleXFHUUN3ME2xOU41Ojl|IN88US=> MXjTRW5ITVJ?
SBC-1 NYnqWmlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTF3LkSzNFUh|ryP Mln2V2FPT0WU
ECC10 M33qWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfxcY1KSzVyPUG1MlQ1PThizszN NHfFTo1USU6JRWK=
Daoy NWnOeGRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3vTWM2OD1zNT63OlE3KM7:TR?= M2XlcXNCVkeHUh?=
SCH MoXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVGwPJlMUUN3ME2xOU44QDN3IN88US=> MYTTRW5ITVJ?
MZ2-MEL NYXUT|VIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TxeWlEPTB;MU[uNFY1PiEQvF2= M{O5NnNCVkeHUh?=
CAL-12T NXvMVIl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTF4LkS4OlIh|ryP M1ywOHNCVkeHUh?=
KE-37 MkfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnadY5KSzVyPUG2MlgyODdizszN M1jVcnNCVkeHUh?=
LS-411N NYLYOZd1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWO2dmN5UUN3ME2xO{4yOThizszN NFP5V5hUSU6JRWK=
NCI-H2228 NUHkVIsxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrOTFVKSzVyPUG3MlMxPzFizszN NFn0VpFUSU6JRWK=
SK-MEL-2 MnzTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4G1dWlEPTB;MUeuOFk3PSEQvF2= M4\Bd3NCVkeHUh?=
HN NH:zdnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTF5LkeyOFgh|ryP Ml\TV2FPT0WU
NCI-H1648 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4[4WGlEPTB;MUeuPFE5KM7:TR?= MYDTRW5ITVJ?
IA-LM NF;N[HNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDoS4RvUUN3ME2xPE4{OTd{IN88US=> M4\hUHNCVkeHUh?=
EW-13 MmDoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;UTWM2OD1zOD61O|A5KM7:TR?= M2joWHNCVkeHUh?=
YKG-1 NUP3SZh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTF7LkW3NVEh|ryP NWPSZ5R[W0GQR1XS
KNS-81-FD MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{O2PGlEPTB;MUmuOVg2QCEQvF2= NUH4S2hqW0GQR1XS
23132-87 NYfrSYdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\CNXRKSzVyPUG5Mlc3PDJizszN MVrTRW5ITVJ?
NUGC-3 NVPJNI5kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2O4SmlEPTB;MUmuPVg5PyEQvF2= NGH5R41USU6JRWK=
5637 NVfVN45rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnrb5Z6UUN3ME2yNE4xPDd6IN88US=> NWG4TWpSW0GQR1XS
NCI-H1755 NVTTXGpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln5TWM2OD1{MD60O|Y1KM7:TR?= MoDXV2FPT0WU
RH-18 Mk\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;LXll{UUN3ME2yNE42PzR6IN88US=> NHr6dZhUSU6JRWK=
RXF393 MoHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHDU2RmUUN3ME2yNE43PzV4IN88US=> M2HKUXNCVkeHUh?=
LU-134-A NY\lOphyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDUTWM2OD1{MD63NFU3KM7:TR?= M4e0bnNCVkeHUh?=
TE-12 MmPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEm4PIRKSzVyPUKwMlczODFizszN NWHUUIZ1W0GQR1XS
MOLT-4 NHPUS5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPU[lZKSzVyPUKxMlE6OTVizszN M2i4NHNCVkeHUh?=
IGR-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PoT2lEPTB;MkGuN|c6PiEQvF2= Mm\6V2FPT0WU
HOP-92 NYDNR2NKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTJzLkS5PFch|ryP MoLCV2FPT0WU
SK-MES-1 NFrqV2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTJzLkezPFEh|ryP NX\zbWY3W0GQR1XS
LU-65 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTJzLki2NlQh|ryP M2HzXHNCVkeHUh?=
MS-1 NFLGR5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEP2[mJKSzVyPUKyMlEzODNizszN NX7GWmpDW0GQR1XS
LoVo M3m3d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTJ{LkK0OEDPxE1? NYO0bHJ2W0GQR1XS
A704 NGPJR2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHSNYQ2UUN3ME2yNk42OTV3IN88US=> NYfOWWVQW0GQR1XS
HT-1376 NXe4N2JsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\STWM2OD1{Mj62NFU6KM7:TR?= MV\TRW5ITVJ?
IST-MEL1 M3jK[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFntVm9KSzVyPUKyMlY4PTFizszN NIDDS4RUSU6JRWK=
Ramos-2G6-4C10 MlnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPZ[IpKSzVyPUKyMlc{PjZizszN M3\x[XNCVkeHUh?=
T47D MoWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUD3Xo1kUUN3ME2yNk44QTd7IN88US=> MlvjV2FPT0WU
HT-1197 MkjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LB[WlEPTB;MkOuNFgyPyEQvF2= NGe3enVUSU6JRWK=
LB2518-MEL NH;SVo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1WzeGlEPTB;MkOuOlQyOiEQvF2= NV\tdJA2W0GQR1XS
J-RT3-T3-5 M2rW[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHxS41QUUN3ME2yOE44PTl3IN88US=> MXPTRW5ITVJ?
SK-NEP-1 M3vUS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWOxeotGUUN3ME2yOE45PzR2IN88US=> MnjxV2FPT0WU
NCI-H526 NEDZ[GxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTJ3LkCwNlMh|ryP MnXOV2FPT0WU
IST-SL1 NHXRU3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzTTWM2OD1{NT6yO|UyKM7:TR?= Mn72V2FPT0WU
HH NV;5O5dHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfvUYpsUUN3ME2yOU4{OTl{IN88US=> MoTIV2FPT0WU
NCI-H82 MorCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn:5TWM2OD1{NT65N|gh|ryP MVvTRW5ITVJ?
SNU-449 NIW4eodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HPXmlEPTB;MkeuNlAyQCEQvF2= NYnuR4g{W0GQR1XS
COR-L23 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnWcYhKSzVyPUK3MlI5OTNizszN M37GTXNCVkeHUh?=
LOXIMVI MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37sNWlEPTB;MkeuN|Y5KM7:TR?= MXTTRW5ITVJ?
GR-ST NInxUnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTJ5Lk[3NFYh|ryP MXnTRW5ITVJ?
NCI-SNU-1 M{HQV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDZTWM2OD1{Nz65OFQh|ryP MmTUV2FPT0WU
ALL-PO M4fCO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTJ6LkG2NFQh|ryP NX70TWpIW0GQR1XS
ML-2 NFvSZVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYS5ZXBpUUN3ME2yPE4zQDF2IN88US=> M3fIdHNCVkeHUh?=
HOP-62 M2DTNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYKzZVU1UUN3ME2yPE44OTNizszN MU\TRW5ITVJ?
EGI-1 MnXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3X1PGlEPTB;MkiuPFg1PSEQvF2= NIm0ZZdUSU6JRWK=
TCCSUP NXizUZRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\HWWlEPTB;MkiuPVI4OiEQvF2= NXvvV3lbW0GQR1XS
LB996-RCC NG[0bYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF23NmtKSzVyPUK5MlU3QDJizszN MoDIV2FPT0WU
LCLC-97TM1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlf6TWM2OD1|Mj6xPVY1KM7:TR?= NH;IXINUSU6JRWK=
NCI-H1304 M4fNeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknzTWM2OD1|Mj6zN|AyKM7:TR?= MX\TRW5ITVJ?
KP-N-YS NGS0[ohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTN{LkW5O|Mh|ryP M1eyR3NCVkeHUh?=
NCI-H1770 NFvKcFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jG[WlEPTB;M{OuNVY1QCEQvF2= NWDydoZVW0GQR1XS
EM-2 NF6wN3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmL0TWM2OD1|Mz62OVA1KM7:TR?= MYHTRW5ITVJ?
ChaGo-K-1 Mn7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XNZ2lEPTB;M{OuO|I{PiEQvF2= MXTTRW5ITVJ?
ACHN MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzVTWM2OD1|Mz64N|g2KM7:TR?= MmX5V2FPT0WU
MN-60 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfZSmNKSzVyPUOzMlg2PDRizszN NIq4clBUSU6JRWK=
EW-18 M4TjVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2njfmlEPTB;M{OuPFk4OSEQvF2= NVjSNok2W0GQR1XS
KGN NFe2WndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHG0WINKSzVyPUO1MlczQTJizszN NFe2ZpBUSU6JRWK=
U031 NWXybHNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTN3LkixN|Ih|ryP M1H0VHNCVkeHUh?=
HMV-II M2\B[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUO0eGw3UUN3ME2zOk4xPzd2IN88US=> MYfTRW5ITVJ?
L-363 NXfIZmhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3UN3RKSzVyPUO3MlY1PTVizszN NYrCR4ZqW0GQR1XS
NCI-H1155 NFLWfYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTN6LkCwNVUh|ryP M3vYPHNCVkeHUh?=
NCI-H1793 NISyXFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTN6LkGwNlYh|ryP M3LoW3NCVkeHUh?=
P30-OHK MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTN6LkGzN|Ih|ryP M{PqbXNCVkeHUh?=
AN3-CA MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DDOGlEPTB;M{iuNVYyPSEQvF2= M4f2e3NCVkeHUh?=
UACC-257 NUTuXlZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nYdGlEPTB;M{iuO|kh|ryP NYGzWoJSW0GQR1XS
MCF7 NH3TTGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXiTWM2OD1|OT64OlI6KM7:TR?= M{\oeHNCVkeHUh?=
KP-N-YN MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTRyLkSyPFUh|ryP MXTTRW5ITVJ?
T98G NE[xd4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEP3eY5KSzVyPUSwMlQ6PTdizszN MnPNV2FPT0WU
HGC-27 NXPodYdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTR|LkK3OEDPxE1? NXzMPIpiW0GQR1XS
NCI-H1092 MkLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYK2XVdLUUN3ME20N{4zQDl3IN88US=> M1;FRnNCVkeHUh?=
KARPAS-299 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYL0NY5xUUN3ME20N{4{ODdzIN88US=> NWjifox4W0GQR1XS
LB1047-RCC MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLaTWM2OD12ND65PVU6KM7:TR?= MnHHV2FPT0WU
786-0 NV\MXnJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Gyb2lEPTB;NEWuOlUh|ryP MWDTRW5ITVJ?
HCC2157 NXjme2h5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3kdY9KSzVyPUS2MlA{PTlizszN NFywSGRUSU6JRWK=
NY NWnP[nNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTR4LkG3O|gh|ryP NVzwc|hjW0GQR1XS
EFM-19 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTR[GNGUUN3ME20Ok44PTN|IN88US=> MXjTRW5ITVJ?
EW-16 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M163bGlEPTB;NE[uO|gxPiEQvF2= MXPTRW5ITVJ?
UM-UC-3 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnTZVlKSzVyPUS2MlgxPTlizszN MlHCV2FPT0WU
HT-29 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;uTWM2OD12Nz64O|kzKM7:TR?= MVLTRW5ITVJ?
LN-405 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TjdmlEPTB;NEiuNFgzPyEQvF2= NXn0eok1W0GQR1XS
NCI-H727 M{j0[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTR6Lke3NlYh|ryP NUT5WXVNW0GQR1XS
D-502MG NVuxeoE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHNWWtKSzVyPUS4Mlk3PzZizszN NHPJW2RUSU6JRWK=
GMS-10 MnnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnj6TWM2OD12OT6yPVc1KM7:TR?= NHnBTIFUSU6JRWK=
MEL-JUSO NXHpV|ZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHnTWM2OD12OT6zOFch|ryP NUf5e5RsW0GQR1XS

... 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