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 78 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 NXjveGlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3kTWM2OD1yLkC3OFU4KM7:TR?= M{SyNHNCVkeHUh?=
EoL-1-cell NILoSI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXrO2lIUUN3ME2wMlE1OTZ4IN88US=> MWrTRW5ITVJ?
C32 MlTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILaUZVKSzVyPUCuNVUyOzFizszN MY\TRW5ITVJ?
M14 NFnsO2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETzTW9KSzVyPUCuNlE4PTdizszN M3[5NnNCVkeHUh?=
CP50-MEL-B NV7CbWljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfI[WRpUUN3ME2wMlI6Pzh2IN88US=> NIXZOmxUSU6JRWK=
A101D MkTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkewTWM2OD1yLkOyOVg6KM7:TR?= M3zEeXNCVkeHUh?=
G-361 M2nHUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTBwM{S2N|ch|ryP NGXJe3NUSU6JRWK=
HT-144 MoPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfuZXRvUUN3ME2wMlM3OzJ7IN88US=> MVzTRW5ITVJ?
ACN NEfCPI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ezWGlEPTB;MD6zPFQ4PyEQvF2= MnfFV2FPT0WU
COLO-829 MkLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXmT|dKSzVyPUCuN|g6PjhizszN MojnV2FPT0WU
MEL-HO MmG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHPTWM2OD1yLkSxNVc6KM7:TR?= MlnIV2FPT0WU
SH-4 NYPTfYJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwNEG0NlIh|ryP NULKRoJuW0GQR1XS
SK-MEL-3 NXTOcnZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIryN|BKSzVyPUCuOVE2PjhizszN MUPTRW5ITVJ?
A375 NX7kU|VyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTBwNkezOVkh|ryP M2fMTHNCVkeHUh?=
MMAC-SF MnnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nIXGlEPTB;MD62PFYyPCEQvF2= MXzTRW5ITVJ?
BHT-101 Mlr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLlb5BKSzVyPUCuO|A4ODJizszN NYHyOGR5W0GQR1XS
K5 NIexcmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLqTWF2UUN3ME2wMlc3OTR6IN88US=> MV\TRW5ITVJ?
BV-173 NGq3[ItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DvVWlEPTB;MD63PVY1PCEQvF2= MWjTRW5ITVJ?
RVH-421 M{TBXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTBwOE[3PVYh|ryP NWHJPYhRW0GQR1XS
HCC2218 NFjEbGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTITWM2OD1yLki3PFQ1KM7:TR?= MljmV2FPT0WU
WM-115 NUXaUoM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGe0R5lKSzVyPUCuPFg3QTJizszN MlfsV2FPT0WU
SK-MEL-28 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDMTWM2OD1zLkC0OVY6KM7:TR?= M{nKWHNCVkeHUh?=
COLO-679 NFHJN2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7jTWM2OD1zLkGwOFY1KM7:TR?= MXvTRW5ITVJ?
MZ7-mel NHH2W4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFwMUS5OlMh|ryP MoTTV2FPT0WU
SK-MEL-30 NVeyT285T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\peXlKSzVyPUGuN|M{QDZizszN NYjDO2F3W0GQR1XS
NCI-H209 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTFwNkC4OkDPxE1? M1Ppe3NCVkeHUh?=
HTC-C3 NVXibot6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYn6VZpIUUN3ME2xMlY3Ojl2IN88US=> M13EU3NCVkeHUh?=
KARPAS-45 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWG1UGYyUUN3ME2yMlA1QTd6IN88US=> M1jhWnNCVkeHUh?=
NCI-SNU-5 NYjhcZJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHqPWw4UUN3ME2yMlEyQTZ7IN88US=> NXjEPJlNW0GQR1XS
KP-4 NFfKe|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rkNGlEPTB;Mj6zNFc5PyEQvF2= Mor3V2FPT0WU
PA-1 NGT5TpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTJwN{K2O|Mh|ryP NEnvTnNUSU6JRWK=
HuO-3N1 NIW3bGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIntcXdKSzVyPUKuPFc6PDZizszN NHi5WoZUSU6JRWK=
NCI-H358 M3\GRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXv6OlVnUUN3ME2yMlkzOjN{IN88US=> NXjDc25zW0GQR1XS
CTB-1 NYfYVnlzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTNwNECxO|Yh|ryP NUjjXpFQW0GQR1XS
697 NFvrNodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUT0S4xzUUN3ME2zMlU2OjZ4IN88US=> NF:z[FVUSU6JRWK=
CP66-MEL NU\1NotXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEm1[VVKSzVyPUSuNVU6OjdizszN M2f3fHNCVkeHUh?=
NB13 NGO1V4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfqTWM2OD12LkS5NVc6KM7:TR?= MkW4V2FPT0WU
DBTRG-05MG MmPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTRwNUOzNlUh|ryP NEP3ZlhUSU6JRWK=
A2058 M1vnNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHG[|ZKSzVyPUSuO|IyPjRizszN MUjTRW5ITVJ?
KG-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XaXGlEPTB;ND63N|kxQCEQvF2= MYXTRW5ITVJ?
8305C M3P1bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XUeGlEPTB;NT6xPFc{KM7:TR?= Mkn0V2FPT0WU
RPMI-7951 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDpUlNKSzVyPUWuPFAzQDNizszN NWDndY96W0GQR1XS
CHL-1 NHO2eItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTVwOUe2NFMh|ryP MkXDV2FPT0WU
TI-73 NHPPO2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HZS2lEPTB;Nj6wNFkxOiEQvF2= NFT3V2dUSU6JRWK=
HT-1080 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTtfFRKSzVyPU[uNVA6PDZizszN Mn[wV2FPT0WU
ES5 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\iOJNlUUN3ME22MlE1QTJ2IN88US=> MVrTRW5ITVJ?
8-MG-BA NYrSNnhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTZwMUixNlkh|ryP MV3TRW5ITVJ?
NB7 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjx[4RKSzVyPU[uNlE{PzNizszN MVXTRW5ITVJ?
H4 M2PYOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknDTWM2OD14LkKyOFk{KM7:TR?= NX3HVnhSW0GQR1XS
CAL-72 MmK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTZwNEW0NlMh|ryP NXPUT25MW0GQR1XS
HCC1806 NVjTRlZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDDflFVUUN3ME22MlgyQTNzIN88US=> NWKw[5NyW0GQR1XS
BCPAP NU\YU2ZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTdwMkG3OlQh|ryP MUXTRW5ITVJ?
LB2241-RCC M{TJdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrMRVBKSzVyPUeuN|Y6ODdizszN NGHvUI5USU6JRWK=
COLO-741 Mm\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnS1TWM2OD16LkCxOlc6KM7:TR?= MkGxV2FPT0WU
HSC-3 M1PySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfPXIZwUUN3ME24MlA4ODZ6IN88US=> M{HJS3NCVkeHUh?=
SW982 M{jxUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkC4TWM2OD16LkSxOVE3KM7:TR?= NHfISIJUSU6JRWK=
GCT MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonjTWM2OD16Lke1N|E1KM7:TR?= MmTMV2FPT0WU
KY821 MnHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTFVZM3UUN3ME25MlA2OTd6IN88US=> M1vuNHNCVkeHUh?=
JVM-3 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXmXGpKSzVyPUmuOVY6QTlizszN NGD5SYxUSU6JRWK=
RS4-11 M3\MUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTlwNkC0PEDPxE1? M{HuSnNCVkeHUh?=
VA-ES-BJ M4HsZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlqzTWM2OD1zMD6wNVQ6KM7:TR?= MVLTRW5ITVJ?
A431 NUG3UogxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfJTWM2OD1zMD60NlEzKM7:TR?= M3HRUXNCVkeHUh?=
LXF-289 M2jVU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7WSYh[UUN3ME2xNE41PThizszN MXnTRW5ITVJ?
SK-MEL-24 MlzJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;Qd2s4UUN3ME2xNE45Ojd2IN88US=> MmfVV2FPT0WU
NOS-1 NXK4cVNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvRTWM2OD1zMD64OFczKM7:TR?= MXvTRW5ITVJ?
KNS-62 NVHIbIJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:0R4hKSzVyPUGxMlI1ODRizszN MWjTRW5ITVJ?
SK-HEP-1 NEW3cGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVK3d3BXUUN3ME2xNU4{PTJ5IN88US=> NYXncmwyW0GQR1XS
A3-KAW MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfSOnZsUUN3ME2xNU44OTd6IN88US=> M17YVHNCVkeHUh?=
SK-LU-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\5TWM2OD1zMj6yOlU2KM7:TR?= MlyzV2FPT0WU
TYK-nu NFvIdW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPYNZpKSzVyPUGyMlM6OzJizszN MYPTRW5ITVJ?
NMC-G1 NU\sfpZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTtSXhrUUN3ME2xNk43ODZ{IN88US=> NXHDfJo6W0GQR1XS
BB65-RCC MnTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPVTWM2OD1zMj63NVY6KM7:TR?= Ml\DV2FPT0WU
QIMR-WIL NXLFd|BYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrwTWM2OD1zMj64PFM{KM7:TR?= NH;5NpBUSU6JRWK=
D-566MG MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\xU2lEPTB;MUOuPVU4PiEQvF2= MnPhV2FPT0WU
KYSE-140 NVfr[5BpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIT6cHlKSzVyPUG0MlA4PTNizszN MlnxV2FPT0WU
SCC-4 MnP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfGe4FKSzVyPUG0MlM{PTlizszN NHTUUYFUSU6JRWK=
U251 NF:5cnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUm0RldiUUN3ME2xOE45PDl{IN88US=> MnTpV2FPT0WU
D-542MG MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTF2LkmyNlIh|ryP NWrqfoRTW0GQR1XS
LAMA-84 NYW3PWgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELZd4dKSzVyPUG0Mlk6OzJizszN Mlv3V2FPT0WU
NCI-H720 M3LJ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTF3LkK2PFQh|ryP NWGwW|lyW0GQR1XS
DEL NYjvW4dHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4X4[GlEPTB;MUWuOFI6OyEQvF2= MUXTRW5ITVJ?
SBC-1 M4HyeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1[zW2lEPTB;MUWuOFMxPSEQvF2= MlzlV2FPT0WU
ECC10 Ml75S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHyTWM2OD1zNT60OFU5KM7:TR?= MmDSV2FPT0WU
Daoy MoPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfxOJNRUUN3ME2xOU44PjF4IN88US=> M3zSbnNCVkeHUh?=
SCH M{P0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXOTWM2OD1zNT63PFM2KM7:TR?= MlvoV2FPT0WU
MZ2-MEL MnvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXMSZhOUUN3ME2xOk4xPjR4IN88US=> NF:zWoZUSU6JRWK=
CAL-12T M365PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTF4LkS4OlIh|ryP NYnwWo1SW0GQR1XS
KE-37 NVXLVlRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHPTWM2OD1zNj64NVA4KM7:TR?= NIWzO4hUSU6JRWK=
LS-411N MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TzfmlEPTB;MUeuNVE5KM7:TR?= NFnOdVJUSU6JRWK=
NCI-H2228 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTF5LkOwO|Eh|ryP M1TSdnNCVkeHUh?=
SK-MEL-2 NWHtVYdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrXT5drUUN3ME2xO{41QTZ3IN88US=> MXfTRW5ITVJ?
HN MonUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXCeVhpUUN3ME2xO{44OjR6IN88US=> MXPTRW5ITVJ?
NCI-H1648 M1jiWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGD0[m9KSzVyPUG3MlgyQCEQvF2= MYDTRW5ITVJ?
IA-LM NU[5N5dVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1mzcGlEPTB;MUiuN|E4OiEQvF2= M4fBT3NCVkeHUh?=
EW-13 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTF6LkW3NFgh|ryP NYrV[IZtW0GQR1XS
YKG-1 NY\3fmZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX6zW4xWUUN3ME2xPU42PzFzIN88US=> MmXWV2FPT0WU
KNS-81-FD NYTOS29ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Tzb2lEPTB;MUmuOVg2QCEQvF2= NYTuTlJCW0GQR1XS
23132-87 M2LMXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTF7Lke2OFIh|ryP M3OwWnNCVkeHUh?=
NUGC-3 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn0eHpKSzVyPUG5Mlk5QDdizszN M3XuUnNCVkeHUh?=
5637 NXf1dIs{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3LTWM2OD1{MD6wOFc5KM7:TR?= NVLwR|U6W0GQR1XS
NCI-H1755 NX23SYhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHUfIdKSzVyPUKwMlQ4PjRizszN MXzTRW5ITVJ?
RH-18 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTJyLkW3OFgh|ryP M1HVdnNCVkeHUh?=
RXF393 NXHySGlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVv5cFN5UUN3ME2yNE43PzV4IN88US=> MkHZV2FPT0WU
LU-134-A M{SwWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHWTWM2OD1{MD63NFU3KM7:TR?= NFv4eXdUSU6JRWK=
TE-12 MmTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfCUpNFUUN3ME2yNE44OjBzIN88US=> NXnxenpFW0GQR1XS
MOLT-4 NX\3VoZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTJzLkG5NVUh|ryP NWPNV4VVW0GQR1XS
IGR-1 NIexU|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTjR2FQUUN3ME2yNU4{Pzl4IN88US=> M1LoVXNCVkeHUh?=
HOP-92 MmCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnWTWM2OD1{MT60PVg4KM7:TR?= MV;TRW5ITVJ?
SK-MES-1 NV:wdFQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTJzLkezPFEh|ryP NFzOcHVUSU6JRWK=
LU-65 NEXsZ25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PJXGlEPTB;MkGuPFYzPCEQvF2= M4fCR3NCVkeHUh?=
MS-1 NV:xNGh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnFTWM2OD1{Mj6xNlA{KM7:TR?= MV\TRW5ITVJ?
LoVo M{TzPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoW0TWM2OD1{Mj6yOFQh|ryP NFXldXRUSU6JRWK=
A704 NILtZY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2H1emlEPTB;MkKuOVE2PSEQvF2= M3TienNCVkeHUh?=
HT-1376 M1PIXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHCTWM2OD1{Mj62NFU6KM7:TR?= MV\TRW5ITVJ?
IST-MEL1 NV\WUmF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoW3TWM2OD1{Mj62O|UyKM7:TR?= MnXlV2FPT0WU
Ramos-2G6-4C10 M4\NSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfPbYJCUUN3ME2yNk44OzZ4IN88US=> M3\DSnNCVkeHUh?=
T47D NVTKe|RQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEX5V5NKSzVyPUKyMlc6PzlizszN MXTTRW5ITVJ?
HT-1197 M1TVT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWr0d4lVUUN3ME2yN{4xQDF5IN88US=> MmSwV2FPT0WU
LB2518-MEL NEjJTJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1S4cWlEPTB;MkOuOlQyOiEQvF2= MVfTRW5ITVJ?
J-RT3-T3-5 NUPm[Gw6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTJ2Lke1PVUh|ryP MmGxV2FPT0WU
SK-NEP-1 Mlz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmX4TWM2OD1{ND64O|Q1KM7:TR?= NGfL[I9USU6JRWK=
NCI-H526 MonwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPvTWM2OD1{NT6wNFI{KM7:TR?= NXTQfJNtW0GQR1XS
IST-SL1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HlT2lEPTB;MkWuNlc2OSEQvF2= NGP3XGVUSU6JRWK=
HH MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXi1Vok6UUN3ME2yOU4{OTl{IN88US=> NYjx[INXW0GQR1XS
NCI-H82 M{n3XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DGVmlEPTB;MkWuPVM5KM7:TR?= NYi5eWZtW0GQR1XS
SNU-449 NGHkWI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHH1UWhKSzVyPUK3MlIxOThizszN MY\TRW5ITVJ?
COR-L23 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDYTWM2OD1{Nz6yPFE{KM7:TR?= MXXTRW5ITVJ?
LOXIMVI NHnTRoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjifFdKSzVyPUK3MlM3QCEQvF2= NXLoTWxEW0GQR1XS
GR-ST NIW1dItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETwS3VKSzVyPUK3MlY4ODZizszN MmLkV2FPT0WU
NCI-SNU-1 NF\TVoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTJ5Lkm0OEDPxE1? M3j5fHNCVkeHUh?=
ALL-PO MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jZSGlEPTB;MkiuNVYxPCEQvF2= NIHreG9USU6JRWK=
ML-2 NGD4S3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTJ6LkK4NVQh|ryP NUDNV5dqW0GQR1XS
HOP-62 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HUO2lEPTB;MkiuO|E{KM7:TR?= M{j4e3NCVkeHUh?=
EGI-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1i2dWlEPTB;MkiuPFg1PSEQvF2= MUTTRW5ITVJ?
TCCSUP M4TqXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{W0bWlEPTB;MkiuPVI4OiEQvF2= NHjnZpFUSU6JRWK=
LB996-RCC NHTzNGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWL5[m5NUUN3ME2yPU42Pjh{IN88US=> NGPQXJRUSU6JRWK=
LCLC-97TM1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTN{LkG5OlQh|ryP MmXYV2FPT0WU
NCI-H1304 M2HnTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrmR4llUUN3ME2zNk4{OzBzIN88US=> NV[wO2h4W0GQR1XS
KP-N-YS MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILqXlZKSzVyPUOyMlU6PzNizszN NFvYVJVUSU6JRWK=
NCI-H1770 M1riVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHv2elVKSzVyPUOzMlE3PDhizszN Mlq2V2FPT0WU
EM-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojuTWM2OD1|Mz62OVA1KM7:TR?= MVXTRW5ITVJ?
ChaGo-K-1 NWLrfHU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlToTWM2OD1|Mz63NlM3KM7:TR?= M1rGVnNCVkeHUh?=
ACHN M2TMW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrrTWM2OD1|Mz64N|g2KM7:TR?= NW\FcGxXW0GQR1XS
MN-60 MnzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYG1NGxIUUN3ME2zN{45PTR2IN88US=> M{H2d3NCVkeHUh?=
EW-18 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PT[WlEPTB;M{OuPFk4OSEQvF2= M365SHNCVkeHUh?=
KGN M1X3fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTN3LkeyPVIh|ryP MnrmV2FPT0WU
U031 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfl[3c2UUN3ME2zOU45OTN{IN88US=> MkjjV2FPT0WU
HMV-II MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PZXmlEPTB;M{[uNFc4PCEQvF2= MUHTRW5ITVJ?
L-363 MmfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnO0TWM2OD1|Nz62OFU2KM7:TR?= M{DQOXNCVkeHUh?=
NCI-H1155 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfXNIRSUUN3ME2zPE4xODF3IN88US=> MnHmV2FPT0WU
NCI-H1793 NEjtU|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoX6TWM2OD1|OD6xNFI3KM7:TR?= NXv6PXIzW0GQR1XS
P30-OHK NX;4PJhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\zTWM2OD1|OD6xN|MzKM7:TR?= M2XVTnNCVkeHUh?=
AN3-CA MnnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vVemlEPTB;M{iuNVYyPSEQvF2= Mn\GV2FPT0WU
UACC-257 MnfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnkW4FKSzVyPUO4Mlc6KM7:TR?= MYHTRW5ITVJ?
MCF7 NX34VFNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nafmlEPTB;M{muPFYzQSEQvF2= Mn;CV2FPT0WU
KP-N-YN NELMSHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jYXGlEPTB;NECuOFI5PSEQvF2= NUfBOYpUW0GQR1XS
T98G Mlu5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTzTWM2OD12MD60PVU4KM7:TR?= NES5dWhUSU6JRWK=
HGC-27 M1ztTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVq0cWZJUUN3ME20N{4zPzRizszN NXHr[|BnW0GQR1XS
NCI-H1092 NUfQfGRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTR|LkK4PVUh|ryP M3vTbHNCVkeHUh?=
KARPAS-299 MnHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{L2dmlEPTB;NEOuN|A4OSEQvF2= MVzTRW5ITVJ?
LB1047-RCC MmLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTR2Lkm5OVkh|ryP MmfmV2FPT0WU
786-0 NWTlUJJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILtNJFKSzVyPUS1MlY2KM7:TR?= NGnTUGhUSU6JRWK=
HCC2157 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPyTWM2OD12Nj6wN|U6KM7:TR?= MUjTRW5ITVJ?
NY MlzxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjuXYFKSzVyPUS2MlE4PzhizszN MnnZV2FPT0WU
EFM-19 M1KzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rTcWlEPTB;NE[uO|U{OyEQvF2= MXTTRW5ITVJ?
EW-16 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUD4cWV[UUN3ME20Ok44QDB4IN88US=> M{G0V3NCVkeHUh?=
UM-UC-3 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzEZY1KSzVyPUS2MlgxPTlizszN NYfTUIRNW0GQR1XS
HT-29 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTR5Lki3PVIh|ryP MXLTRW5ITVJ?
LN-405 NEPrfFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljnTWM2OD12OD6wPFI4KM7:TR?= NFqxfIFUSU6JRWK=
NCI-H727 M1\rTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTPTWM2OD12OD63O|I3KM7:TR?= MkP0V2FPT0WU
D-502MG NGXaeo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzaTWM2OD12OD65Olc3KM7:TR?= NFWzdFNUSU6JRWK=
GMS-10 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nsWGlEPTB;NEmuNlk4PCEQvF2= M2LyTnNCVkeHUh?=
MEL-JUSO Mkf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7MfolKSzVyPUS5MlM1PyEQvF2= NIO2dW9USU6JRWK=

... 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

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