PLX-4720

For research use only.

Catalog No.S1152

120 publications

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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Selleck's PLX-4720 has been cited by 120 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 NGDaeoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnv6TWM2OD1yLkC3OFU4KM7:TR?= NVvWcI1UW0GQR1XS
EoL-1-cell NF24fYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrSenRwUUN3ME2wMlE1OTZ4IN88US=> MnG1V2FPT0WU
C32 Ml:0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fVcmlEPTB;MD6xOVE{OSEQvF2= MUnTRW5ITVJ?
M14 NVzJSHkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTBwMkG3OVch|ryP MmfvV2FPT0WU
CP50-MEL-B M2LyNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7hb3VKSzVyPUCuNlk4QDRizszN NHW4UWVUSU6JRWK=
A101D M4HMZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwM{K1PFkh|ryP NYf1XWR4W0GQR1XS
G-361 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTBwM{S2N|ch|ryP M3P3NXNCVkeHUh?=
HT-144 MnO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTBwM{[zNlkh|ryP MoLjV2FPT0WU
ACN M1nYdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXwRoc{UUN3ME2wMlM5PDd5IN88US=> NVTlPIJjW0GQR1XS
COLO-829 M3TPfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFi4eGFKSzVyPUCuN|g6PjhizszN NXuyeVFqW0GQR1XS
MEL-HO NUixOolkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIn2fYZKSzVyPUCuOFEyPzlizszN Mn;yV2FPT0WU
SH-4 MkDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mli5TWM2OD1yLkSxOFIzKM7:TR?= NXPoRZVlW0GQR1XS
SK-MEL-3 NETEN|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDVTWM2OD1yLkWxOVY5KM7:TR?= NELFeIJUSU6JRWK=
A375 NGDSPVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml[zTWM2OD1yLk[3N|U6KM7:TR?= M2fROXNCVkeHUh?=
MMAC-SF MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M162XmlEPTB;MD62PFYyPCEQvF2= MXHTRW5ITVJ?
BHT-101 M3;FcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnBNYxKSzVyPUCuO|A4ODJizszN MV;TRW5ITVJ?
K5 NFrHd21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ixRmlEPTB;MD63OlE1QCEQvF2= MX7TRW5ITVJ?
BV-173 NYW4bYhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7j[lVKSzVyPUCuO|k3PDRizszN MnH2V2FPT0WU
RVH-421 NFj0b3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nHUWlEPTB;MD64Olc6PiEQvF2= MVvTRW5ITVJ?
HCC2218 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrJNGtuUUN3ME2wMlg4QDR2IN88US=> NHO3c|BUSU6JRWK=
WM-115 MnraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjWTWM2OD1yLki4OlkzKM7:TR?= NYqwbFlyW0GQR1XS
SK-MEL-28 MmLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVO0fm54UUN3ME2xMlA1PTZ7IN88US=> MV7TRW5ITVJ?
COLO-679 NHvkWFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nEV2lEPTB;MT6xNFQ3PCEQvF2= NUHTOnV5W0GQR1XS
MZ7-mel MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDsdWdQUUN3ME2xMlE1QTZ|IN88US=> MoC3V2FPT0WU
SK-MEL-30 NIPHTG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTFwM{OzPFYh|ryP NELJNFFUSU6JRWK=
NCI-H209 NIm5ZnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\2dWtKSzVyPUGuOlA5PiEQvF2= NF;ReWVUSU6JRWK=
HTC-C3 NWDQbIVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrBR3JlUUN3ME2xMlY3Ojl2IN88US=> NGXuV|BUSU6JRWK=
KARPAS-45 M1PWZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3CTWM2OD1{LkC0PVc5KM7:TR?= M1L5UHNCVkeHUh?=
NCI-SNU-5 NF;WO3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnHTlFtUUN3ME2yMlEyQTZ7IN88US=> M1rZcnNCVkeHUh?=
KP-4 NGPWXlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnWTWM2OD1{LkOwO|g4KM7:TR?= NGWzT|hUSU6JRWK=
PA-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTaXm8yUUN3ME2yMlczPjd|IN88US=> MmrmV2FPT0WU
HuO-3N1 NHTuPJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TVT2lEPTB;Mj64O|k1PiEQvF2= M4\HPHNCVkeHUh?=
NCI-H358 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXS4e3IzUUN3ME2yMlkzOjN{IN88US=> NH;LZ5pUSU6JRWK=
CTB-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfLemR2UUN3ME2zMlQxOTd4IN88US=> NY\vOppNW0GQR1XS
697 MnrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzNZVdRUUN3ME2zMlU2OjZ4IN88US=> MmrsV2FPT0WU
CP66-MEL MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLPNGtCUUN3ME20MlE2QTJ5IN88US=> MWnTRW5ITVJ?
NB13 MkG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjLfZZKSzVyPUSuOFkyPzlizszN Ml36V2FPT0WU
DBTRG-05MG MkDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTRwNUOzNlUh|ryP NFnmbFlUSU6JRWK=
A2058 NGnDUlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPVeo1KSzVyPUSuO|IyPjRizszN NV;DZVh2W0GQR1XS
KG-1 M3fURmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\TVmlEPTB;ND63N|kxQCEQvF2= NHfzfnNUSU6JRWK=
8305C Mn3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITU[HpKSzVyPUWuNVg4OyEQvF2= MoPCV2FPT0WU
RPMI-7951 NWe1[HNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\1cXRVUUN3ME21MlgxOjh|IN88US=> NV[3RY5qW0GQR1XS
CHL-1 M33Bbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXrVZdKSzVyPUWuPVc3ODNizszN MnzuV2FPT0WU
TI-73 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:4NWxKSzVyPU[uNFA6ODJizszN M2qxSXNCVkeHUh?=
HT-1080 Ml7IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XYU2lEPTB;Nj6xNFk1PiEQvF2= NWfNdWFrW0GQR1XS
ES5 MnL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTZwMUS5NlQh|ryP MUDTRW5ITVJ?
8-MG-BA NUfweHJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\IendKSzVyPU[uNVgyOjlizszN NUHUNVg{W0GQR1XS
NB7 M4nrdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofaTWM2OD14LkKxN|c{KM7:TR?= Mmn3V2FPT0WU
H4 NUGwfYVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzFTWM2OD14LkKyOFk{KM7:TR?= NFvFU2FUSU6JRWK=
CAL-72 MmntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XYdWlEPTB;Nj60OVQzOyEQvF2= M{W3O3NCVkeHUh?=
HCC1806 NW\CNmZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHWbpJbUUN3ME22MlgyQTNzIN88US=> MortV2FPT0WU
BCPAP MonXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTdwMkG3OlQh|ryP NGP2PFBUSU6JRWK=
LB2241-RCC M362[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7RZmFKSzVyPUeuN|Y6ODdizszN M2nJOXNCVkeHUh?=
COLO-741 MnzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\5SmlEPTB;OD6wNVY4QSEQvF2= MVnTRW5ITVJ?
HSC-3 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrQfHp{UUN3ME24MlA4ODZ6IN88US=> M4DLbXNCVkeHUh?=
SW982 NFTZbpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjZPHdTUUN3ME24MlQyPTF4IN88US=> M122SnNCVkeHUh?=
GCT MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml35TWM2OD16Lke1N|E1KM7:TR?= MYrTRW5ITVJ?
KY821 MnjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTlwMEWxO|gh|ryP MkfpV2FPT0WU
JVM-3 NXzKcXJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTKOFNKSzVyPUmuOVY6QTlizszN MlLoV2FPT0WU
RS4-11 NYPoOGFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3r5fmlEPTB;OT62NFQ5KM7:TR?= NVzCfIE4W0GQR1XS
VA-ES-BJ MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfuTWM2OD1zMD6wNVQ6KM7:TR?= NEHnepdUSU6JRWK=
A431 NVjmcZBOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWqydJBrUUN3ME2xNE41OjF{IN88US=> M2HxOXNCVkeHUh?=
LXF-289 NWnRPZZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTtdFBvUUN3ME2xNE41PThizszN MnHHV2FPT0WU
SK-MEL-24 NGjsVJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIj4OoxKSzVyPUGwMlgzPzRizszN MYnTRW5ITVJ?
NOS-1 NYG4N49sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;VOHdKSzVyPUGwMlg1PzJizszN M1PSV3NCVkeHUh?=
KNS-62 M1flXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTJXlhKSzVyPUGxMlI1ODRizszN Mn7LV2FPT0WU
SK-HEP-1 NWizOpBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7vTWM2OD1zMT6zOVI4KM7:TR?= NXLadIRyW0GQR1XS
A3-KAW MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkm4TWM2OD1zMT63NVc5KM7:TR?= M3:3THNCVkeHUh?=
SK-LU-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\MVlFKSzVyPUGyMlI3PTVizszN MWrTRW5ITVJ?
TYK-nu NUjHN|BRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDX[oVuUUN3ME2xNk4{QTN{IN88US=> NV;JSlR[W0GQR1XS
NMC-G1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3WTWM2OD1zMj62NFYzKM7:TR?= M161VHNCVkeHUh?=
BB65-RCC MkPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzmb|RKSzVyPUGyMlcyPjlizszN NYHQVFV5W0GQR1XS
QIMR-WIL MoLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjy[FFKSzVyPUGyMlg5OzNizszN MYnTRW5ITVJ?
D-566MG NHflUI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXZWpZKSzVyPUGzMlk2PzZizszN MoLvV2FPT0WU
KYSE-140 NF3ndYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXi1dXNqUUN3ME2xOE4xPzV|IN88US=> M1v1cXNCVkeHUh?=
SCC-4 MnHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD3c|FDUUN3ME2xOE4{OzV7IN88US=> MYrTRW5ITVJ?
U251 M1Wz[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HOPWlEPTB;MUSuPFQ6OiEQvF2= NGPqfGZUSU6JRWK=
D-542MG NVTqTYV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTF2LkmyNlIh|ryP MYfTRW5ITVJ?
LAMA-84 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHPSnVFUUN3ME2xOE46QTN{IN88US=> NF;ibnlUSU6JRWK=
NCI-H720 Mo\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;rTWM2OD1zNT6yOlg1KM7:TR?= NWD0cXVTW0GQR1XS
DEL MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4SwPWlEPTB;MUWuOFI6OyEQvF2= M2K3TnNCVkeHUh?=
SBC-1 MlXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljYTWM2OD1zNT60N|A2KM7:TR?= MljmV2FPT0WU
ECC10 NVHsZXNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3W4c2lEPTB;MUWuOFQ2QCEQvF2= NYHKTIZUW0GQR1XS
Daoy MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTF3Lke2NVYh|ryP NYfJdmtsW0GQR1XS
SCH MoPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHpTWM2OD1zNT63PFM2KM7:TR?= MVHTRW5ITVJ?
MZ2-MEL NVu3[HJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTF4LkC2OFYh|ryP MkXKV2FPT0WU
CAL-12T NHqzc2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PLS2lEPTB;MU[uOFg3OiEQvF2= MX3TRW5ITVJ?
KE-37 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWP3T4s3UUN3ME2xOk45OTB5IN88US=> NXXFPHBTW0GQR1XS
LS-411N NYTKS4x5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzWc29KSzVyPUG3MlEyQCEQvF2= NXnCOJRmW0GQR1XS
NCI-H2228 MmHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrvTWM2OD1zNz6zNFcyKM7:TR?= MYrTRW5ITVJ?
SK-MEL-2 NF\6XINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkC1TWM2OD1zNz60PVY2KM7:TR?= NHH6WI9USU6JRWK=
HN MmjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDBWY1KSzVyPUG3MlczPDhizszN MWXTRW5ITVJ?
NCI-H1648 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3vXZE{UUN3ME2xO{45OThizszN NV[wS|ZxW0GQR1XS
IA-LM MlTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13SSWlEPTB;MUiuN|E4OiEQvF2= NVfWVG0yW0GQR1XS
EW-13 Mn\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTF6LkW3NFgh|ryP MWPTRW5ITVJ?
YKG-1 NH;2ZmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXrR|dLUUN3ME2xPU42PzFzIN88US=> NH;ydpVUSU6JRWK=
KNS-81-FD MljYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jxTmlEPTB;MUmuOVg2QCEQvF2= M2jZSXNCVkeHUh?=
23132-87 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrzTWM2OD1zOT63OlQzKM7:TR?= M2\kNXNCVkeHUh?=
NUGC-3 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnkdotoUUN3ME2xPU46QDh5IN88US=> Mn3aV2FPT0WU
5637 MmjHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTJyLkC0O|gh|ryP MmX4V2FPT0WU
NCI-H1755 NUXXUXk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\OTWM2OD1{MD60O|Y1KM7:TR?= MkfLV2FPT0WU
RH-18 Mo\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTJyLkW3OFgh|ryP Mnj5V2FPT0WU
RXF393 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHxOJJKSzVyPUKwMlY4PTZizszN M3uy[XNCVkeHUh?=
LU-134-A MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHVTWM2OD1{MD63NFU3KM7:TR?= M1HYV3NCVkeHUh?=
TE-12 M2HUOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq1TWM2OD1{MD63NlAyKM7:TR?= NU\3eGxrW0GQR1XS
MOLT-4 MonrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnMZlJ7UUN3ME2yNU4yQTF3IN88US=> M2PNVHNCVkeHUh?=
IGR-1 NInxNJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37pdWlEPTB;MkGuN|c6PiEQvF2= MWLTRW5ITVJ?
HOP-92 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXORnVQUUN3ME2yNU41QTh5IN88US=> NFu4WZZUSU6JRWK=
SK-MES-1 NGfId4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\jUY1xUUN3ME2yNU44OzhzIN88US=> NGTjfFNUSU6JRWK=
LU-65 M4\0eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPjTWM2OD1{MT64OlI1KM7:TR?= MYrTRW5ITVJ?
MS-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HJSmlEPTB;MkKuNVIxOyEQvF2= MXTTRW5ITVJ?
LoVo NHHxNmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULtZlBPUUN3ME2yNk4zPDRizszN M3LuRnNCVkeHUh?=
A704 NIPJdZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUeyUlZ{UUN3ME2yNk42OTV3IN88US=> NIfBO3VUSU6JRWK=
HT-1376 M1P4R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYK4PGwxUUN3ME2yNk43ODV7IN88US=> NYm4RoFyW0GQR1XS
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Ramos-2G6-4C10 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17tfmlEPTB;MkKuO|M3PiEQvF2= MYTTRW5ITVJ?
T47D M2DQfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTJ{Lke5O|kh|ryP MmXPV2FPT0WU
HT-1197 M4mzdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;SPGlEPTB;MkOuNFgyPyEQvF2= Mnm0V2FPT0WU
LB2518-MEL MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mly0TWM2OD1{Mz62OFEzKM7:TR?= MlP2V2FPT0WU
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SK-NEP-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTJ2Lki3OFQh|ryP MV;TRW5ITVJ?
NCI-H526 M1LJPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlq2TWM2OD1{NT6wNFI{KM7:TR?= NYW5fIlOW0GQR1XS
IST-SL1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;zdWVKUUN3ME2yOU4zPzVzIN88US=> MWLTRW5ITVJ?
HH NHzMeZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHnUplKSzVyPUK1MlMyQTJizszN M3TlSnNCVkeHUh?=
NCI-H82 NEfwb3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XsVGlEPTB;MkWuPVM5KM7:TR?= M2[wXnNCVkeHUh?=
SNU-449 M12ySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXJVpl3UUN3ME2yO{4zODF6IN88US=> M1;3bHNCVkeHUh?=
COR-L23 NFPKSoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzFTWM2OD1{Nz6yPFE{KM7:TR?= MnzmV2FPT0WU
LOXIMVI NHLnVYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfVTWM2OD1{Nz6zOlgh|ryP MV3TRW5ITVJ?
GR-ST NF3ZWWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJ5Lk[3NFYh|ryP M{fZWHNCVkeHUh?=
NCI-SNU-1 NITT[FFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHaTWM2OD1{Nz65OFQh|ryP M372W3NCVkeHUh?=
ALL-PO M3nxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvlTWM2OD1{OD6xOlA1KM7:TR?= MmjvV2FPT0WU
ML-2 M1OyT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\LTWM2OD1{OD6yPFE1KM7:TR?= M2LkZXNCVkeHUh?=
HOP-62 M3vWcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zidWlEPTB;MkiuO|E{KM7:TR?= NEDHdoVUSU6JRWK=
EGI-1 NY\1XWd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHxTWM2OD1{OD64PFQ2KM7:TR?= NGf1e3FUSU6JRWK=
TCCSUP NITa[WVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{K1VWlEPTB;MkiuPVI4OiEQvF2= M4LucXNCVkeHUh?=
LB996-RCC M1fGZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnGTWM2OD1{OT61OlgzKM7:TR?= NUX2S2I4W0GQR1XS
LCLC-97TM1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTN{LkG5OlQh|ryP NFrtV3pUSU6JRWK=
NCI-H1304 NV7mbYh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTN{LkOzNFEh|ryP MUfTRW5ITVJ?
KP-N-YS MnfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTN{LkW5O|Mh|ryP M1zwW3NCVkeHUh?=
NCI-H1770 MnXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLlTWM2OD1|Mz6xOlQ5KM7:TR?= MoHJV2FPT0WU
EM-2 MlHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nS[GlEPTB;M{OuOlUxPCEQvF2= M4DpWnNCVkeHUh?=
ChaGo-K-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2THXmlEPTB;M{OuO|I{PiEQvF2= NIHPWVVUSU6JRWK=
ACHN NVGzV5V2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTN|LkizPFUh|ryP M17QNnNCVkeHUh?=
MN-60 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTGbmxGUUN3ME2zN{45PTR2IN88US=> NVfpR481W0GQR1XS
EW-18 NUXlTYFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLkPYV5UUN3ME2zN{45QTdzIN88US=> MkLwV2FPT0WU
KGN MnLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4r3RmlEPTB;M{WuO|I6OiEQvF2= M1ey[XNCVkeHUh?=
U031 NITXb45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7vTWM2OD1|NT64NVMzKM7:TR?= MnPNV2FPT0WU
HMV-II MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTN4LkC3O|Qh|ryP NX65bHBsW0GQR1XS
L-363 NHn6cZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnmwTWM2OD1|Nz62OFU2KM7:TR?= NX;XSZVxW0GQR1XS
NCI-H1155 M1HQemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jiNWlEPTB;M{iuNFAyPSEQvF2= MoW4V2FPT0WU
NCI-H1793 NXXCU5poT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnnUGtRUUN3ME2zPE4yODJ4IN88US=> NXO1WFAzW0GQR1XS
P30-OHK M3qy[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnyTWM2OD1|OD6xN|MzKM7:TR?= NWTYXHd[W0GQR1XS
AN3-CA MmnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfqTWM2OD1|OD6xOlE2KM7:TR?= MWfTRW5ITVJ?
UACC-257 M1G4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVj0W4I2UUN3ME2zPE44QSEQvF2= MoH5V2FPT0WU
MCF7 NI\IeGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTN7Lki2Nlkh|ryP M3Lae3NCVkeHUh?=
KP-N-YN MnvoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3X3SmlEPTB;NECuOFI5PSEQvF2= MX;TRW5ITVJ?
T98G MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHDTWM2OD12MD60PVU4KM7:TR?= M3LqW3NCVkeHUh?=
HGC-27 M2PBVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jBd2lEPTB;NEOuNlc1KM7:TR?= M3uwZ3NCVkeHUh?=
NCI-H1092 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUi0ToI3UUN3ME20N{4zQDl3IN88US=> MoLXV2FPT0WU
KARPAS-299 NYL4W25QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfCTWM2OD12Mz6zNFcyKM7:TR?= NH3MVopUSU6JRWK=
LB1047-RCC NUPHbXllT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTR2Lkm5OVkh|ryP M{fsTnNCVkeHUh?=
786-0 NVTiPVdZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrFXGFoUUN3ME20OU43PSEQvF2= NHXqW5FUSU6JRWK=
HCC2157 NYnTc3p1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{X6W2lEPTB;NE[uNFM2QSEQvF2= MVHTRW5ITVJ?
NY M3Xzc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTR4LkG3O|gh|ryP M2jIWHNCVkeHUh?=
EFM-19 NWXhRpN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHoe2FKSzVyPUS2Mlc2OzNizszN NWTmdmdsW0GQR1XS
EW-16 Mm\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUC0Um1oUUN3ME20Ok44QDB4IN88US=> NFjpfYdUSU6JRWK=
UM-UC-3 NYTqVVFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkK5TWM2OD12Nj64NFU6KM7:TR?= NGjqcZFUSU6JRWK=
HT-29 MkL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTR5Lki3PVIh|ryP NEPsS4NUSU6JRWK=
LN-405 MoTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPtTWM2OD12OD6wPFI4KM7:TR?= MV;TRW5ITVJ?
NCI-H727 NY[yfZFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTR6Lke3NlYh|ryP NUHacYh5W0GQR1XS
D-502MG Mn7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HTeGlEPTB;NEiuPVY4PiEQvF2= M1;lZ3NCVkeHUh?=
GMS-10 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTR7LkK5O|Qh|ryP NUPKV4p3W0GQR1XS
MEL-JUSO NFjnWnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTR7LkO0O{DPxE1? MoLkV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-MEK / MEK / p-ERK / ERK / p-FAK(S910); 

PubMed: 23076151     


WM793 and WM793-Res NRAS cells were seeded overnight in the absence of PLX4720 and then treated with 1 μm PLX4720 for times ranging from 0 to 24 h. Samples were analyzed by Western blotting for phospho-MEK, total MEK, phospho-ERK1/2, total ERK1/2, phospho-S910 FAK, and total FAK.

p-EGFR 1173 / EGFR / p-Akt / Akt; 

PubMed: 26023796     


Three BRAF(V600E) glioma cell lines, NMC-G1, AM38 and DBTRG-05MG were subjected to a 24 hour time course treatment with 5 μM PLX4720 in the presence or absence of 1 μM HKI-272. These cells were serum starved for 16 hours before being stimulated with 10% FBS and harvested for immunoblotting analysis. Cells treated with PLX4720 alone showed an initial suppression of MEK and ERK phosphorylation followed by a profound rebound of MAPK pathway activation as early as one hour post-PLX4720 treatment. Elevated levels of EGFR phosphorylation were also observed in the PLX4720 treated cells. The extent of Akt phosphorylation increased upon PLX4720 treatment, although the extent varies between cell lines. In contrast, no reactivation of EGFR, MEK, ERK or Akt was observed in cells pre-treated with HKI-272.

p27 / Cyclin D1 / pRb; 

PubMed: 21828154     


Immunoblot analysis revealed that PLX4720 (3 μM) decreased levels of phosphorylated ERK, decreased levels of cyclin D1, increased levels of p27, and decreased levels of phosphorylated Rb in BRAF-mutant (OCM3) cells. On the contrary, in Gα-mutant (OMM1.3) UM cells, PLX4720 induced a paradoxical increase in phosphorylated ERK and Rb levels and an early increase in cyclin D1 levels but did not stimulate p27 levels.

pAkt(Ser473) / pAkt(Thr308); 

PubMed: 21828154     


Immunoblot analysis revealed that both AZD6244 and PLX4720 induced an early (within 2–6 hours of exposure) increase in the levels of phosphorylated Akt (at residues Ser473 and Thr308) in both BRAF-mutant OCM3 and Gα-mutant OMM1.3 cells. Eventually, and with prolonged drug exposure, the phosphorylation of Akt returned to baseline in Gα-mutant OMM1.3 cells and decreased even below baseline levels in BRAF-mutant OCM3 cells.

23076151 26023796 21828154
Immunofluorescence
LAMP1; 

PubMed: 30979895     


Representative images of LysoTracker Red (red) and LAMP1 (green) immunostaining of PLX4720 (1 μM, 12 h-treated) A375 cells with depletion of the indicated genes. Note the reduced lysosome staining in PLX4720-treated cells upon TFEB depletion. 

ZKSCAN3 / TFEB ; 

PubMed: 30979895     


Representative confocal images of subcellular translocation of endogenous TFEB (green) and ZKSCAN3 (red) in A375 cells treated with PLX4720 (1 μM, 12 h). n = 3 independent experiments. 

30979895
Growth inhibition assay
Cell viability; 

PubMed: 27848137     


AM-38 and DBTRG-05MG cells were treated for 5 days. Media was changed once every 3 days. Cell viability was measured using WST-1 assay. Error bars indicate the variation between triplicate measurements. PLX4720 and PD0325901 alone or in combination reduced cell viability significantly. However, combined therapy led to the most significant cell viability reduction compared to either monotherapy in both AM-38 and DBTRG-05MG cell lines.

27848137
ELISA
mIFN-γ; 

PubMed: 23204132     


(C, D and E) IFN-γ secretion by pmel-1 T cells co-cultured with transduced melanoma cells (after cell sorting) that had been pre-treated with the indicated concentrations of PLX4720, as determined by ELISA. (*P<0.05, ** P<0.01) Data are representative of 3 independent experiments.

23204132
In vivo Oral administration of PLX-4720 at 20 mg/kg/day induces significant tumor growth delays and regressions in B-RafV600E-dependent COLO205 tumor xenografts, without obvious adverse effects in mice even at dose of 1 g/kg. PLX-4720 at 100 mg/kg twice daily almost completely eliminates the 1205Lu xenografts bearing B-RafV600E, while has no activity against C8161 xenografts bearing wild-type B-Raf. The anti-tumor effects of PLX-4720 correlate with the blockade of MAPK pathway in those cells harboring the V600E mutation. [1] PLX-4720 treatment at 30 mg/kg/day significant inhibits the tumor growth of 8505c xenografts by >90%, and dramatically decreases distant lung metastases. [3]

Protocol

Kinase Assay:[1]
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In vitro Raf kinase activities:

The in vitro kinase activities of wild type Raf and mutants are determined by measuring phosphorylation of biotinylated-MEK protein using Perkin-Elmer's AlphaScreen Technology. For each enzyme (0.1 ng), 20-μL reactions are carried out in 20 mM Hepes (pH 7.0), 10 mM MgCl2, 1 mM DTT, 0.01% Tween-20, 100 nM biotin-MEK protein, various ATP concentrations, and increasing concentrations of PLX-4720 at room temperature. Reactions are stopped at 2, 5, 8, 10, 20, and 30 minutes with 5 μL of a solution containing 20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, and 0.3% BSA. The stop solution also includes phospho-MEK Antibody, Streptavidin-coated Donor beads and Protein A Acceptor beads from the AlphaScreen Protein A Detection Kit. The antibody and beads are preincubated in stop solution in the dark at room temperature for 30 minutes. The final dilution of antibody is 1/2,000, and the final concentration of each bead is 10 μg/mL. The assay plates are incubated at room temperature for one hour then are read on a PerkinElmer AlphaQuest reader.
Cell Research:[1]
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  • Cell lines: COLO205, A375, WM2664, COLO829, HT716, SW620, H460, Calu-6, HCT116, SK-MEL2, SK-MEL3, Lovo, H1299, 1205Lu, and C8161 cells
  • Concentrations: Dissolved in DMSO, final concentrations ~1 mM
  • Incubation Time: 24, 48, and 72 hours
  • Method: Cells are treated with various concentrations PLX-4720 for 24, 48, and 72 hours. Cell proliferation is measured by using the CellTiter-Glo Luminescent Cell Viability Assay or MTT assay. For cell cycle analysis, supernatant and cells are collected, pelleted, and fixed with 70% ethanol. Before staining with propidium iodide (10 μg/mL), cells are incubated for 1 hour at 37 °C in 0.5 mg/mL RNase I to rid samples of residual RNA contamination. Samples are then analyzed by using the EPICS XL apparatus. For the assessment of apoptosis, media and cells are harvested and pelleted before staining with annexin-FITC and propidium iodide. Samples are subsequently analyzed by using the EPICS XL apparatus.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Female athymic mice (NCr nu/nu) implanted s.c. with COLO205 cells, and SCID mice with 1205Lu or C8161 cells
  • Dosages: 5, 20, or 100 mg/kg
  • Administration: Oral gavage once or twice daily
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 413.83
Formula

C17H14ClF2N3O3S

CAS No. 918505-84-7
Storage powder
in solvent
Synonyms N/A
Smiles CCC[S](=O)(=O)NC1=CC=C(F)C(=C1F)C(=O)C2=C[NH]C3=NC=C(Cl)C=C23

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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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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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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