PLX-4720

For research use only.

Catalog No.S1152

123 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 123 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 MmTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYe1cXV1UUN3ME2wMlA4PDV5IN88US=> NEnQTWhUSU6JRWK=
EoL-1-cell NYrWNYNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3WTWM2OD1yLkG0NVY3KM7:TR?= Mn7iV2FPT0WU
C32 NEjldHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzHTWM2OD1yLkG1NVMyKM7:TR?= M{XJTXNCVkeHUh?=
M14 NEjHUY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTBwMkG3OVch|ryP NV:wbYdVW0GQR1XS
CP50-MEL-B M1fhfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknUTWM2OD1yLkK5O|g1KM7:TR?= MWHTRW5ITVJ?
A101D NIr2e2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PrWGlEPTB;MD6zNlU5QSEQvF2= M1nLTXNCVkeHUh?=
G-361 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3CZY9KSzVyPUCuN|Q3OzdizszN M1zncXNCVkeHUh?=
HT-144 M3TkOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFOxN5FKSzVyPUCuN|Y{OjlizszN MlfUV2FPT0WU
ACN MnntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfpTWM2OD1yLkO4OFc4KM7:TR?= M{[zTnNCVkeHUh?=
COLO-829 NYHvWIFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;YTWM2OD1yLkO4PVY5KM7:TR?= MornV2FPT0WU
MEL-HO M3;wTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHReHM2UUN3ME2wMlQyOTd7IN88US=> MVLTRW5ITVJ?
SH-4 NXrrOZczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1P4RmlEPTB;MD60NVQzOiEQvF2= MX\TRW5ITVJ?
SK-MEL-3 M3\GUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3IR5BKSzVyPUCuOVE2PjhizszN Ml;PV2FPT0WU
A375 NUPOdlZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\NZZlkUUN3ME2wMlY4OzV7IN88US=> M{fLVnNCVkeHUh?=
MMAC-SF M1rDemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfqVFFVUUN3ME2wMlY5PjF2IN88US=> NUDrSGQxW0GQR1XS
BHT-101 MoH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPlTWM2OD1yLkewO|AzKM7:TR?= NEnP[IJUSU6JRWK=
K5 NE\GdZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPhTWM2OD1yLke2NVQ5KM7:TR?= NHrIWnRUSU6JRWK=
BV-173 NGPpNoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFuwVIpKSzVyPUCuO|k3PDRizszN MlXGV2FPT0WU
RVH-421 NHHXcVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmr5TWM2OD1yLki2O|k3KM7:TR?= MlLhV2FPT0WU
HCC2218 MmHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTBwOEe4OFQh|ryP NIHOdolUSU6JRWK=
WM-115 NXftXlhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwOEi2PVIh|ryP NIPUOllUSU6JRWK=
SK-MEL-28 NV[2UGE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHUTWM2OD1zLkC0OVY6KM7:TR?= M{jCbHNCVkeHUh?=
COLO-679 M3fmU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjDXHNKSzVyPUGuNVA1PjRizszN M125ZnNCVkeHUh?=
MZ7-mel NV3DT3NVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rNbWlEPTB;MT6xOFk3OyEQvF2= NWfheXFuW0GQR1XS
SK-MEL-30 MkD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvkTWM2OD1zLkOzN|g3KM7:TR?= M3fveXNCVkeHUh?=
NCI-H209 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3j0cWlEPTB;MT62NFg3KM7:TR?= NFzwOopUSU6JRWK=
HTC-C3 MlPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7TOWxKSzVyPUGuOlYzQTRizszN MV;TRW5ITVJ?
KARPAS-45 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPW[VBKSzVyPUKuNFQ6PzhizszN NYLSd|luW0GQR1XS
NCI-SNU-5 NFTaU|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzYbo1mUUN3ME2yMlEyQTZ7IN88US=> M33YdXNCVkeHUh?=
KP-4 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3sW3R2UUN3ME2yMlMxPzh5IN88US=> MnLHV2FPT0WU
PA-1 M3n5NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnFV3pKSzVyPUKuO|I3PzNizszN NGrpVlBUSU6JRWK=
HuO-3N1 NEPUVm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1G5[mlEPTB;Mj64O|k1PiEQvF2= MoXmV2FPT0WU
NCI-H358 NHTZWmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTJwOUKyN|Ih|ryP NUnJTIE1W0GQR1XS
CTB-1 MlHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXWxbHNKUUN3ME2zMlQxOTd4IN88US=> M{DG[HNCVkeHUh?=
697 MkPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTNwNUWyOlYh|ryP NUj1RZE{W0GQR1XS
CP66-MEL MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\Oe2lEPTB;ND6xOVkzPyEQvF2= MXXTRW5ITVJ?
NB13 MoDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTRwNEmxO|kh|ryP NGLNUWpUSU6JRWK=
DBTRG-05MG NXjwRlhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVO2dGFqUUN3ME20MlU{OzJ3IN88US=> M1u2VHNCVkeHUh?=
A2058 NWLm[pV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDMdHZoUUN3ME20MlczOTZ2IN88US=> MlHkV2FPT0WU
KG-1 NYPXb2hNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUf3c2gyUUN3ME20Mlc{QTB6IN88US=> MXTTRW5ITVJ?
8305C MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYn0VGlCUUN3ME21MlE5PzNizszN MorDV2FPT0WU
RPMI-7951 M1fjPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zlXmlEPTB;NT64NFI5OyEQvF2= Mly5V2FPT0WU
CHL-1 NGXjNmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTVwOUe2NFMh|ryP NWWzbWxoW0GQR1XS
TI-73 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\3TmlEPTB;Nj6wNFkxOiEQvF2= NUH2ZlNJW0GQR1XS
HT-1080 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\CNmlEPTB;Nj6xNFk1PiEQvF2= M2TkVXNCVkeHUh?=
ES5 MlTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTZwMUS5NlQh|ryP NVPzbZhLW0GQR1XS
8-MG-BA MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml:zTWM2OD14LkG4NVI6KM7:TR?= M17hRnNCVkeHUh?=
NB7 M322cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfBWVRxUUN3ME22MlIyOzd|IN88US=> NUPtbmF6W0GQR1XS
H4 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Lqd2lEPTB;Nj6yNlQ6OyEQvF2= M2\UNXNCVkeHUh?=
CAL-72 MljCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTZwNEW0NlMh|ryP M33vcXNCVkeHUh?=
HCC1806 NInyVoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DZRWlEPTB;Nj64NVk{OSEQvF2= MnnVV2FPT0WU
BCPAP M2j6fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTdwMkG3OlQh|ryP M1HQPXNCVkeHUh?=
LB2241-RCC MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\XTYpKSzVyPUeuN|Y6ODdizszN M2O5SnNCVkeHUh?=
COLO-741 NVXCOWx[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXQPHdKSzVyPUiuNFE3PzlizszN NVu5boxNW0GQR1XS
HSC-3 M2LRVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rxdWlEPTB;OD6wO|A3QCEQvF2= MX7TRW5ITVJ?
SW982 M17udWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvIS5hvUUN3ME24MlQyPTF4IN88US=> NIXFUJlUSU6JRWK=
GCT Ml:4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fJ[GlEPTB;OD63OVMyPCEQvF2= MorWV2FPT0WU
KY821 M1zNSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXjPGNqUUN3ME25MlA2OTd6IN88US=> NGn1eIxUSU6JRWK=
JVM-3 NF7PNldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjr[o5rUUN3ME25MlU3QTl7IN88US=> NUO2eJBEW0GQR1XS
RS4-11 NVvkV2Z1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTlwNkC0PEDPxE1? NXr5XJpMW0GQR1XS
VA-ES-BJ M1TJ[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn76TWM2OD1zMD6wNVQ6KM7:TR?= Mon3V2FPT0WU
A431 M37uc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXxTWM2OD1zMD60NlEzKM7:TR?= NUDmcFF{W0GQR1XS
LXF-289 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\kTWM2OD1zMD60OVgh|ryP NITOPJBUSU6JRWK=
SK-MEL-24 NXnVU3UyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTjTWM2OD1zMD64Nlc1KM7:TR?= M2j2cnNCVkeHUh?=
NOS-1 NYTT[ZptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3uwNGlEPTB;MUCuPFQ4OiEQvF2= NFLrZoJUSU6JRWK=
KNS-62 M1XJTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrITWM2OD1zMT6yOFA1KM7:TR?= NYLUbmJsW0GQR1XS
SK-HEP-1 M4LFN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnvTWM2OD1zMT6zOVI4KM7:TR?= MmD2V2FPT0WU
A3-KAW NETnPFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFzLkexO|gh|ryP MlL6V2FPT0WU
SK-LU-1 NWn0dIhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\qUopKSzVyPUGyMlI3PTVizszN NVHPd4pVW0GQR1XS
TYK-nu MkXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFe0XnVKSzVyPUGyMlM6OzJizszN MY\TRW5ITVJ?
NMC-G1 NIrLbppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7wU3dkUUN3ME2xNk43ODZ{IN88US=> M3XjTHNCVkeHUh?=
BB65-RCC MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTF{LkexOlkh|ryP Mn3GV2FPT0WU
QIMR-WIL NInEXHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjuTWM2OD1zMj64PFM{KM7:TR?= MXnTRW5ITVJ?
D-566MG MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPRTWM2OD1zMz65OVc3KM7:TR?= NVv5TpE6W0GQR1XS
KYSE-140 Mnz0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHYTWM2OD1zND6wO|U{KM7:TR?= MYfTRW5ITVJ?
SCC-4 M{nUcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XoWGlEPTB;MUSuN|M2QSEQvF2= NYfQSYhIW0GQR1XS
U251 NWnYdJBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHUTWM2OD1zND64OFkzKM7:TR?= NV;ZRXJFW0GQR1XS
D-542MG MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml35TWM2OD1zND65NlIzKM7:TR?= M4WyVXNCVkeHUh?=
LAMA-84 MlPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfWfYJKSzVyPUG0Mlk6OzJizszN M4LsOHNCVkeHUh?=
NCI-H720 MnH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3UTWM2OD1zNT6yOlg1KM7:TR?= M1K2RnNCVkeHUh?=
DEL NY\lTJQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3ETWM2OD1zNT60Nlk{KM7:TR?= Mn3QV2FPT0WU
SBC-1 NUTo[HE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjZOYtKSzVyPUG1MlQ{ODVizszN NGexPJVUSU6JRWK=
ECC10 NInIdI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrYdoxKSzVyPUG1MlQ1PThizszN NWm0NpVEW0GQR1XS
Daoy NV\PZndMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTF3Lke2NVYh|ryP NYS4NndXW0GQR1XS
SCH Mn3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTF3Lke4N|Uh|ryP M4Ox[XNCVkeHUh?=
MZ2-MEL MkLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWCzSpF7UUN3ME2xOk4xPjR4IN88US=> MVzTRW5ITVJ?
CAL-12T M2jvWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTF4LkS4OlIh|ryP MVLTRW5ITVJ?
KE-37 M2PKbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHETWM2OD1zNj64NVA4KM7:TR?= M2nXOnNCVkeHUh?=
LS-411N MlTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mon1TWM2OD1zNz6xNVgh|ryP MoH6V2FPT0WU
NCI-H2228 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXqcIhJUUN3ME2xO{4{ODdzIN88US=> NGfHNIFUSU6JRWK=
SK-MEL-2 M1;KRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPBRY5FUUN3ME2xO{41QTZ3IN88US=> M{nhXHNCVkeHUh?=
HN M4DPXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXnWVhKSzVyPUG3MlczPDhizszN MorBV2FPT0WU
NCI-H1648 M1H2dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYG2S|hNUUN3ME2xO{45OThizszN MnWzV2FPT0WU
IA-LM NUDNU2xkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPhO49KSzVyPUG4MlMyPzJizszN NGSxUplUSU6JRWK=
EW-13 NUDWNlBsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTF6LkW3NFgh|ryP MnzoV2FPT0WU
YKG-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmW3TWM2OD1zOT61O|EyKM7:TR?= NF64[VlUSU6JRWK=
KNS-81-FD MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLkUI5KSzVyPUG5MlU5PThizszN NED3fo9USU6JRWK=
23132-87 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTF7Lke2OFIh|ryP Mn7sV2FPT0WU
NUGC-3 M17GRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYf5TnZwUUN3ME2xPU46QDh5IN88US=> NXzYN5E3W0GQR1XS
5637 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTJyLkC0O|gh|ryP NFjRcJlUSU6JRWK=
NCI-H1755 M4fJeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTJyLkS3OlQh|ryP MWjTRW5ITVJ?
RH-18 M4\tPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHpeJVKSzVyPUKwMlU4PDhizszN NGDRR2dUSU6JRWK=
RXF393 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\wZ|ZWUUN3ME2yNE43PzV4IN88US=> MWHTRW5ITVJ?
LU-134-A M4njXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDZU21JUUN3ME2yNE44ODV4IN88US=> M1\qOnNCVkeHUh?=
TE-12 MlT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTBTWM2OD1{MD63NlAyKM7:TR?= M3y0dHNCVkeHUh?=
MOLT-4 NGjKc4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnkPJNKSzVyPUKxMlE6OTVizszN M1v5O3NCVkeHUh?=
IGR-1 NHjk[VZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXixWpdbUUN3ME2yNU4{Pzl4IN88US=> MYDTRW5ITVJ?
HOP-92 M3fvV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fKdWlEPTB;MkGuOFk5PyEQvF2= MkXxV2FPT0WU
SK-MES-1 MoTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33TW2lEPTB;MkGuO|M5OSEQvF2= MlfFV2FPT0WU
LU-65 NW\BRZZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfjWIJKSzVyPUKxMlg3OjRizszN MXHTRW5ITVJ?
MS-1 MknNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnT4TWM2OD1{Mj6xNlA{KM7:TR?= NFPITHZUSU6JRWK=
LoVo MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfqRVBKSzVyPUKyMlI1PCEQvF2= MWTTRW5ITVJ?
A704 MoTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDKdotKSzVyPUKyMlUyPTVizszN NUXVfndnW0GQR1XS
HT-1376 NXrXcHE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{L3[2lEPTB;MkKuOlA2QSEQvF2= M{fkPXNCVkeHUh?=
IST-MEL1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TuemlEPTB;MkKuOlc2OSEQvF2= M2DV[nNCVkeHUh?=
Ramos-2G6-4C10 NVzOVXRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTJ{LkezOlYh|ryP NEjySpVUSU6JRWK=
T47D M2PpeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTJ{Lke5O|kh|ryP MVnTRW5ITVJ?
HT-1197 NVPIRmlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIe1N3FKSzVyPUKzMlA5OTdizszN MVrTRW5ITVJ?
LB2518-MEL M13YNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTJ|Lk[0NVIh|ryP MmfHV2FPT0WU
J-RT3-T3-5 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH6zeVFKSzVyPUK0Mlc2QTVizszN NIDJVGhUSU6JRWK=
SK-NEP-1 MnTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPHUVNKSzVyPUK0Mlg4PDRizszN MkHDV2FPT0WU
NCI-H526 MnH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHGTWM2OD1{NT6wNFI{KM7:TR?= M2L2WnNCVkeHUh?=
IST-SL1 M1nuVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX70dVd2UUN3ME2yOU4zPzVzIN88US=> M33MXXNCVkeHUh?=
HH NEm3bmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\XTWM2OD1{NT6zNVkzKM7:TR?= NUDrVHRLW0GQR1XS
NCI-H82 MnO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fxemlEPTB;MkWuPVM5KM7:TR?= NFPCPVJUSU6JRWK=
SNU-449 MorTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;SRVRKSzVyPUK3MlIxOThizszN NF3PVFdUSU6JRWK=
COR-L23 NXf3fWZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojRTWM2OD1{Nz6yPFE{KM7:TR?= M3LiXHNCVkeHUh?=
LOXIMVI NY\EV|hsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTXcVNKSzVyPUK3MlM3QCEQvF2= M3i4UXNCVkeHUh?=
GR-ST MonpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jk[GlEPTB;MkeuOlcxPiEQvF2= NFjybVVUSU6JRWK=
NCI-SNU-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17wWWlEPTB;MkeuPVQ1KM7:TR?= MWnTRW5ITVJ?
ALL-PO MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTJ6LkG2NFQh|ryP MUjTRW5ITVJ?
ML-2 M2P5N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXFTWM2OD1{OD6yPFE1KM7:TR?= NWroUY9xW0GQR1XS
HOP-62 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXRTWM2OD1{OD63NVMh|ryP NFLaNI9USU6JRWK=
EGI-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTJ6Lki4OFUh|ryP NVLzUGpCW0GQR1XS
TCCSUP NY\yZ5liT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWroXmZUUUN3ME2yPE46Ojd{IN88US=> MYjTRW5ITVJ?
LB996-RCC NFHWcVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTJ7LkW2PFIh|ryP MYfTRW5ITVJ?
LCLC-97TM1 M2\IUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDYeHlkUUN3ME2zNk4yQTZ2IN88US=> M1foPXNCVkeHUh?=
NCI-H1304 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlf2TWM2OD1|Mj6zN|AyKM7:TR?= NGTXUYVUSU6JRWK=
KP-N-YS M4\4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTN{LkW5O|Mh|ryP MkW1V2FPT0WU
NCI-H1770 Mn3LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\Rc2lEPTB;M{OuNVY1QCEQvF2= MVXTRW5ITVJ?
EM-2 M{K3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTN|Lk[1NFQh|ryP NVe3eZRzW0GQR1XS
ChaGo-K-1 MlX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NImxXnhKSzVyPUOzMlczOzZizszN Mnn4V2FPT0WU
ACHN MoL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHvN|R1UUN3ME2zN{45Ozh3IN88US=> NXXyXpVlW0GQR1XS
MN-60 M2nqcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTN|Lki1OFQh|ryP NW\GbFY2W0GQR1XS
EW-18 MkPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHtbGdjUUN3ME2zN{45QTdzIN88US=> NEj3V|dUSU6JRWK=
KGN MlvrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zZOWlEPTB;M{WuO|I6OiEQvF2= MUjTRW5ITVJ?
U031 NXT1TZlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTN3LkixN|Ih|ryP M1jMfXNCVkeHUh?=
HMV-II MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[1PWlEPTB;M{[uNFc4PCEQvF2= MVvTRW5ITVJ?
L-363 MnP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PMdGlEPTB;M{euOlQ2PSEQvF2= NWLt[2NQW0GQR1XS
NCI-H1155 M3PpcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTN6LkCwNVUh|ryP MWjTRW5ITVJ?
NCI-H1793 MkTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTN6LkGwNlYh|ryP MnTVV2FPT0WU
P30-OHK MmDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LFR2lEPTB;M{iuNVM{OiEQvF2= M2\mUnNCVkeHUh?=
AN3-CA MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX61WVJTUUN3ME2zPE4yPjF3IN88US=> M3nvTHNCVkeHUh?=
UACC-257 MlnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfod3VKSzVyPUO4Mlc6KM7:TR?= M{jFcnNCVkeHUh?=
MCF7 MkT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTN7Lki2Nlkh|ryP NYCwSmYzW0GQR1XS
KP-N-YN Mn:wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDy[WdlUUN3ME20NE41Ojh3IN88US=> NH3zXFlUSU6JRWK=
T98G NHe2eGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfrTWM2OD12MD60PVU4KM7:TR?= NEXxRYRUSU6JRWK=
HGC-27 MofGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjwVppKUUN3ME20N{4zPzRizszN MorhV2FPT0WU
NCI-H1092 Mm[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHUTWM2OD12Mz6yPFk2KM7:TR?= NF7uOHNUSU6JRWK=
KARPAS-299 M{S1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\UenlKSzVyPUSzMlMxPzFizszN NVz5UIkzW0GQR1XS
LB1047-RCC NFruTlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;IeHBKSzVyPUS0Mlk6PTlizszN MU\TRW5ITVJ?
786-0 M3Ph[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjzWJY5UUN3ME20OU43PSEQvF2= MoXvV2FPT0WU
HCC2157 NXnhcIUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33QXmlEPTB;NE[uNFM2QSEQvF2= NIS2OppUSU6JRWK=
NY Mmf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlr2TWM2OD12Nj6xO|c5KM7:TR?= NX3VOWFrW0GQR1XS
EFM-19 MkftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIP5Z49KSzVyPUS2Mlc2OzNizszN M3y3enNCVkeHUh?=
EW-16 NIXzOmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXkTWM2OD12Nj63PFA3KM7:TR?= NVfMNpdUW0GQR1XS
UM-UC-3 Mk[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nDfmlEPTB;NE[uPFA2QSEQvF2= NXK4bGRUW0GQR1XS
HT-29 NHPFfFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DQeGlEPTB;NEeuPFc6OiEQvF2= NFziZYlUSU6JRWK=
LN-405 NFnkfXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTR6LkC4Nlch|ryP MnvqV2FPT0WU
NCI-H727 NFjHeJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTR6Lke3NlYh|ryP Mn7lV2FPT0WU
D-502MG M3ToUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIqzOppKSzVyPUS4Mlk3PzZizszN MoTMV2FPT0WU
GMS-10 NVTrfnNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTR7LkK5O|Qh|ryP MkO1V2FPT0WU
MEL-JUSO NWXlUVN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIWz[IpKSzVyPUS5MlM1PyEQvF2= NHHYeGNUSU6JRWK=

... 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)

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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