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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Cited by 49 Publications

9 Customer Reviews

  • Combinatorial knockdown of NF1 and C-RAF abrogates NF1-mediated resistance to B-RAF inhibition at the level of ERK phosphorylation. A375 cells were infected with NF1 shRNA and treated with either DMSO or PLX4720 for 16 h. Cell lysates were analyzed for the indicated proteins.

    Cancer Discov 2013 3, 350-62. PLX-4720 purchased from Selleck.

    RAF inhibitors induce dimer formation between KSR and RAF, and activate KSR by CRAF. (A) GDC0879 but not PLX4720 induces BRAF/CRAF dimers. Cells overexpressing myc-CRAF and BRAF were treated with drug for 1 h and CRAF immunoprecipitates were immunoblotted for BRAF and CRAF (epitope tagged with myc). (B) GDC0879 but not PLX4720 enhances KSR/BRAF complexes. KSR immunoprecipitates were prepared from cells overexpressing FLAG-KSR and BRAF after treatment with the indicated drug for 1 h and immunoblotted using antibodies to BRAF. (C) Both GDC0879 and PLX4720 induce KSR/CRAF complexes.KSR immunoprecipitates were prepared from cells overexpressing FLAG-KSR and myc-CRAF after treatment with the indicated drug for 1 h and immunoblotted for CRAF using myc antibodies. (D and E) Requirement of KSR for drug-induced ERK activation. Lysates fromwild-type and KSR deficient fibroblasts, transfected with RASV12, were treated with the indicated doses of either GDC-0879 (D) or PLX4720 (E) for 1 h. Lysates were immunoblotted for phospho-ERK1 and 2, ERK2, and RASV12. (F) KSR and CRAF cooperate to activate MEK. Cells expressing the indicated constructs were treated with a 50 μM PLX4720 for 2 h before cell lysates were prepared and analyzed for pMEK by immunoblotting. CRAF(TM) refers to the T421M gatekeeper mutant that cannot bind to the drug(4). (G) KSR in vitro kinase reactions. Cells were cotransfected with WT or ATP binding deficient KSR and CRAF and immunoprecipitates prepared after cells were treated with an activating dose of PLX (10 μM) for 1 h. KSR immunoprecipitates were prepared, pretreated with 50 uM PLX4720 to inhibit coprecipitating RAF activity, and then tested for kinase activity using purified MEK. MEK phosphorylation was detected using a pMEK specific antibody.

    Proc Natl Acad Sci USA 2011 108, 6067-6072. PLX-4720 purchased from Selleck.

  • (D)Melanoma cell lines were treated with 0.5 uM Pi-103 and/or 2 uM PLX4720 for 4 h. Samples were analyzed by Western blotting for the indicated proteins. β-Actin served as a loading control. (E) Melanoma cell lines were treated with a dilution series of Pi-103 either alone or in combination with the BRAFV600E inhibitor PLX4720 at a concentration of 3 uM (D10) or 1 uM (453A0) for 3 d. Total cell numbers were determined with a cell titer blue assay. The Y-axis represents the percentage of living cells.

    Genes Dev 2012 26, 1055-69. PLX-4720 purchased from Selleck.

    PTEN predicts for PLX4720-induced apoptosis. A, basal PTEN and phospho-AKT(pAKT; S473, T308) expression in PTENt (WM164, 451Lu, SK-mel-28, WM983A, WM35, WM51) and PTEN (WM239A, WM266-4, WM793, M233, WM9, 1205Lu) melanoma cell lines. B, MTT assay of PTENt (gray)-expressing versus PTEN (black) cell lines. C, PTENt cells are more sensitive than PTEN cells to PLX4720-mediated apoptosis. Cells treated for 48 hours with 3 or 10 μmol/L PLX4720 before being stained for TMRM and Annexin-V. Apoptosis was measured by flow cytometry. Data shows mean SE mean of 3 independent experiments.*, PTENt cohort significantly different from PTEN cohort(P < 0.05).

    Cancer Res 2011 71, 2750-2760. PLX-4720 purchased from Selleck.

  • Loss of PTEN is associated with PI3K/AKT signaling following BRAF inhibition. A, PTENt (WM35, WM164, WM983A) and PTEN (M233, WM9,WM793, 1205Lu) cells were treated with PLX4720 (24 hours: 0.03-3 μmol/L) and probed for phospho-PDK1 (pPDK1), total PDK1, phospho-AKT (pAKT), total AKT (tAKT), phospho-S6 (pS6), and total S6. Numbers indicate relative intensity of pPDK1 normalized to PDK1 and pAKT normalized to tAKT. B, PLX4720 increases pAKT following PTEN knockdown. WM35 cells were incubated with nontargeting siRNA (NT) or 2 different PTEN-specific siRNA's (PTEN) before treatment with either vehicle or PLX4720 (3 μmol/L). C, siRNA knockdown of BRAF increases pAKT in melanoma cell lines that are PTEN. WM164 (PTENt) and WM793 (PTEN) cells were incubated with lipofectamine alone (L), nontargeting siRNA (NT), or BRAF-specific siRNA (BRAF). Protein was extracted, resolved, and probed for BRAF, pAKT, total AKT, and GAPDH.

     

     

    Cancer Res 2011 71, 2750-2760. PLX-4720 purchased from Selleck.

    Dual PI3K/BRAF inhibition upregulates BIM and enhances apoptosis in PTEN cells. A, left, Western blot of 1205Lu cells treated with PLX4720 (3 μmol/L, 48 hours), the PI3K inhibitor GDC-0941 (3 μmol/L, 48 hours), or both drugs in combination (PtG); right, immunofluorescence staining of BIM (green) and DAPI (blue) in PTEN cells following PLX4720 treatment (3 μmol/L, 48 hours), the PI3K inhibitor LY294002 (10 μmol/L, 48 hours), or both drugs in combination (PLXtLY). B, left, immunofluorescence staining of PTEN 1205Lu following combined inhibition (3 μmol/L PLX4720 t 10 μmol/L LY294002, 48hours) increases nuclear localization of FOXO3a (green). DAPI is shown in blue. Magnification 40. Right, combined inhibition (3 μmol/L PLX4720 t 10 μmol/L LY294002, 48 hours) increases PTEN WM793 BIM mRNA levels to those observed with single BRAF inhibition (3 μmol/L PLX4720, 48 hours) in the PTENt WM35. C, PTEN cells were treated with PLX4720 (3 μmol/L, 48 hours), GDC-0941 (3 μmol/L, 48hours), or a combination of the 2 drugs (3Pt3G) before Annexin-V staining was analyzed by flow cytometry (*, P < 0.05 between the drug combination and each inhibitor alone). D, combined BRAF/PI3K inhibitor treatment blocks the escape of 1205Lu cells (PTEN) from therapy. Spheroids of 1205Lu cells were treated with either PLX4720 alone (3 and 10 μmol/L: data shows 3 μmol/L), LY294002 (10 μmol/L) alone or a combination of the 2 drugs for 72 hours. In other studies, spheroids were treated with drugs for 72 hours and then allowed to recover for 120 hours. Micrograph shows viability staining (green ?live cells, red ?dead cells). Magnification 10.

    Cancer Res 2011 71, 2750-2760. PLX-4720 purchased from Selleck.

  • LC-MRM identifies differential regulation of BIM in PTENt and PTEN cell lines following PLX4720 treatment. A, representative LC-MRM data showing the fold changes in the expression of Bak, Bax, Bcl-2, Bcl-w, Bcl-xL, BID, BIM, Bok, and Mcl-1 over internal standard in the WM164 (PTENt) and 1205Lu (PTEN) cell lines following treatment with PLX4720 (10 μmol/L, 0-48 hours). Statistical analysis of BIM fold change in PTEN versus PTENt. *, P < 0.05. B, Western blot showing BIM expression following PLX4720 treatment (10 μmol/L, 0-48 hours) in PTEN (WM793, 1205Lu) and WM164 cell lines (PTENt). C, immunofluorescence staining, showing expression of BIM and DAPI staining of PTEN (M233, WM9, WM793, 1205Lu) and PTENt (WM35, WM164, WM983A) cells following PLX4720 treatment (3 μmol/L, 48 hours).D, Western blot showing BAD phosphorylation following treatment with PLX4720 (0-48 hours) in PTEN (WM793,1205Lu) and PTENt WM164. Annexin V binding following treatment with 3 or 10 μmol/L PLX4720 (48 hours) showing increased apoptosis in WM793 stably overexpressing WT BAD. *, P < 0.05.

    Cancer Res 2011 71, 2750-2760. PLX-4720 purchased from Selleck.

    B-RafV600E mutated melanoma line, SK-MEL-28, was treated with different doses of PLX-4720 for 4 h or 22 h.  Cell lysates were analyzed by Western blotting to determine the levels of phosphorylated MEK1/2 (pMEK1/2) and phosphorylated ERK1/2 (pERK1/2). MEK1/2 is the substrate of B-Raf while ERK1/2 is the substrate of MEK1/2.  Data show that phosphorylation of MEK1/2 and ERK1/2 was significantly inhibited by PLX-4720 treatment although total MEK1/2 or ERK1/2 protein levels were not affected. No pMEK1/2 or pERK1/2 signal was detected even after prolonged exposure, indicating that the inhibitor at 1 μM is very effective in blocking the constitutive kinase activity of B-RafV600E.  This data is consistent with the previous result demonstrating the effect of PLX-4720 in the B-RafV600E mutated melanoma line, A375 – Fig. 2A, Nature 464:431 (2010)

     

     

    Dr. Jong-In Park of Medical College of Wisconsin. PLX-4720 purchased from Selleck.

  • A dose titration of PLX-4720 in A375 melanoma cells which possess a V600E B-Raf mutation.Effects of  increasing PLX-4720 dose on Erk phosphorylation and on tumor cell proliferation as determined by MTT  assay are shown.

     

     

    Dr. Daniel C.Cho of Harvard Medical School. PLX-4720 purchased from Selleck.

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 NFzub|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\ne2pTUUN3ME2wMlA4PDV5IN88US=> M4D5VnNCVkeHUh?=
EoL-1-cell MnjHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF31PYhKSzVyPUCuNVQyPjZizszN M4n2SnNCVkeHUh?=
C32 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLDTWM2OD1yLkG1NVMyKM7:TR?= NFr4dHNUSU6JRWK=
M14 M1Pr[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\PbJlXUUN3ME2wMlIyPzV5IN88US=> Ml\RV2FPT0WU
CP50-MEL-B NIfjPVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{j5cWlEPTB;MD6yPVc5PCEQvF2= NYnFeoJ4W0GQR1XS
A101D M37xZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[1TWM2OD1yLkOyOVg6KM7:TR?= MmPPV2FPT0WU
G-361 M3\j[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHOfmJJUUN3ME2wMlM1PjN5IN88US=> MlrzV2FPT0WU
HT-144 NWHXV|lKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;WTWM2OD1yLkO2N|I6KM7:TR?= M1jNdnNCVkeHUh?=
ACN MnnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHyeYNKSzVyPUCuN|g1PzdizszN NUmzVXQ4W0GQR1XS
COLO-829 M1LxUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYKzPJFYUUN3ME2wMlM5QTZ6IN88US=> NGLQO2dUSU6JRWK=
MEL-HO MlfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTBwNEGxO|kh|ryP MnrvV2FPT0WU
SH-4 NH\LblFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTBwNEG0NlIh|ryP MYjTRW5ITVJ?
SK-MEL-3 NEHSUnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDvcVNKSzVyPUCuOVE2PjhizszN MVvTRW5ITVJ?
A375 NHi0R4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXJPGt{UUN3ME2wMlY4OzV7IN88US=> MmrMV2FPT0WU
MMAC-SF M1\Pdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXT6Z21pUUN3ME2wMlY5PjF2IN88US=> NWfiU3g2W0GQR1XS
BHT-101 MmXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXCTWM2OD1yLkewO|AzKM7:TR?= MnzyV2FPT0WU
K5 NGi2UphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHGUZljUUN3ME2wMlc3OTR6IN88US=> MlnmV2FPT0WU
BV-173 M2KyZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFv1b2dKSzVyPUCuO|k3PDRizszN NGLMNW1USU6JRWK=
RVH-421 MojPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIK4W3lKSzVyPUCuPFY4QTZizszN M1z0V3NCVkeHUh?=
HCC2218 NI[yfXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW[1Z5RVUUN3ME2wMlg4QDR2IN88US=> NUjIdYNQW0GQR1XS
WM-115 M{jsSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLtTWM2OD1yLki4OlkzKM7:TR?= MWfTRW5ITVJ?
SK-MEL-28 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3qfmtKSzVyPUGuNFQ2PjlizszN NUj1c3JkW0GQR1XS
COLO-679 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTFwMUC0OlQh|ryP MV3TRW5ITVJ?
MZ7-mel MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzLTWM2OD1zLkG0PVY{KM7:TR?= NELDWlRUSU6JRWK=
SK-MEL-30 NH\P[ohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrWTWM2OD1zLkOzN|g3KM7:TR?= NHHPO|lUSU6JRWK=
NCI-H209 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFv0NIpKSzVyPUGuOlA5PiEQvF2= MYjTRW5ITVJ?
HTC-C3 NVHv[ZRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVj5OIQ4UUN3ME2xMlY3Ojl2IN88US=> NVj2NYFEW0GQR1XS
KARPAS-45 NX7ndFdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7nTGtKSzVyPUKuNFQ6PzhizszN NUD2TGJYW0GQR1XS
NCI-SNU-5 NV7qNnJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3z1emlEPTB;Mj6xNVk3QSEQvF2= MojlV2FPT0WU
KP-4 NIm3emxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTJwM{C3PFch|ryP NH6yVWpUSU6JRWK=
PA-1 M1O4Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEe2OFlKSzVyPUKuO|I3PzNizszN NHLwcWFUSU6JRWK=
HuO-3N1 NYrPVGdPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3FN2JGUUN3ME2yMlg4QTR4IN88US=> NH3LeWhUSU6JRWK=
NCI-H358 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmi3TWM2OD1{LkmyNlMzKM7:TR?= NYDmNJE5W0GQR1XS
CTB-1 M3H2UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHez[2FKSzVyPUOuOFAyPzZizszN NYXPfYNEW0GQR1XS
697 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3yzV2lEPTB;Mz61OVI3PiEQvF2= M4\QZXNCVkeHUh?=
CP66-MEL M3raN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[4TWM2OD12LkG1PVI4KM7:TR?= M2jJXHNCVkeHUh?=
NB13 NEO3bmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D6UWlEPTB;ND60PVE4QSEQvF2= NF;5dGlUSU6JRWK=
DBTRG-05MG MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYC3VWc3UUN3ME20MlU{OzJ3IN88US=> NEPvXnpUSU6JRWK=
A2058 MnHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnq5TWM2OD12LkeyNVY1KM7:TR?= Mly0V2FPT0WU
KG-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTRwN{O5NFgh|ryP MlvOV2FPT0WU
8305C MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnmVXNKSzVyPUWuNVg4OyEQvF2= M1LyOnNCVkeHUh?=
RPMI-7951 M2\2fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTVwOECyPFMh|ryP MVfTRW5ITVJ?
CHL-1 NXH1eYdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7iNXR4UUN3ME21Mlk4PjB|IN88US=> M4i3VnNCVkeHUh?=
TI-73 MlLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoGwTWM2OD14LkCwPVAzKM7:TR?= MVzTRW5ITVJ?
HT-1080 MmXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTZwMUC5OFYh|ryP NIHoZ4xUSU6JRWK=
ES5 Mkf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXKTWM2OD14LkG0PVI1KM7:TR?= NF70NI1USU6JRWK=
8-MG-BA MnHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTZwMUixNlkh|ryP M3PSW3NCVkeHUh?=
NB7 M2K5[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3r4UGlEPTB;Nj6yNVM4OyEQvF2= MVfTRW5ITVJ?
H4 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTZwMkK0PVMh|ryP MlXnV2FPT0WU
CAL-72 M4DlNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXyyWnZ3UUN3ME22MlQ2PDJ|IN88US=> M3HBSnNCVkeHUh?=
HCC1806 Mly3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrie|NKSzVyPU[uPFE6OzFizszN M2DMc3NCVkeHUh?=
BCPAP MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fnUGlEPTB;Nz6yNVc3PCEQvF2= Mo\3V2FPT0WU
LB2241-RCC M1rkfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTdwM{[5NFch|ryP MYPTRW5ITVJ?
COLO-741 M4jSdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRThwMEG2O|kh|ryP NGj5cVVUSU6JRWK=
HSC-3 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LUW2lEPTB;OD6wO|A3QCEQvF2= NW\IWXFQW0GQR1XS
SW982 M4XKe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRThwNEG1NVYh|ryP NVrRRpgxW0GQR1XS
GCT NFvGcVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDPcGwyUUN3ME24Mlc2OzF2IN88US=> NXHZU5A3W0GQR1XS
KY821 M3rwdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXye3dKSzVyPUmuNFUyPzhizszN NIr4d25USU6JRWK=
JVM-3 M3rTbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXITWM2OD17LkW2PVk6KM7:TR?= M1HxTHNCVkeHUh?=
RS4-11 NXzWbJBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTlwNkC0PEDPxE1? MlvTV2FPT0WU
VA-ES-BJ Mmm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\j[WlEPTB;MUCuNFE1QSEQvF2= MXLTRW5ITVJ?
A431 NV\yRWdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHF[GZKSzVyPUGwMlQzOTJizszN NF3J[Y5USU6JRWK=
LXF-289 NFTxVG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3Pe4dSUUN3ME2xNE41PThizszN NVrLZ3loW0GQR1XS
SK-MEL-24 M3Syb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TBR2lEPTB;MUCuPFI4PCEQvF2= MU\TRW5ITVJ?
NOS-1 NIP5[YRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2n6dmlEPTB;MUCuPFQ4OiEQvF2= M33RbHNCVkeHUh?=
KNS-62 Mk\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHTc2tKSzVyPUGxMlI1ODRizszN MWHTRW5ITVJ?
SK-HEP-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LW[2lEPTB;MUGuN|UzPyEQvF2= NV7PflVIW0GQR1XS
A3-KAW M4XPZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1P3ZmlEPTB;MUGuO|E4QCEQvF2= MWLTRW5ITVJ?
SK-LU-1 NEKyV4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUmxd2xJUUN3ME2xNk4zPjV3IN88US=> Ml7kV2FPT0WU
TYK-nu M4j4VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULUfopGUUN3ME2xNk4{QTN{IN88US=> M1vlUXNCVkeHUh?=
NMC-G1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTF{Lk[wOlIh|ryP MkHiV2FPT0WU
BB65-RCC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jje2lEPTB;MUKuO|E3QSEQvF2= NX;RcZZFW0GQR1XS
QIMR-WIL NYf2VoFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofSTWM2OD1zMj64PFM{KM7:TR?= M1P6SnNCVkeHUh?=
D-566MG MnftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTF|Lkm1O|Yh|ryP MUDTRW5ITVJ?
KYSE-140 M1rEUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDhV3lRUUN3ME2xOE4xPzV|IN88US=> NWDCOlI5W0GQR1XS
SCC-4 MoGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvkfYNKSzVyPUG0MlM{PTlizszN NIj1VHJUSU6JRWK=
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HH M333OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnGNo9bUUN3ME2yOU4{OTl{IN88US=> MWHTRW5ITVJ?
NCI-H82 NH;MeXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILMNIRKSzVyPUK1Mlk{QCEQvF2= NWW5XnNrW0GQR1XS
SNU-449 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ThOmlEPTB;MkeuNlAyQCEQvF2= M3LtVnNCVkeHUh?=
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NCI-SNU-1 NGm2eFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJ5Lkm0OEDPxE1? MmfkV2FPT0WU
ALL-PO NVmybGt6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTZTWM2OD1{OD6xOlA1KM7:TR?= M4fhe3NCVkeHUh?=
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HOP-62 NF7xT3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTJ6LkexN{DPxE1? MWHTRW5ITVJ?
EGI-1 MmSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITT[41KSzVyPUK4Mlg5PDVizszN M1;IZnNCVkeHUh?=
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LCLC-97TM1 Ml3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTN{LkG5OlQh|ryP Mo\rV2FPT0WU
NCI-H1304 NHTuTYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{THSmlEPTB;M{KuN|MxOSEQvF2= NEPtZlFUSU6JRWK=
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NCI-H1770 M3:x[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXIWohzUUN3ME2zN{4yPjR6IN88US=> MkPDV2FPT0WU
EM-2 NEPpNG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTN|Lk[1NFQh|ryP NX3YRZBbW0GQR1XS
ChaGo-K-1 M1nxPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfTU49RUUN3ME2zN{44OjN4IN88US=> NITzTZVUSU6JRWK=
ACHN M1TrfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3G0T2lEPTB;M{OuPFM5PSEQvF2= Mmq4V2FPT0WU
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KGN MkTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTN3LkeyPVIh|ryP NGCyU3VUSU6JRWK=
U031 NUnWO2k1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH36VZBKSzVyPUO1MlgyOzJizszN MVXTRW5ITVJ?
HMV-II M{fYU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;ZTWM2OD1|Nj6wO|c1KM7:TR?= NGLieIhUSU6JRWK=
L-363 Mn7sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TmZWlEPTB;M{euOlQ2PSEQvF2= NUXFTWR4W0GQR1XS
NCI-H1155 M1TKeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFP0SHpKSzVyPUO4MlAxOTVizszN NVPmfoFiW0GQR1XS
NCI-H1793 NWTQZng4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXUUlRKSzVyPUO4MlExOjZizszN MlXXV2FPT0WU
P30-OHK NEDyUVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTN6LkGzN|Ih|ryP NV;tbmw2W0GQR1XS
AN3-CA NXrDfFF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfhTWM2OD1|OD6xOlE2KM7:TR?= MkPNV2FPT0WU
UACC-257 M4XNRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2ezOmlEPTB;M{iuO|kh|ryP M2jiWHNCVkeHUh?=
MCF7 M17KPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITiN4JKSzVyPUO5Mlg3OjlizszN NV[2OYs1W0GQR1XS
KP-N-YN NWriO417T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DndmlEPTB;NECuOFI5PSEQvF2= MlzNV2FPT0WU
T98G M2DXOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\LeVBqUUN3ME20NE41QTV5IN88US=> Mof5V2FPT0WU
HGC-27 NUTuZVU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHOWWlKSzVyPUSzMlI4PCEQvF2= NXTaZZRlW0GQR1XS
NCI-H1092 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLEPXI1UUN3ME20N{4zQDl3IN88US=> NVzJW2Z2W0GQR1XS
KARPAS-299 NH\t[mNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13aSWlEPTB;NEOuN|A4OSEQvF2= NG\O[mhUSU6JRWK=
LB1047-RCC NEn6bnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETpc4VKSzVyPUS0Mlk6PTlizszN NWrXfodoW0GQR1XS
786-0 MomwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDFTWM2OD12NT62OUDPxE1? NYPiTGNPW0GQR1XS
HCC2157 M4fpb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XudWlEPTB;NE[uNFM2QSEQvF2= Ml3zV2FPT0WU
NY M122Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7M[VJEUUN3ME20Ok4yPzd6IN88US=> MV7TRW5ITVJ?
EFM-19 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrrfFZLUUN3ME20Ok44PTN|IN88US=> MnHSV2FPT0WU
EW-16 MkK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjMXW45UUN3ME20Ok44QDB4IN88US=> MnL5V2FPT0WU
UM-UC-3 NIjRV2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTCR5BKSzVyPUS2MlgxPTlizszN MXXTRW5ITVJ?
HT-29 NUXTb2llT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vFfGlEPTB;NEeuPFc6OiEQvF2= MX3TRW5ITVJ?
LN-405 M3vmRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTR6LkC4Nlch|ryP NXLLc5lUW0GQR1XS
NCI-H727 MlfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn3O3JFUUN3ME20PE44PzJ4IN88US=> MUHTRW5ITVJ?
D-502MG MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[5OFRKSzVyPUS4Mlk3PzZizszN M2LJRnNCVkeHUh?=
GMS-10 NWKx[llXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;mTWM2OD12OT6yPVc1KM7:TR?= MkDzV2FPT0WU
MEL-JUSO NV7NR3NWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTR7LkO0O{DPxE1? MUfTRW5ITVJ?

... Click to View More Cell Line Experimental Data

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

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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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