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
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Cited by 46 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.

    (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.

  • 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.

    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 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXe0XotZUUN3ME2wMlA4PDV5IN88US=> NIr1U21USU6JRWK=
EoL-1-cell NGOy[|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTBwMUSxOlYh|ryP NVXsbZRjW0GQR1XS
C32 NVr6elFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rPbmlEPTB;MD6xOVE{OSEQvF2= MYDTRW5ITVJ?
M14 Mo\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3yTWM2OD1yLkKxO|U4KM7:TR?= NGDSNFlUSU6JRWK=
CP50-MEL-B MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHvTWM2OD1yLkK5O|g1KM7:TR?= NV3mV3UzW0GQR1XS
A101D M33xUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPLNHRKSzVyPUCuN|I2QDlizszN NWSwN3hiW0GQR1XS
G-361 NYHa[mh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jjUWlEPTB;MD6zOFY{PyEQvF2= MW\TRW5ITVJ?
HT-144 MoO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXo[GlKSzVyPUCuN|Y{OjlizszN MorMV2FPT0WU
ACN MkTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTiTWM2OD1yLkO4OFc4KM7:TR?= M4PKfnNCVkeHUh?=
COLO-829 NVfTfZZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHjTWM2OD1yLkO4PVY5KM7:TR?= MkCxV2FPT0WU
MEL-HO NHjQSo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTBwNEGxO|kh|ryP NUHkT5NIW0GQR1XS
SH-4 NGPpbpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHuTWM2OD1yLkSxOFIzKM7:TR?= MnqyV2FPT0WU
SK-MEL-3 M4naTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTBwNUG1Olgh|ryP M1PJenNCVkeHUh?=
A375 Mn20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDsNpZKSzVyPUCuOlc{PTlizszN NYLFUnlwW0GQR1XS
MMAC-SF Ml7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3wSYlKSzVyPUCuOlg3OTRizszN MnfhV2FPT0WU
BHT-101 NU[2WmJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M36yTWlEPTB;MD63NFcxOiEQvF2= MlPWV2FPT0WU
K5 M2rTcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnHeYZmUUN3ME2wMlc3OTR6IN88US=> NUO4SoxqW0GQR1XS
BV-173 MmXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfTTWM2OD1yLke5OlQ1KM7:TR?= NG\ne|JUSU6JRWK=
RVH-421 M4XkTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfVXXZKSzVyPUCuPFY4QTZizszN M17iWHNCVkeHUh?=
HCC2218 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXQTWM2OD1yLki3PFQ1KM7:TR?= NWHMRW01W0GQR1XS
WM-115 NWfNN5NTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXEdo42UUN3ME2wMlg5Pjl{IN88US=> Ml7BV2FPT0WU
SK-MEL-28 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTFwMES1Olkh|ryP NEL0d4tUSU6JRWK=
COLO-679 MoXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFX0bJBKSzVyPUGuNVA1PjRizszN NV7ScHFuW0GQR1XS
MZ7-mel MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHVVGdnUUN3ME2xMlE1QTZ|IN88US=> MWHTRW5ITVJ?
SK-MEL-30 Ml;6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFwM{OzPFYh|ryP MlL5V2FPT0WU
NCI-H209 MlXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTFwNkC4OkDPxE1? M3jLcHNCVkeHUh?=
HTC-C3 NWS1bJlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjYTWM2OD1zLk[2Nlk1KM7:TR?= NWe0Z3BSW0GQR1XS
KARPAS-45 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVmyU3VZUUN3ME2yMlA1QTd6IN88US=> MkHIV2FPT0WU
NCI-SNU-5 NIrIe4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGeyOldKSzVyPUKuNVE6PjlizszN NIjxfJdUSU6JRWK=
KP-4 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrVTWM2OD1{LkOwO|g4KM7:TR?= NWL4dlB[W0GQR1XS
PA-1 NYnUU|hvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TES2lEPTB;Mj63NlY4OyEQvF2= NUHIV3d3W0GQR1XS
HuO-3N1 NYHOToxoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGC1cmNKSzVyPUKuPFc6PDZizszN M2\WbnNCVkeHUh?=
NCI-H358 Ml;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\KeYFpUUN3ME2yMlkzOjN{IN88US=> NVzqSm9iW0GQR1XS
CTB-1 NIDZepZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXruT2s3UUN3ME2zMlQxOTd4IN88US=> M3TtWHNCVkeHUh?=
697 Mle0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTNwNUWyOlYh|ryP MYfTRW5ITVJ?
CP66-MEL NWHzO5d4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTRwMUW5Nlch|ryP Mmj4V2FPT0WU
NB13 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrpRW1KSzVyPUSuOFkyPzlizszN MmryV2FPT0WU
DBTRG-05MG NGe1NnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLETWM2OD12LkWzN|I2KM7:TR?= NUfnfppSW0GQR1XS
A2058 MoXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPHTWM2OD12LkeyNVY1KM7:TR?= MmPYV2FPT0WU
KG-1 NXHiV3ZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rWNGlEPTB;ND63N|kxQCEQvF2= MlrwV2FPT0WU
8305C MmmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3ZeXlKSzVyPUWuNVg4OyEQvF2= M1\tV3NCVkeHUh?=
RPMI-7951 NEnORZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPHfVdKSzVyPUWuPFAzQDNizszN MmXXV2FPT0WU
CHL-1 NFTJbYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4m4VGlEPTB;NT65O|YxOyEQvF2= NYq2e|loW0GQR1XS
TI-73 NFu1cnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPzSYdKSzVyPU[uNFA6ODJizszN M4PMd3NCVkeHUh?=
HT-1080 NFnvcGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTZwMUC5OFYh|ryP NI\1OVhUSU6JRWK=
ES5 NV;MfWJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTZeXp[UUN3ME22MlE1QTJ2IN88US=> MWXTRW5ITVJ?
8-MG-BA NGTwdFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3frWmlEPTB;Nj6xPFEzQSEQvF2= Mly2V2FPT0WU
NB7 M3zMPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTZwMkGzO|Mh|ryP M4LzRXNCVkeHUh?=
H4 NH\Ec4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1K3bWlEPTB;Nj6yNlQ6OyEQvF2= MWfTRW5ITVJ?
CAL-72 MnuzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTZwNEW0NlMh|ryP NIq1RVBUSU6JRWK=
HCC1806 Ml[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTZwOEG5N|Eh|ryP NFrvcXpUSU6JRWK=
BCPAP M3\sWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTdwMkG3OlQh|ryP NWPHOFRQW0GQR1XS
LB2241-RCC MoDoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfnTWM2OD15LkO2PVA4KM7:TR?= MWPTRW5ITVJ?
COLO-741 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRThwMEG2O|kh|ryP MoG3V2FPT0WU
HSC-3 Mnr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HlRWlEPTB;OD6wO|A3QCEQvF2= NYT4VZV1W0GQR1XS
SW982 NWfscJRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUToUFhvUUN3ME24MlQyPTF4IN88US=> M1HGO3NCVkeHUh?=
GCT MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETEfVVKSzVyPUiuO|U{OTRizszN NFj1[XJUSU6JRWK=
KY821 NVKxVZdET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTlwMEWxO|gh|ryP MlS1V2FPT0WU
JVM-3 NH:5UYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mof2TWM2OD17LkW2PVk6KM7:TR?= NGHlSY1USU6JRWK=
RS4-11 NH:1RotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXPdXRKSzVyPUmuOlA1QCEQvF2= MV7TRW5ITVJ?
VA-ES-BJ NWTwXXdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2j3S2lEPTB;MUCuNFE1QSEQvF2= M1fSNnNCVkeHUh?=
A431 NVnVVlRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3S4SGlEPTB;MUCuOFIyOiEQvF2= Mk\0V2FPT0WU
LXF-289 M1\KNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTFyLkS1PEDPxE1? MUnTRW5ITVJ?
SK-MEL-24 Mm\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2f6RWlEPTB;MUCuPFI4PCEQvF2= M1\LWXNCVkeHUh?=
NOS-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\iXIdKSzVyPUGwMlg1PzJizszN NHPZWXBUSU6JRWK=
KNS-62 M2XCXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXQN2NKSzVyPUGxMlI1ODRizszN NHnzRZhUSU6JRWK=
SK-HEP-1 NUDQV5gzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmCwTWM2OD1zMT6zOVI4KM7:TR?= NHjMb4hUSU6JRWK=
A3-KAW M2TI[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPVS417UUN3ME2xNU44OTd6IN88US=> MofOV2FPT0WU
SK-LU-1 M4D6eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XVTGlEPTB;MUKuNlY2PSEQvF2= NVXwR|h2W0GQR1XS
TYK-nu NEC0VlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTF{LkO5N|Ih|ryP NX20[GduW0GQR1XS
NMC-G1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvNemlKSzVyPUGyMlYxPjJizszN NEHve2xUSU6JRWK=
BB65-RCC NVn5fIdKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIO5fVJKSzVyPUGyMlcyPjlizszN NVnhPHRCW0GQR1XS
QIMR-WIL MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7ifWNTUUN3ME2xNk45QDN|IN88US=> M4TsZXNCVkeHUh?=
D-566MG M13PN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXDSYJJUUN3ME2xN{46PTd4IN88US=> MVPTRW5ITVJ?
KYSE-140 M3znemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEKyXIFKSzVyPUG0MlA4PTNizszN NWDT[YRwW0GQR1XS
SCC-4 NX;2TFJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NED4WHBKSzVyPUG0MlM{PTlizszN M4H2WXNCVkeHUh?=
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NCI-H526 NGnHe45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHnVpVQUUN3ME2yOU4xODJ|IN88US=> NG\UTXBUSU6JRWK=
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NCI-H82 M{DkNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrvTWM2OD1{NT65N|gh|ryP MVnTRW5ITVJ?
SNU-449 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\BZYFKSzVyPUK3MlIxOThizszN NW[4dJl5W0GQR1XS
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NCI-SNU-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHYUpNZUUN3ME2yO{46PDRizszN MoXwV2FPT0WU
ALL-PO NU[yT5k5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\nT2lEPTB;MkiuNVYxPCEQvF2= MlHwV2FPT0WU
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HOP-62 NV7QVmx[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjZdWMxUUN3ME2yPE44OTNizszN NFTEOpVUSU6JRWK=
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NCI-H1304 NVH3bVZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYr6OXl7UUN3ME2zNk4{OzBzIN88US=> MmTSV2FPT0WU
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U031 NGP1eZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTN3LkixN|Ih|ryP NWLZZ4F6W0GQR1XS
HMV-II NVHsXnQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojJTWM2OD1|Nj6wO|c1KM7:TR?= NUHIN4NFW0GQR1XS
L-363 M{njOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXZVFNJUUN3ME2zO{43PDV3IN88US=> MUDTRW5ITVJ?
NCI-H1155 M1iyO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\ORXhKSzVyPUO4MlAxOTVizszN NEPQbXhUSU6JRWK=
NCI-H1793 NV7LV3Z[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rCZ2lEPTB;M{iuNVAzPiEQvF2= M4nOU3NCVkeHUh?=
P30-OHK NEfybWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTN6LkGzN|Ih|ryP NVHaR49oW0GQR1XS
AN3-CA NH\PW4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELyeohKSzVyPUO4MlE3OTVizszN MVfTRW5ITVJ?
UACC-257 M2XTbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTH[XRlUUN3ME2zPE44QSEQvF2= MmnzV2FPT0WU
MCF7 MlTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHx[YFKSzVyPUO5Mlg3OjlizszN MnnkV2FPT0WU
KP-N-YN M1nrXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvjSZBKSzVyPUSwMlQzQDVizszN M120T3NCVkeHUh?=
T98G MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{n0cGlEPTB;NECuOFk2PyEQvF2= NWO2WndOW0GQR1XS
HGC-27 NH3aWINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:wNII6UUN3ME20N{4zPzRizszN MnjIV2FPT0WU
NCI-H1092 NGi2SY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGKzOItKSzVyPUSzMlI5QTVizszN M1f5Z3NCVkeHUh?=
KARPAS-299 M{e4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HpVmlEPTB;NEOuN|A4OSEQvF2= NGLyZ4dUSU6JRWK=
LB1047-RCC NG\MW49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEe0TFJKSzVyPUS0Mlk6PTlizszN M2LXN3NCVkeHUh?=
786-0 NH;KN41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ix[GlEPTB;NEWuOlUh|ryP MULTRW5ITVJ?
HCC2157 M336eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTR4LkCzOVkh|ryP MlLPV2FPT0WU
NY NVvJbI1qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTR4LkG3O|gh|ryP MWLTRW5ITVJ?
EFM-19 NUHNXVU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTR4Lke1N|Mh|ryP M{jHTXNCVkeHUh?=
EW-16 M1;qTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DBPWlEPTB;NE[uO|gxPiEQvF2= M3The3NCVkeHUh?=
UM-UC-3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPYTWM2OD12Nj64NFU6KM7:TR?= NELWfolUSU6JRWK=
HT-29 MoTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTR5Lki3PVIh|ryP NX\hZ4NYW0GQR1XS
LN-405 M1fMZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XvbmlEPTB;NEiuNFgzPyEQvF2= M{XLZ3NCVkeHUh?=
NCI-H727 NUDuXXg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfFTWM2OD12OD63O|I3KM7:TR?= NVPrSmZDW0GQR1XS
D-502MG NHf4eIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUi1fpZ4UUN3ME20PE46Pjd4IN88US=> MWTTRW5ITVJ?
GMS-10 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljGTWM2OD12OT6yPVc1KM7:TR?= NXnIRmY{W0GQR1XS
MEL-JUSO M1Lyb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLsTWM2OD12OT6zOFch|ryP NYHlfpRtW0GQR1XS

... 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:
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
Synonyms N/A

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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

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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.

Raf Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID