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 NWjHXnB3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTBwMEe0OVch|ryP M3K1e3NCVkeHUh?=
EoL-1-cell NFSwc|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTBwMUSxOlYh|ryP NUXhVGxZW0GQR1XS
C32 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjzSJZKSzVyPUCuNVUyOzFizszN MXTTRW5ITVJ?
M14 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPLN3lKSzVyPUCuNlE4PTdizszN M1PFZXNCVkeHUh?=
CP50-MEL-B NYX6VZNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2q5PWlEPTB;MD6yPVc5PCEQvF2= M2LnO3NCVkeHUh?=
A101D M1XMfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[wTWM2OD1yLkOyOVg6KM7:TR?= MUfTRW5ITVJ?
G-361 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\YOHFKSzVyPUCuN|Q3OzdizszN NEf6OlhUSU6JRWK=
HT-144 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInYfolKSzVyPUCuN|Y{OjlizszN Mln5V2FPT0WU
ACN Mn3hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmi5TWM2OD1yLkO4OFc4KM7:TR?= MlvHV2FPT0WU
COLO-829 MmLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTBwM{i5Olgh|ryP NUPzT3NjW0GQR1XS
MEL-HO MlfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjKTWM2OD1yLkSxNVc6KM7:TR?= MWrTRW5ITVJ?
SH-4 Mmf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPxWopKSzVyPUCuOFE1OjJizszN MmjDV2FPT0WU
SK-MEL-3 M2TGXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLLbXgyUUN3ME2wMlUyPTZ6IN88US=> NYjXe2ROW0GQR1XS
A375 M{Hrfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTBwNkezOVkh|ryP NWDnb5pCW0GQR1XS
MMAC-SF NEXpSXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGL3eFdKSzVyPUCuOlg3OTRizszN MnTBV2FPT0WU
BHT-101 NFrLb21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXq[4JCUUN3ME2wMlcxPzB{IN88US=> Mln3V2FPT0WU
K5 NYXpPXU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHZRmxKSzVyPUCuO|YyPDhizszN MXTTRW5ITVJ?
BV-173 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rucmlEPTB;MD63PVY1PCEQvF2= NFHmVJdUSU6JRWK=
RVH-421 NIH6VXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;FV2lEPTB;MD64Olc6PiEQvF2= NULEOIRqW0GQR1XS
HCC2218 MnrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTBwOEe4OFQh|ryP M4DWNnNCVkeHUh?=
WM-115 NWXOUpZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTBwOEi2PVIh|ryP NEHuWZVUSU6JRWK=
SK-MEL-28 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfQTWM2OD1zLkC0OVY6KM7:TR?= NHfWXphUSU6JRWK=
COLO-679 NIHmPYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7JfYg2UUN3ME2xMlExPDZ2IN88US=> MkOwV2FPT0WU
MZ7-mel M1rlOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF[4[HhKSzVyPUGuNVQ6PjNizszN MYDTRW5ITVJ?
SK-MEL-30 NUT4fGZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHOTWM2OD1zLkOzN|g3KM7:TR?= NVr6ZWJYW0GQR1XS
NCI-H209 NHXiUFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvoV2ZKSzVyPUGuOlA5PiEQvF2= NXfSTGNkW0GQR1XS
HTC-C3 MmflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXHTWM2OD1zLk[2Nlk1KM7:TR?= NVTuXmY3W0GQR1XS
KARPAS-45 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTJwMES5O|gh|ryP M3vQbHNCVkeHUh?=
NCI-SNU-5 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;UfIFKSzVyPUKuNVE6PjlizszN MUTTRW5ITVJ?
KP-4 M1vGW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJwM{C3PFch|ryP Mn\CV2FPT0WU
PA-1 M3rVNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTJwN{K2O|Mh|ryP M{j1T3NCVkeHUh?=
HuO-3N1 M2LpXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\Kd3FKSzVyPUKuPFc6PDZizszN NXf5eYRuW0GQR1XS
NCI-H358 NInqXlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{mzdGlEPTB;Mj65NlI{OiEQvF2= Mmj4V2FPT0WU
CTB-1 MlH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7DRY4zUUN3ME2zMlQxOTd4IN88US=> M32wW3NCVkeHUh?=
697 MlG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjp[|A4UUN3ME2zMlU2OjZ4IN88US=> MWLTRW5ITVJ?
CP66-MEL M3KyVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXn4OG1PUUN3ME20MlE2QTJ5IN88US=> Ml7FV2FPT0WU
NB13 NIS3TFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVu1dWpLUUN3ME20MlQ6OTd7IN88US=> Mlu0V2FPT0WU
DBTRG-05MG MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTRwNUOzNlUh|ryP NIXLSG1USU6JRWK=
A2058 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTvZnFKSzVyPUSuO|IyPjRizszN MYPTRW5ITVJ?
KG-1 M1fuPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{niXWlEPTB;ND63N|kxQCEQvF2= NXizbHQyW0GQR1XS
8305C MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVK4XlBXUUN3ME21MlE5PzNizszN MV3TRW5ITVJ?
RPMI-7951 NFnIdldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTVwOECyPFMh|ryP NGXab4xUSU6JRWK=
CHL-1 MlTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWSzeGpxUUN3ME21Mlk4PjB|IN88US=> NEO0WWdUSU6JRWK=
TI-73 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fMZ2lEPTB;Nj6wNFkxOiEQvF2= NIC4elFUSU6JRWK=
HT-1080 M3jnfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDKUJVKSzVyPU[uNVA6PDZizszN MkH6V2FPT0WU
ES5 NFuyNVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTZwMUS5NlQh|ryP NH7QR21USU6JRWK=
8-MG-BA M1nqVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEG3NZhKSzVyPU[uNVgyOjlizszN MVHTRW5ITVJ?
NB7 MnW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX[w[I9bUUN3ME22MlIyOzd|IN88US=> NIrCVWxUSU6JRWK=
H4 M16xWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjqTHlKSzVyPU[uNlI1QTNizszN NH\2OmVUSU6JRWK=
CAL-72 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTMTWM2OD14LkS1OFI{KM7:TR?= NX[1NIdFW0GQR1XS
HCC1806 M4TZZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml6zTWM2OD14LkixPVMyKM7:TR?= NU\BTYw1W0GQR1XS
BCPAP Mnu5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\uO2lEPTB;Nz6yNVc3PCEQvF2= NUf1c5EzW0GQR1XS
LB2241-RCC NF;iSYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTdwM{[5NFch|ryP M36xdnNCVkeHUh?=
COLO-741 NUnPZmU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LCXGlEPTB;OD6wNVY4QSEQvF2= MUHTRW5ITVJ?
HSC-3 NFnhfpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\5d5VKSzVyPUiuNFcxPjhizszN M2\ZNXNCVkeHUh?=
SW982 NUPONY5NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{GwdGlEPTB;OD60NVUyPiEQvF2= M1zYVXNCVkeHUh?=
GCT Mm\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nzPWlEPTB;OD63OVMyPCEQvF2= MkjrV2FPT0WU
KY821 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITXNoNKSzVyPUmuNFUyPzhizszN Mk\kV2FPT0WU
JVM-3 M1uxbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3oOG5TUUN3ME25MlU3QTl7IN88US=> Mmn5V2FPT0WU
RS4-11 MoXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrVTWM2OD17Lk[wOFgh|ryP MmjMV2FPT0WU
VA-ES-BJ MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XUZWlEPTB;MUCuNFE1QSEQvF2= M{LIXHNCVkeHUh?=
A431 NFjweoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TZbmlEPTB;MUCuOFIyOiEQvF2= NVHme|JuW0GQR1XS
LXF-289 NGS2dGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrvVmVKSzVyPUGwMlQ2QCEQvF2= MoPKV2FPT0WU
SK-MEL-24 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nRSmlEPTB;MUCuPFI4PCEQvF2= M3S3SnNCVkeHUh?=
NOS-1 MmXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTFyLki0O|Ih|ryP NEnNT2ZUSU6JRWK=
KNS-62 NWm1NHNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXSTWM2OD1zMT6yOFA1KM7:TR?= NEnDNHlUSU6JRWK=
SK-HEP-1 M4nwXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTFzLkO1Nlch|ryP MUfTRW5ITVJ?
A3-KAW NVraNJlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTOSlNKSzVyPUGxMlcyPzhizszN NWXpOZNEW0GQR1XS
SK-LU-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTF{LkK2OVUh|ryP MoDJV2FPT0WU
TYK-nu M3n3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDITWM2OD1zMj6zPVMzKM7:TR?= NXKxV|BPW0GQR1XS
NMC-G1 Mk\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\hTWM2OD1zMj62NFYzKM7:TR?= NV7JbnBnW0GQR1XS
BB65-RCC NFX5N4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPYTWM2OD1zMj63NVY6KM7:TR?= NUXDbW4xW0GQR1XS
QIMR-WIL M2TGcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHYTWM2OD1zMj64PFM{KM7:TR?= MWHTRW5ITVJ?
D-566MG MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTF|Lkm1O|Yh|ryP MVLTRW5ITVJ?
KYSE-140 NYPO[|ViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljWTWM2OD1zND6wO|U{KM7:TR?= NUH3eZlpW0GQR1XS
SCC-4 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvITWM2OD1zND6zN|U6KM7:TR?= NY\wNlBSW0GQR1XS
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NCI-H526 NHvXepBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfTfI1UUUN3ME2yOU4xODJ|IN88US=> NEfjSYJUSU6JRWK=
IST-SL1 MkfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;OUXBKSzVyPUK1MlI4PTFizszN MkL2V2FPT0WU
HH NFKyfZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHmTWM2OD1{NT6zNVkzKM7:TR?= M2CxSXNCVkeHUh?=
NCI-H82 Mn74S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUL2XnM5UUN3ME2yOU46OzhizszN NVz0WHlrW0GQR1XS
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COR-L23 MonGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTGVYJMUUN3ME2yO{4zQDF|IN88US=> MnrWV2FPT0WU
LOXIMVI NUPIWm1TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\WUGlEPTB;MkeuN|Y5KM7:TR?= M4\PfnNCVkeHUh?=
GR-ST MmPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TuZ2lEPTB;MkeuOlcxPiEQvF2= M17Ee3NCVkeHUh?=
NCI-SNU-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVW5fJA3UUN3ME2yO{46PDRizszN MmjrV2FPT0WU
ALL-PO NFLoZnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTLTWM2OD1{OD6xOlA1KM7:TR?= MXrTRW5ITVJ?
ML-2 NYmz[4UyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnH4TWM2OD1{OD6yPFE1KM7:TR?= MmHvV2FPT0WU
HOP-62 NGLNS5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnlTWM2OD1{OD63NVMh|ryP MkX4V2FPT0WU
EGI-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nVSmlEPTB;MkiuPFg1PSEQvF2= MnL5V2FPT0WU
TCCSUP NYCx[VNZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;RTWM2OD1{OD65NlczKM7:TR?= NYHHeHZYW0GQR1XS
LB996-RCC NYHYXodtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfWdFF{UUN3ME2yPU42Pjh{IN88US=> MXjTRW5ITVJ?
LCLC-97TM1 NEflZ45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLGTWM2OD1|Mj6xPVY1KM7:TR?= NHi4fHBUSU6JRWK=
NCI-H1304 NEfFWZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTN{LkOzNFEh|ryP Mo[0V2FPT0WU
KP-N-YS NY\1VopiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGr2cldKSzVyPUOyMlU6PzNizszN MYHTRW5ITVJ?
NCI-H1770 NFG1cpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXGTWM2OD1|Mz6xOlQ5KM7:TR?= Mn7GV2FPT0WU
EM-2 NH7UbnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLFTWM2OD1|Mz62OVA1KM7:TR?= NYTMVlZzW0GQR1XS
ChaGo-K-1 NEXRXGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTN|LkeyN|Yh|ryP NF7kcldUSU6JRWK=
ACHN NFLD[YpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrOTWM2OD1|Mz64N|g2KM7:TR?= M2PJfnNCVkeHUh?=
MN-60 M4Owfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnCc5dKSzVyPUOzMlg2PDRizszN MlzDV2FPT0WU
EW-18 MknYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPQVZVKSzVyPUOzMlg6PzFizszN NV22dIdKW0GQR1XS
KGN NXjTR2dMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{i2d2lEPTB;M{WuO|I6OiEQvF2= MmDKV2FPT0WU
U031 NGDOS5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvEUFlPUUN3ME2zOU45OTN{IN88US=> NUHXbXVZW0GQR1XS
HMV-II M1;lVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzPTWM2OD1|Nj6wO|c1KM7:TR?= M{XGTHNCVkeHUh?=
L-363 M4jTOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjBUIZYUUN3ME2zO{43PDV3IN88US=> NWW0OYFNW0GQR1XS
NCI-H1155 NX:0[|U1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfWPYFKSzVyPUO4MlAxOTVizszN NUPITZVqW0GQR1XS
NCI-H1793 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYO3ZY1bUUN3ME2zPE4yODJ4IN88US=> M{PUTHNCVkeHUh?=
P30-OHK NX;rW5JQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XzSmlEPTB;M{iuNVM{OiEQvF2= M2LoeXNCVkeHUh?=
AN3-CA M1P6VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLNVmJKSzVyPUO4MlE3OTVizszN NYHRdlM5W0GQR1XS
UACC-257 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTMOYV{UUN3ME2zPE44QSEQvF2= MlO1V2FPT0WU
MCF7 M1jrUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2O1OmlEPTB;M{muPFYzQSEQvF2= NEHnWXhUSU6JRWK=
KP-N-YN NVqwXnh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrlNnZKSzVyPUSwMlQzQDVizszN MlW1V2FPT0WU
T98G M2jxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLCXHZsUUN3ME20NE41QTV5IN88US=> M1K4[3NCVkeHUh?=
HGC-27 NWrlRZBLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTR|LkK3OEDPxE1? MV\TRW5ITVJ?
NCI-H1092 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXrTWM2OD12Mz6yPFk2KM7:TR?= NWrMc2tuW0GQR1XS
KARPAS-299 M4T3fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rCS2lEPTB;NEOuN|A4OSEQvF2= MWPTRW5ITVJ?
LB1047-RCC M4CyWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXJTWM2OD12ND65PVU6KM7:TR?= NID2XmRUSU6JRWK=
786-0 MmC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTR3Lk[1JO69VQ>? NXPm[FQ3W0GQR1XS
HCC2157 NGLs[mlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rwSWlEPTB;NE[uNFM2QSEQvF2= Mk\5V2FPT0WU
NY MnLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWD4[JBGUUN3ME20Ok4yPzd6IN88US=> MVTTRW5ITVJ?
EFM-19 NX\QfXdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrkc2hWUUN3ME20Ok44PTN|IN88US=> NHnVb5NUSU6JRWK=
EW-16 MkXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1j6cGlEPTB;NE[uO|gxPiEQvF2= M2HxNnNCVkeHUh?=
UM-UC-3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnHXlVKSzVyPUS2MlgxPTlizszN M2HLZXNCVkeHUh?=
HT-29 NFnOWWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\NV2pKSzVyPUS3Mlg4QTJizszN NVLXOJBLW0GQR1XS
LN-405 NH65TFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1O1[mlEPTB;NEiuNFgzPyEQvF2= Mk\PV2FPT0WU
NCI-H727 M2LNOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVuwVpg1UUN3ME20PE44PzJ4IN88US=> NGrOS4NUSU6JRWK=
D-502MG NFjkcItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnlUZhwUUN3ME20PE46Pjd4IN88US=> M1W1OnNCVkeHUh?=
GMS-10 M4\2ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rU[GlEPTB;NEmuNlk4PCEQvF2= MnXiV2FPT0WU
MEL-JUSO M{fIS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfP[Y9KSzVyPUS5MlM1PyEQvF2= NFu1d|RUSU6JRWK=

... 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 individually and in order:
2% DMSO+50% PEG 300+5% Tween 80+ddH2O
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