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 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.

    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 NUnlcY8yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwMEe0OVch|ryP NIDQcoZUSU6JRWK=
EoL-1-cell NHTTOIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTBwMUSxOlYh|ryP MkW4V2FPT0WU
C32 M4OxSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPoTWM2OD1yLkG1NVMyKM7:TR?= MoPZV2FPT0WU
M14 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fOVWlEPTB;MD6yNVc2PyEQvF2= NVnxdmxzW0GQR1XS
CP50-MEL-B MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXj2fIZoUUN3ME2wMlI6Pzh2IN88US=> NGLIeIpUSU6JRWK=
A101D NWTnXW9ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3e5SWlEPTB;MD6zNlU5QSEQvF2= Mn;LV2FPT0WU
G-361 NWrkfnl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTBwM{S2N|ch|ryP NGjJUVNUSU6JRWK=
HT-144 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEW1[YlKSzVyPUCuN|Y{OjlizszN NHfrSJNUSU6JRWK=
ACN MkfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFqzd|JKSzVyPUCuN|g1PzdizszN Mo\jV2FPT0WU
COLO-829 NYTmO5VLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4C4VGlEPTB;MD6zPFk3QCEQvF2= M{HsWnNCVkeHUh?=
MEL-HO NYO4OWRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3uRohKSzVyPUCuOFEyPzlizszN MnrFV2FPT0WU
SH-4 NV;DSJJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3oTWM2OD1yLkSxOFIzKM7:TR?= MoGwV2FPT0WU
SK-MEL-3 M3ThOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwNUG1Olgh|ryP NG\jcZFUSU6JRWK=
A375 NIi0SVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDXTWM2OD1yLk[3N|U6KM7:TR?= M1[4eXNCVkeHUh?=
MMAC-SF MlTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTBwNki2NVQh|ryP M3;TZ3NCVkeHUh?=
BHT-101 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfGNppKSzVyPUCuO|A4ODJizszN M4T5PXNCVkeHUh?=
K5 Mof0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rITGlEPTB;MD63OlE1QCEQvF2= M1SxZ3NCVkeHUh?=
BV-173 M2HFeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPsb4VVUUN3ME2wMlc6PjR2IN88US=> M2nWO3NCVkeHUh?=
RVH-421 NUDhTZk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvMdZhMUUN3ME2wMlg3Pzl4IN88US=> MmexV2FPT0WU
HCC2218 MkXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVm2XIZnUUN3ME2wMlg4QDR2IN88US=> M3PtPXNCVkeHUh?=
WM-115 M4jpOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXlNpFSUUN3ME2wMlg5Pjl{IN88US=> NFvsdpRUSU6JRWK=
SK-MEL-28 NUG5UGQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fCPGlEPTB;MT6wOFU3QSEQvF2= NH3uRXRUSU6JRWK=
COLO-679 NISy[phIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTvTWM2OD1zLkGwOFY1KM7:TR?= NIHzbVdUSU6JRWK=
MZ7-mel M1Pmc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTFwMUS5OlMh|ryP M3X0TXNCVkeHUh?=
SK-MEL-30 NF;BZmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjmeFZKSzVyPUGuN|M{QDZizszN NHvPdmxUSU6JRWK=
NCI-H209 NFLDTFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\3N2lEPTB;MT62NFg3KM7:TR?= NET6W|dUSU6JRWK=
HTC-C3 NUO0OIFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHHXo1KSzVyPUGuOlYzQTRizszN MVrTRW5ITVJ?
KARPAS-45 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTJwMES5O|gh|ryP M2rEbHNCVkeHUh?=
NCI-SNU-5 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fRcWlEPTB;Mj6xNVk3QSEQvF2= Mme5V2FPT0WU
KP-4 NIrNRmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fRR2lEPTB;Mj6zNFc5PyEQvF2= MkPKV2FPT0WU
PA-1 NWS3dHlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{[zTmlEPTB;Mj63NlY4OyEQvF2= M2C3enNCVkeHUh?=
HuO-3N1 M4LpOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTtRpdXUUN3ME2yMlg4QTR4IN88US=> MVjTRW5ITVJ?
NCI-H358 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjhTWM2OD1{LkmyNlMzKM7:TR?= NWjLcFBkW0GQR1XS
CTB-1 M4rucmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TGS2lEPTB;Mz60NFE4PiEQvF2= MX7TRW5ITVJ?
697 MkT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rjfmlEPTB;Mz61OVI3PiEQvF2= Mm\iV2FPT0WU
CP66-MEL NVL1XG9pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2CweWlEPTB;ND6xOVkzPyEQvF2= M33y[nNCVkeHUh?=
NB13 M3uwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVu3d|V3UUN3ME20MlQ6OTd7IN88US=> NGrqWYRUSU6JRWK=
DBTRG-05MG NFL3eVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Gx[WlEPTB;ND61N|MzPSEQvF2= Mk\NV2FPT0WU
A2058 NXW4NYxPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nq[2lEPTB;ND63NlE3PCEQvF2= MUPTRW5ITVJ?
KG-1 NYPIdJc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTRwN{O5NFgh|ryP MkTVV2FPT0WU
8305C M3TjVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\hTWM2OD13LkG4O|Mh|ryP NXzIW2VMW0GQR1XS
RPMI-7951 NEK4bVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrrXIJtUUN3ME21MlgxOjh|IN88US=> NUX1XmhZW0GQR1XS
CHL-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFP2e5NKSzVyPUWuPVc3ODNizszN Mn:3V2FPT0WU
TI-73 NE[2W2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFH3NJZKSzVyPU[uNFA6ODJizszN M3HvdXNCVkeHUh?=
HT-1080 NFH6VI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjGTWM2OD14LkGwPVQ3KM7:TR?= NV\zTJd6W0GQR1XS
ES5 NFq2bFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTZwMUS5NlQh|ryP NHTnV5BUSU6JRWK=
8-MG-BA MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTZwMUixNlkh|ryP M4C0T3NCVkeHUh?=
NB7 NHPwNJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrGeYNKSzVyPU[uNlE{PzNizszN MknSV2FPT0WU
H4 MorTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDzcFlQUUN3ME22MlIzPDl|IN88US=> MmrLV2FPT0WU
CAL-72 NYOyWFdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorHTWM2OD14LkS1OFI{KM7:TR?= M2DSZXNCVkeHUh?=
HCC1806 M3LnNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTZwOEG5N|Eh|ryP MnT0V2FPT0WU
BCPAP MkjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\XdmlEPTB;Nz6yNVc3PCEQvF2= MYXTRW5ITVJ?
LB2241-RCC NEnUcHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTdwM{[5NFch|ryP NGXlRVVUSU6JRWK=
COLO-741 M1\SO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrC[W5KSzVyPUiuNFE3PzlizszN MWXTRW5ITVJ?
HSC-3 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnMTWM2OD16LkC3NFY5KM7:TR?= MU\TRW5ITVJ?
SW982 MmLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvOOIh7UUN3ME24MlQyPTF4IN88US=> NGexRmhUSU6JRWK=
GCT MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRThwN{WzNVQh|ryP NHi5PYtUSU6JRWK=
KY821 MknTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTlwMEWxO|gh|ryP MYrTRW5ITVJ?
JVM-3 NH7hTVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEP1N45KSzVyPUmuOVY6QTlizszN MY\TRW5ITVJ?
RS4-11 MkTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTlwNkC0PEDPxE1? MofMV2FPT0WU
VA-ES-BJ M{nYXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTFyLkCxOFkh|ryP NULub|ZNW0GQR1XS
A431 NVPrSmNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7kTWM2OD1zMD60NlEzKM7:TR?= NYXoOo5IW0GQR1XS
LXF-289 MnrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\zO3dKSzVyPUGwMlQ2QCEQvF2= NHn0UW1USU6JRWK=
SK-MEL-24 NIjvWHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTFyLkiyO|Qh|ryP M3fncHNCVkeHUh?=
NOS-1 NXjkdJYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DyOWlEPTB;MUCuPFQ4OiEQvF2= M{PyVHNCVkeHUh?=
KNS-62 MnTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkS3TWM2OD1zMT6yOFA1KM7:TR?= NXXSW4JCW0GQR1XS
SK-HEP-1 Ml:2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\TTWM2OD1zMT6zOVI4KM7:TR?= MVzTRW5ITVJ?
A3-KAW M3L4b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HoU2lEPTB;MUGuO|E4QCEQvF2= MmjHV2FPT0WU
SK-LU-1 NHm1fnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGflZ2RKSzVyPUGyMlI3PTVizszN MVzTRW5ITVJ?
TYK-nu MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljlTWM2OD1zMj6zPVMzKM7:TR?= NXnKPHhCW0GQR1XS
NMC-G1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTF{Lk[wOlIh|ryP MoPDV2FPT0WU
BB65-RCC NGm0SGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPhXWRKSzVyPUGyMlcyPjlizszN MoPtV2FPT0WU
QIMR-WIL NUX6R4VRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fjXWlEPTB;MUKuPFg{OyEQvF2= Mn;QV2FPT0WU
D-566MG MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYH4XWpWUUN3ME2xN{46PTd4IN88US=> M3;m[nNCVkeHUh?=
KYSE-140 NVzKO5NmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXFTWM2OD1zND6wO|U{KM7:TR?= Mo\1V2FPT0WU
SCC-4 MnTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXv2fXB2UUN3ME2xOE4{OzV7IN88US=> NH\UbGVUSU6JRWK=
U251 NXGxOVRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlf6TWM2OD1zND64OFkzKM7:TR?= NH3WOHNUSU6JRWK=
D-542MG NYjMWWxrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnpbXoxUUN3ME2xOE46OjJ{IN88US=> M3XxRnNCVkeHUh?=
LAMA-84 M2W3dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rLOGlEPTB;MUSuPVk{OiEQvF2= NVfocHBXW0GQR1XS
NCI-H720 NGLl[2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXriTocxUUN3ME2xOU4zPjh2IN88US=> NIqxT4RUSU6JRWK=
DEL MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTuemFrUUN3ME2xOU41Ojl|IN88US=> NXvRSXhqW0GQR1XS
SBC-1 Ml7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fycmlEPTB;MUWuOFMxPSEQvF2= MXPTRW5ITVJ?
ECC10 NV7FSoJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXntSVl4UUN3ME2xOU41PDV6IN88US=> MV\TRW5ITVJ?
Daoy Mk\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfFfndKSzVyPUG1Mlc3OTZizszN NUfjbZVHW0GQR1XS
SCH MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTF3Lke4N|Uh|ryP NEPjTpdUSU6JRWK=
MZ2-MEL NV;1XoxMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTF4LkC2OFYh|ryP MWjTRW5ITVJ?
CAL-12T NWna[Zg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTaTWM2OD1zNj60PFYzKM7:TR?= Ml\kV2FPT0WU
KE-37 NXLETGc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTF4LkixNFch|ryP NVHBVo1CW0GQR1XS
LS-411N M1HadGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3i5VWlEPTB;MUeuNVE5KM7:TR?= NFvFWo9USU6JRWK=
NCI-H2228 NG\Xc|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTF5LkOwO|Eh|ryP MUXTRW5ITVJ?
SK-MEL-2 NUDzSFBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\yfmZKSzVyPUG3MlQ6PjVizszN NF;ze4lUSU6JRWK=
HN MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPITWM2OD1zNz63NlQ5KM7:TR?= M4q1TnNCVkeHUh?=
NCI-H1648 MnTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlH3TWM2OD1zNz64NVgh|ryP MnnNV2FPT0WU
IA-LM MnS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTF6LkOxO|Ih|ryP MmPxV2FPT0WU
EW-13 Ml7KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTF6LkW3NFgh|ryP MU\TRW5ITVJ?
YKG-1 M4fGOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoX3TWM2OD1zOT61O|EyKM7:TR?= MV7TRW5ITVJ?
KNS-81-FD MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjXfZBKSzVyPUG5MlU5PThizszN MUjTRW5ITVJ?
23132-87 M3LscGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;vWJJKSzVyPUG5Mlc3PDJizszN NYnQcmVRW0GQR1XS
NUGC-3 M3u4[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHMNIxKUUN3ME2xPU46QDh5IN88US=> MVPTRW5ITVJ?
5637 NIjVcnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvzTWM2OD1{MD6wOFc5KM7:TR?= NH\ueoFUSU6JRWK=
NCI-H1755 Mk\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHvU5JqUUN3ME2yNE41PzZ2IN88US=> MY\TRW5ITVJ?
RH-18 M1:4dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XqeGlEPTB;MkCuOVc1QCEQvF2= M1q2SnNCVkeHUh?=
RXF393 M4DnTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fhSGlEPTB;MkCuOlc2PiEQvF2= MYrTRW5ITVJ?
LU-134-A M4\lS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXyflVIUUN3ME2yNE44ODV4IN88US=> M1zqSnNCVkeHUh?=
TE-12 M1P4S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTJyLkeyNFEh|ryP MX\TRW5ITVJ?
MOLT-4 Mn;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\tdoJNUUN3ME2yNU4yQTF3IN88US=> M37xTnNCVkeHUh?=
IGR-1 M3jjU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTJzLkO3PVYh|ryP M{XjPHNCVkeHUh?=
HOP-92 M13JO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTJzLkS5PFch|ryP MkTDV2FPT0WU
SK-MES-1 NYCzSINGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXO4V4Q1UUN3ME2yNU44OzhzIN88US=> NE\sbWxUSU6JRWK=
LU-65 M4K5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TwN2lEPTB;MkGuPFYzPCEQvF2= MUHTRW5ITVJ?
MS-1 NWLrU4htT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTJ{LkGyNFMh|ryP MYfTRW5ITVJ?
LoVo M4G1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTJ{LkK0OEDPxE1? M1fEOXNCVkeHUh?=
A704 NUjnWZpFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4e4S2lEPTB;MkKuOVE2PSEQvF2= MXTTRW5ITVJ?
HT-1376 M3fKfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rocmlEPTB;MkKuOlA2QSEQvF2= NInkXVhUSU6JRWK=
IST-MEL1 NV\pb|RiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jmdWlEPTB;MkKuOlc2OSEQvF2= MlPoV2FPT0WU
Ramos-2G6-4C10 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\XU49KSzVyPUKyMlc{PjZizszN NFexbHNUSU6JRWK=
T47D NYTnO25iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTJ{Lke5O|kh|ryP NVTMTJQ3W0GQR1XS
HT-1197 M4OwXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUn3[oJ[UUN3ME2yN{4xQDF5IN88US=> M3[xOnNCVkeHUh?=
LB2518-MEL NXfQOnhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLzTWM2OD1{Mz62OFEzKM7:TR?= NXfYfGdrW0GQR1XS
J-RT3-T3-5 NH3uNXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnuTWM2OD1{ND63OVk2KM7:TR?= M{nWUXNCVkeHUh?=
SK-NEP-1 MmnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEL1SJZKSzVyPUK0Mlg4PDRizszN NFXxeFNUSU6JRWK=
NCI-H526 NGXadmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTJ3LkCwNlMh|ryP M{P4OnNCVkeHUh?=
IST-SL1 M2nK[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHneGZKSzVyPUK1MlI4PTFizszN MVHTRW5ITVJ?
HH M2WxPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Pyd2lEPTB;MkWuN|E6OiEQvF2= MXPTRW5ITVJ?
NCI-H82 MkDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\zTWM2OD1{NT65N|gh|ryP NYLVV3htW0GQR1XS
SNU-449 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDMTWM2OD1{Nz6yNFE5KM7:TR?= M{DWXnNCVkeHUh?=
COR-L23 M{nzV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPSdHZKSzVyPUK3MlI5OTNizszN NF:5eG5USU6JRWK=
LOXIMVI NGGyWWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljCTWM2OD1{Nz6zOlgh|ryP NWXaSVVuW0GQR1XS
GR-ST M{DEOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\jTWM2OD1{Nz62O|A3KM7:TR?= MUfTRW5ITVJ?
NCI-SNU-1 NUS4VXFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTJ5Lkm0OEDPxE1? NWq1[JBSW0GQR1XS
ALL-PO NX;Obnh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rlbGlEPTB;MkiuNVYxPCEQvF2= MlSyV2FPT0WU
ML-2 NFf4PZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTJ6LkK4NVQh|ryP NVXoWHp7W0GQR1XS
HOP-62 NE[wTY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWW2PFQ2UUN3ME2yPE44OTNizszN MX\TRW5ITVJ?
EGI-1 NEXRXIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvvTWM2OD1{OD64PFQ2KM7:TR?= NF[1WmdUSU6JRWK=
TCCSUP NYCyO4RtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFX2TWlKSzVyPUK4MlkzPzJizszN M13Ye3NCVkeHUh?=
LB996-RCC NYfwWIRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vwZ2lEPTB;MkmuOVY5OiEQvF2= MmPpV2FPT0WU
LCLC-97TM1 MlSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTN{LkG5OlQh|ryP M1jJXHNCVkeHUh?=
NCI-H1304 NX7NSollT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;lT2NpUUN3ME2zNk4{OzBzIN88US=> MmjoV2FPT0WU
KP-N-YS NYqwSIo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfKTWM2OD1|Mj61PVc{KM7:TR?= MYXTRW5ITVJ?
NCI-H1770 NEPzTHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml:1TWM2OD1|Mz6xOlQ5KM7:TR?= M2n4NXNCVkeHUh?=
EM-2 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTN|Lk[1NFQh|ryP NH[weIlUSU6JRWK=
ChaGo-K-1 M3PKfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPOTWM2OD1|Mz63NlM3KM7:TR?= MXPTRW5ITVJ?
ACHN Mnm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzhTWM2OD1|Mz64N|g2KM7:TR?= M2TTSHNCVkeHUh?=
MN-60 M3TL[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYH6eJM6UUN3ME2zN{45PTR2IN88US=> MmPhV2FPT0WU
EW-18 MkO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHIeXZZUUN3ME2zN{45QTdzIN88US=> NHzBcGVUSU6JRWK=
KGN NY\abYl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTN3LkeyPVIh|ryP MoX3V2FPT0WU
U031 NFfBWmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\2TGlEPTB;M{WuPFE{OiEQvF2= MV;TRW5ITVJ?
HMV-II Mm\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzmN3RCUUN3ME2zOk4xPzd2IN88US=> MnTWV2FPT0WU
L-363 NGO2bJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\6PZhKSzVyPUO3MlY1PTVizszN Mk\UV2FPT0WU
NCI-H1155 M3fFPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fHPGlEPTB;M{iuNFAyPSEQvF2= NULq[ldFW0GQR1XS
NCI-H1793 NGKwNG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTHTWM2OD1|OD6xNFI3KM7:TR?= NVzlOVJDW0GQR1XS
P30-OHK NFrsOYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTN6LkGzN|Ih|ryP Ml;lV2FPT0WU
AN3-CA M1zGcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17EXGlEPTB;M{iuNVYyPSEQvF2= MnO2V2FPT0WU
UACC-257 NIHnXVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PaV2lEPTB;M{iuO|kh|ryP M4jFbnNCVkeHUh?=
MCF7 MnzwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnITWM2OD1|OT64OlI6KM7:TR?= NEfEfoxUSU6JRWK=
KP-N-YN Mor2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnGbohXUUN3ME20NE41Ojh3IN88US=> NX[1[ppkW0GQR1XS
T98G NV\xNWpDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7ITWM2OD12MD60PVU4KM7:TR?= MkLVV2FPT0WU
HGC-27 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfE[YNmUUN3ME20N{4zPzRizszN MXvTRW5ITVJ?
NCI-H1092 M{fVUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTR|LkK4PVUh|ryP NIi3SZdUSU6JRWK=
KARPAS-299 NX25ZWhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTR|LkOwO|Eh|ryP MXHTRW5ITVJ?
LB1047-RCC MnrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTR2Lkm5OVkh|ryP Mlm2V2FPT0WU
786-0 MnHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDIWI1KSzVyPUS1MlY2KM7:TR?= NYn0PIVnW0GQR1XS
HCC2157 NVfi[3ZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHtTWM2OD12Nj6wN|U6KM7:TR?= MX3TRW5ITVJ?
NY NVXiPY53T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPtSnNKSzVyPUS2MlE4PzhizszN M3Xi[3NCVkeHUh?=
EFM-19 NYD0fIVZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Hpc2lEPTB;NE[uO|U{OyEQvF2= MorNV2FPT0WU
EW-16 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkntTWM2OD12Nj63PFA3KM7:TR?= MVHTRW5ITVJ?
UM-UC-3 MkLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTR4LkiwOVkh|ryP NUjTW5JVW0GQR1XS
HT-29 NFTLcFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTR5Lki3PVIh|ryP MkHKV2FPT0WU
LN-405 NEXwTIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fwPWlEPTB;NEiuNFgzPyEQvF2= MUHTRW5ITVJ?
NCI-H727 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;GTWM2OD12OD63O|I3KM7:TR?= M2H2dHNCVkeHUh?=
D-502MG MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;2TWM2OD12OD65Olc3KM7:TR?= NH3zOo1USU6JRWK=
GMS-10 M4q3XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTR7LkK5O|Qh|ryP M{L2ZnNCVkeHUh?=
MEL-JUSO MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jGZWlEPTB;NEmuN|Q4KM7:TR?= NH75XHZUSU6JRWK=

... 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

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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

Raf Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID