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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USD 270 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 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TMPGlEPTB;MD6wO|Q2PyEQvF2= MWLTRW5ITVJ?
EoL-1-cell MmjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17n[2lEPTB;MD6xOFE3PiEQvF2= NH6wdY1USU6JRWK=
C32 NWHafnFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnK3TWM2OD1yLkG1NVMyKM7:TR?= NGDqT2hUSU6JRWK=
M14 NYfnV5lPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTJ[5dKSzVyPUCuNlE4PTdizszN M{Dqb3NCVkeHUh?=
CP50-MEL-B NEO0XlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHVTWM2OD1yLkK5O|g1KM7:TR?= MlvkV2FPT0WU
A101D MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV6wZlloUUN3ME2wMlMzPTh7IN88US=> MlfOV2FPT0WU
G-361 NInLXHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfkTWM2OD1yLkO0OlM4KM7:TR?= NUjzN|NOW0GQR1XS
HT-144 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTBwM{[zNlkh|ryP NU\rT|FKW0GQR1XS
ACN NEe4eJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\uTWM2OD1yLkO4OFc4KM7:TR?= NXfFOohkW0GQR1XS
COLO-829 NFi4S5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HNZWlEPTB;MD6zPFk3QCEQvF2= NGHXNWJUSU6JRWK=
MEL-HO NIHwUnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfSVGhKSzVyPUCuOFEyPzlizszN MnjxV2FPT0WU
SH-4 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHneohKSzVyPUCuOFE1OjJizszN NV\qZoQ4W0GQR1XS
SK-MEL-3 NYHle|JpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELtRWlKSzVyPUCuOVE2PjhizszN MYnTRW5ITVJ?
A375 M2TEWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\rTWM2OD1yLk[3N|U6KM7:TR?= NYrQSWlPW0GQR1XS
MMAC-SF Mn3TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmCzTWM2OD1yLk[4OlE1KM7:TR?= MnTJV2FPT0WU
BHT-101 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITyTHRKSzVyPUCuO|A4ODJizszN MofpV2FPT0WU
K5 NWHX[3lxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfaPFdKSzVyPUCuO|YyPDhizszN M2fOXHNCVkeHUh?=
BV-173 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml35TWM2OD1yLke5OlQ1KM7:TR?= MVnTRW5ITVJ?
RVH-421 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTBwOE[3PVYh|ryP NFG5fItUSU6JRWK=
HCC2218 MmPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLLTWM2OD1yLki3PFQ1KM7:TR?= MYLTRW5ITVJ?
WM-115 M2L5fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTBwOEi2PVIh|ryP NWDJZpY2W0GQR1XS
SK-MEL-28 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmP3TWM2OD1zLkC0OVY6KM7:TR?= NGT6VpZUSU6JRWK=
COLO-679 MmLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPFTWM2OD1zLkGwOFY1KM7:TR?= M3\oeXNCVkeHUh?=
MZ7-mel NE\abWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTjdppFUUN3ME2xMlE1QTZ|IN88US=> MnjYV2FPT0WU
SK-MEL-30 MkDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTmTWM2OD1zLkOzN|g3KM7:TR?= M{LtO3NCVkeHUh?=
NCI-H209 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrOTWM2OD1zLk[wPFYh|ryP M4CyTXNCVkeHUh?=
HTC-C3 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vDfWlEPTB;MT62OlI6PCEQvF2= Ml;6V2FPT0WU
KARPAS-45 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nYZ2lEPTB;Mj6wOFk4QCEQvF2= MXjTRW5ITVJ?
NCI-SNU-5 MmDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3P1SWlEPTB;Mj6xNVk3QSEQvF2= MnW4V2FPT0WU
KP-4 MoLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn71TWM2OD1{LkOwO|g4KM7:TR?= NYrLcHpzW0GQR1XS
PA-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTJwN{K2O|Mh|ryP Moj5V2FPT0WU
HuO-3N1 NI[2VmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D1PWlEPTB;Mj64O|k1PiEQvF2= NWPUbnpxW0GQR1XS
NCI-H358 NXHWfYVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;vTWM2OD1{LkmyNlMzKM7:TR?= NFPqUYlUSU6JRWK=
CTB-1 NUm4e|VNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTNwNECxO|Yh|ryP MULTRW5ITVJ?
697 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTNwNUWyOlYh|ryP NVy5NYN7W0GQR1XS
CP66-MEL NWHScY1uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\WcZVsUUN3ME20MlE2QTJ5IN88US=> M2POTnNCVkeHUh?=
NB13 MlzHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljsTWM2OD12LkS5NVc6KM7:TR?= MVnTRW5ITVJ?
DBTRG-05MG NXTlXWNiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHy4To1KSzVyPUSuOVM{OjVizszN M4\mXnNCVkeHUh?=
A2058 M1XZeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrkXHVEUUN3ME20MlczOTZ2IN88US=> MlPmV2FPT0WU
KG-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnlSXRLUUN3ME20Mlc{QTB6IN88US=> MoPQV2FPT0WU
8305C NH22UJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPjTWM2OD13LkG4O|Mh|ryP Mn7uV2FPT0WU
RPMI-7951 MkSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTVwOECyPFMh|ryP NWTj[3BpW0GQR1XS
CHL-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTVwOUe2NFMh|ryP MlvqV2FPT0WU
TI-73 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLM[5dKSzVyPU[uNFA6ODJizszN M4Du[nNCVkeHUh?=
HT-1080 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTZwMUC5OFYh|ryP NH[yTmtUSU6JRWK=
ES5 NHTHeIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTZwMUS5NlQh|ryP MlPJV2FPT0WU
8-MG-BA NIX4cGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTZwMUixNlkh|ryP MX\TRW5ITVJ?
NB7 M37EXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF[2XGxKSzVyPU[uNlE{PzNizszN MoCzV2FPT0WU
H4 M4HWTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzXT2dKSzVyPU[uNlI1QTNizszN NV\OSlFNW0GQR1XS
CAL-72 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvCRVF7UUN3ME22MlQ2PDJ|IN88US=> MXzTRW5ITVJ?
HCC1806 MmT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHjS2pKSzVyPU[uPFE6OzFizszN MVXTRW5ITVJ?
BCPAP MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTdwMkG3OlQh|ryP NGrmPVdUSU6JRWK=
LB2241-RCC NYPJOHF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvLbXBuUUN3ME23MlM3QTB5IN88US=> MnXrV2FPT0WU
COLO-741 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRThwMEG2O|kh|ryP NIDabHdUSU6JRWK=
HSC-3 NEjI[WZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmW1TWM2OD16LkC3NFY5KM7:TR?= NHywdWxUSU6JRWK=
SW982 M1\hN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRThwNEG1NVYh|ryP NUfBcodyW0GQR1XS
GCT MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlviTWM2OD16Lke1N|E1KM7:TR?= NYTJO45SW0GQR1XS
KY821 MkLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXwTWM2OD17LkC1NVc5KM7:TR?= NXGyWm44W0GQR1XS
JVM-3 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTlwNU[5PVkh|ryP MYPTRW5ITVJ?
RS4-11 MlPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3[0R2lEPTB;OT62NFQ5KM7:TR?= Mkj5V2FPT0WU
VA-ES-BJ MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzxTWM2OD1zMD6wNVQ6KM7:TR?= NXrubWdCW0GQR1XS
A431 MojSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkn3TWM2OD1zMD60NlEzKM7:TR?= Mn7aV2FPT0WU
LXF-289 NVT6elZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTFyLkS1PEDPxE1? MUDTRW5ITVJ?
SK-MEL-24 M3fzeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXiTIdJUUN3ME2xNE45Ojd2IN88US=> MUTTRW5ITVJ?
NOS-1 NUPRTI9VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fPWGlEPTB;MUCuPFQ4OiEQvF2= MU\TRW5ITVJ?
KNS-62 NXzBZoxDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYW3cXZzUUN3ME2xNU4zPDB2IN88US=> MomzV2FPT0WU
SK-HEP-1 NGnMWppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jDR2lEPTB;MUGuN|UzPyEQvF2= NUPJb|VOW0GQR1XS
A3-KAW MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33XTmlEPTB;MUGuO|E4QCEQvF2= M{LWOXNCVkeHUh?=
SK-LU-1 NUezWFNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;rTWM2OD1zMj6yOlU2KM7:TR?= NV;ocop2W0GQR1XS
TYK-nu NVr1cJkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3O5NmlEPTB;MUKuN|k{OiEQvF2= MmHLV2FPT0WU
NMC-G1 MkPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmC5TWM2OD1zMj62NFYzKM7:TR?= NWTZTYdKW0GQR1XS
BB65-RCC MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\DeG9KSzVyPUGyMlcyPjlizszN NHe0V3FUSU6JRWK=
QIMR-WIL NGPHT21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzkTWM2OD1zMj64PFM{KM7:TR?= MoDTV2FPT0WU
D-566MG MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\tPVRtUUN3ME2xN{46PTd4IN88US=> MWPTRW5ITVJ?
KYSE-140 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEK2VW9KSzVyPUG0MlA4PTNizszN NVTrcGFRW0GQR1XS
SCC-4 MlPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTF2LkOzOVkh|ryP NITabYNUSU6JRWK=
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5637 MnzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLyTWM2OD1{MD6wOFc5KM7:TR?= NVLYdYNvW0GQR1XS
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T47D MlHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTJ{Lke5O|kh|ryP NUjEfnFbW0GQR1XS
HT-1197 NGDScYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnjfm9KSzVyPUKzMlA5OTdizszN NXnBU3NxW0GQR1XS
LB2518-MEL M{LYO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjudIV1UUN3ME2yN{43PDF{IN88US=> MUfTRW5ITVJ?
J-RT3-T3-5 MkLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\PTWM2OD1{ND63OVk2KM7:TR?= NGHhcI1USU6JRWK=
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NCI-H526 NY\GeXFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTJ3LkCwNlMh|ryP NEHkRXFUSU6JRWK=
IST-SL1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;CRmlEPTB;MkWuNlc2OSEQvF2= NG\aSmxUSU6JRWK=
HH NULaUJhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfIfmE6UUN3ME2yOU4{OTl{IN88US=> NUX5co51W0GQR1XS
NCI-H82 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTj[otKSzVyPUK1Mlk{QCEQvF2= MlLhV2FPT0WU
SNU-449 MkTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzyeXl2UUN3ME2yO{4zODF6IN88US=> MnP0V2FPT0WU
COR-L23 Mm\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHqfpdKSzVyPUK3MlI5OTNizszN NYjaZ5FHW0GQR1XS
LOXIMVI MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPtUpJKSzVyPUK3MlM3QCEQvF2= MVLTRW5ITVJ?
GR-ST MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkW4TWM2OD1{Nz62O|A3KM7:TR?= MXvTRW5ITVJ?
NCI-SNU-1 NVPRfYlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HvT2lEPTB;MkeuPVQ1KM7:TR?= MnjlV2FPT0WU
ALL-PO MlPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTJ6LkG2NFQh|ryP NHHlcXRUSU6JRWK=
ML-2 M1THNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7LWW1KSzVyPUK4MlI5OTRizszN NHT6[WNUSU6JRWK=
HOP-62 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTpTWM2OD1{OD63NVMh|ryP NH:5TYxUSU6JRWK=
EGI-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTnXnBKSzVyPUK4Mlg5PDVizszN M4fn[3NCVkeHUh?=
TCCSUP NGntR2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXi5[oxHUUN3ME2yPE46Ojd{IN88US=> M4XJNXNCVkeHUh?=
LB996-RCC NFy4NoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4S5SmlEPTB;MkmuOVY5OiEQvF2= M1P3ZXNCVkeHUh?=
LCLC-97TM1 M1nlRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHviV5dKSzVyPUOyMlE6PjRizszN NYfJWpVlW0GQR1XS
NCI-H1304 NYPNeGRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTN{LkOzNFEh|ryP MV;TRW5ITVJ?
KP-N-YS M{fPd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTN{LkW5O|Mh|ryP NFe0S|hUSU6JRWK=
NCI-H1770 MojNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTN|LkG2OFgh|ryP M1fuVnNCVkeHUh?=
EM-2 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLV[FlKSzVyPUOzMlY2ODRizszN MkToV2FPT0WU
ChaGo-K-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTQTWM2OD1|Mz63NlM3KM7:TR?= NUjLSIlqW0GQR1XS
ACHN NWH3eIZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HId2lEPTB;M{OuPFM5PSEQvF2= NVPXfpBEW0GQR1XS
MN-60 MoCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M173fWlEPTB;M{OuPFU1PCEQvF2= MkDVV2FPT0WU
EW-18 NYjwZlhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUj1[lZsUUN3ME2zN{45QTdzIN88US=> MlThV2FPT0WU
KGN MkLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\mSFJZUUN3ME2zOU44Ojl{IN88US=> MoTVV2FPT0WU
U031 NInrTXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\lN2lEPTB;M{WuPFE{OiEQvF2= NVnhTVVYW0GQR1XS
HMV-II NVT5O3dVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTN4LkC3O|Qh|ryP M{G4cXNCVkeHUh?=
L-363 M1\CUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnTdWxKSzVyPUO3MlY1PTVizszN NGT0U2NUSU6JRWK=
NCI-H1155 MljTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v4bmlEPTB;M{iuNFAyPSEQvF2= MnPnV2FPT0WU
NCI-H1793 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTN6LkGwNlYh|ryP NXPRbGdKW0GQR1XS
P30-OHK NVjoZop4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvPUYxKSzVyPUO4MlE{OzJizszN MV\TRW5ITVJ?
AN3-CA NVflflRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXCTnVKSzVyPUO4MlE3OTVizszN MXHTRW5ITVJ?
UACC-257 M4jSTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmP3TWM2OD1|OD63PUDPxE1? MVrTRW5ITVJ?
MCF7 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzKXIlVUUN3ME2zPU45PjJ7IN88US=> MVnTRW5ITVJ?
KP-N-YN MmfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPCWFBKSzVyPUSwMlQzQDVizszN MkXyV2FPT0WU
T98G MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTPOmFUUUN3ME20NE41QTV5IN88US=> NF3kR4hUSU6JRWK=
HGC-27 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrLTJhGUUN3ME20N{4zPzRizszN NVjtSYcxW0GQR1XS
NCI-H1092 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTR|LkK4PVUh|ryP Mn;0V2FPT0WU
KARPAS-299 M2LVd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7zNFYxUUN3ME20N{4{ODdzIN88US=> NYDQTYJiW0GQR1XS
LB1047-RCC M4DxUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHPOmY3UUN3ME20OE46QTV7IN88US=> Mlq0V2FPT0WU
786-0 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEO2XnJKSzVyPUS1MlY2KM7:TR?= NGfUSJZUSU6JRWK=
HCC2157 MonjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFr3W4pKSzVyPUS2MlA{PTlizszN M4LVW3NCVkeHUh?=
NY M2L5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonHTWM2OD12Nj6xO|c5KM7:TR?= MVHTRW5ITVJ?
EFM-19 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzhTWM2OD12Nj63OVM{KM7:TR?= MkXCV2FPT0WU
EW-16 NVP2S29uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnETWM2OD12Nj63PFA3KM7:TR?= NUjKOZRtW0GQR1XS
UM-UC-3 MljlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;Dcm9MUUN3ME20Ok45ODV7IN88US=> NYf4eGI6W0GQR1XS
HT-29 MnjrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TiTWlEPTB;NEeuPFc6OiEQvF2= MoOzV2FPT0WU
LN-405 NV3oc2Z6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTR6LkC4Nlch|ryP MlLuV2FPT0WU
NCI-H727 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnn6TWM2OD12OD63O|I3KM7:TR?= MUXTRW5ITVJ?
D-502MG M1PzOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzVTWM2OD12OD65Olc3KM7:TR?= M4rv[3NCVkeHUh?=
GMS-10 NWj3Oo1PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoKxTWM2OD12OT6yPVc1KM7:TR?= Ml3vV2FPT0WU
MEL-JUSO NGDLeHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjVTpN6UUN3ME20PU4{PDdizszN Mo\LV2FPT0WU

... 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