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
USD 120 In stock
USD 270 In stock
USD 670 In stock

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Cited by 45 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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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)
FRK [1]
(Cell-free assay)
6.7 nM 13 nM 130 nM 160 nM 1.3 μM
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 MlrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTBwMEe0OVch|ryP NVHRPVN7W0GQR1XS
EoL-1-cell MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvWTWM2OD1yLkG0NVY3KM7:TR?= MUPTRW5ITVJ?
C32 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPMTWM2OD1yLkG1NVMyKM7:TR?= MnT2V2FPT0WU
M14 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvLTWM2OD1yLkKxO|U4KM7:TR?= Mlu3V2FPT0WU
CP50-MEL-B MnTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDQZlluUUN3ME2wMlI6Pzh2IN88US=> NEHEd|VUSU6JRWK=
A101D Mm\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvVTWM2OD1yLkOyOVg6KM7:TR?= M3HmRXNCVkeHUh?=
G-361 Mm\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnBcG83UUN3ME2wMlM1PjN5IN88US=> NUjBbphmW0GQR1XS
HT-144 NVnhe21JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfIeXlOUUN3ME2wMlM3OzJ7IN88US=> MXnTRW5ITVJ?
ACN NHTWW2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rpemlEPTB;MD6zPFQ4PyEQvF2= M37UWHNCVkeHUh?=
COLO-829 NYHyVmIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIn4R4VKSzVyPUCuN|g6PjhizszN NIX3VYVUSU6JRWK=
MEL-HO MmruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jt[mlEPTB;MD60NVE4QSEQvF2= MXzTRW5ITVJ?
SH-4 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVG0c4VEUUN3ME2wMlQyPDJ{IN88US=> MWTTRW5ITVJ?
SK-MEL-3 MlzuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HvfGlEPTB;MD61NVU3QCEQvF2= M2nqd3NCVkeHUh?=
A375 MoTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{D0Z2lEPTB;MD62O|M2QSEQvF2= NHS0N4tUSU6JRWK=
MMAC-SF NYX6cGxDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3hfoxKSzVyPUCuOlg3OTRizszN MWHTRW5ITVJ?
BHT-101 NXHKSWlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTWXVJKSzVyPUCuO|A4ODJizszN MUPTRW5ITVJ?
K5 NVuzXYhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDPbJhKSzVyPUCuO|YyPDhizszN MULTRW5ITVJ?
BV-173 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzGR2xKSzVyPUCuO|k3PDRizszN M{SxVXNCVkeHUh?=
RVH-421 NXPrXIlDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LNOGlEPTB;MD64Olc6PiEQvF2= MV;TRW5ITVJ?
HCC2218 M2\ZNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\pTWM2OD1yLki3PFQ1KM7:TR?= MnPYV2FPT0WU
WM-115 NXOxTnlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwOEi2PVIh|ryP M2[xeHNCVkeHUh?=
SK-MEL-28 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\kTYNoUUN3ME2xMlA1PTZ7IN88US=> NVH6TZFFW0GQR1XS
COLO-679 M3jzR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF[zOXlKSzVyPUGuNVA1PjRizszN Mnn3V2FPT0WU
MZ7-mel NIf6VVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHG2bWZKSzVyPUGuNVQ6PjNizszN NUXYfFN1W0GQR1XS
SK-MEL-30 M4jqTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDqS5lKSzVyPUGuN|M{QDZizszN NIjlbHlUSU6JRWK=
NCI-H209 M3PDWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\PdHVKSzVyPUGuOlA5PiEQvF2= NXjFTJBIW0GQR1XS
HTC-C3 M3;w[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTFwNk[yPVQh|ryP NXrFTJVTW0GQR1XS
KARPAS-45 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJwMES5O|gh|ryP MVvTRW5ITVJ?
NCI-SNU-5 MlHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnziTWM2OD1{LkGxPVY6KM7:TR?= M2jzbXNCVkeHUh?=
KP-4 M4HPb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJwM{C3PFch|ryP NUK5XGxlW0GQR1XS
PA-1 NX\R[FdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfxTWM2OD1{LkeyOlc{KM7:TR?= NVfhV3ROW0GQR1XS
HuO-3N1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;ZUWpKSzVyPUKuPFc6PDZizszN M4LnbHNCVkeHUh?=
NCI-H358 NGfhTpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn6yTWM2OD1{LkmyNlMzKM7:TR?= M1nHR3NCVkeHUh?=
CTB-1 NVf2N|kyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DKeGlEPTB;Mz60NFE4PiEQvF2= NEnSW3RUSU6JRWK=
697 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTNwNUWyOlYh|ryP MWrTRW5ITVJ?
CP66-MEL M3;3[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;XeWlEPTB;ND6xOVkzPyEQvF2= Mn25V2FPT0WU
NB13 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn75TWM2OD12LkS5NVc6KM7:TR?= NFW3NoFUSU6JRWK=
DBTRG-05MG NVO1RmtyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTRwNUOzNlUh|ryP NG\1O5FUSU6JRWK=
A2058 MlnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rNRWlEPTB;ND63NlE3PCEQvF2= NWfVV3RUW0GQR1XS
KG-1 NUO3elhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTRwN{O5NFgh|ryP NFi5NGZUSU6JRWK=
8305C NHzP[IFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1z0UWlEPTB;NT6xPFc{KM7:TR?= M4LkXnNCVkeHUh?=
RPMI-7951 MoXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTVwOECyPFMh|ryP MX7TRW5ITVJ?
CHL-1 NVmxU|RMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3L6Z2lEPTB;NT65O|YxOyEQvF2= M37UWXNCVkeHUh?=
TI-73 NYL5S5lxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnPd4tWUUN3ME22MlAxQTB{IN88US=> NVjRWGNLW0GQR1XS
HT-1080 NV\1TlB3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTZwMUC5OFYh|ryP MWTTRW5ITVJ?
ES5 M2\kUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\V[lRnUUN3ME22MlE1QTJ2IN88US=> NV7uZpBNW0GQR1XS
8-MG-BA NHe5VnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnOTWM2OD14LkG4NVI6KM7:TR?= MULTRW5ITVJ?
NB7 NYe2NGN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUK1ZmtSUUN3ME22MlIyOzd|IN88US=> MkPaV2FPT0WU
H4 NGDSW2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTCNlhKSzVyPU[uNlI1QTNizszN NHfuSHhUSU6JRWK=
CAL-72 M2jIcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTZwNEW0NlMh|ryP MUjTRW5ITVJ?
HCC1806 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTZwOEG5N|Eh|ryP NWm2Z2p5W0GQR1XS
BCPAP Mn7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITZN4lKSzVyPUeuNlE4PjRizszN MUXTRW5ITVJ?
LB2241-RCC NX\aOVROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rtZmlEPTB;Nz6zOlkxPyEQvF2= NWPlNYZHW0GQR1XS
COLO-741 M{LuZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWiwOmIzUUN3ME24MlAyPjd7IN88US=> NYL2RZFkW0GQR1XS
HSC-3 NXfUO5hXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHW4RndKSzVyPUiuNFcxPjhizszN MXnTRW5ITVJ?
SW982 M{\Qcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRThwNEG1NVYh|ryP MkC2V2FPT0WU
GCT MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;0VGxyUUN3ME24Mlc2OzF2IN88US=> M{XLTXNCVkeHUh?=
KY821 NWXqRWJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTlwMEWxO|gh|ryP NXPqRnlsW0GQR1XS
JVM-3 M4W0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\5TWM2OD17LkW2PVk6KM7:TR?= MXPTRW5ITVJ?
RS4-11 MnfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHuUnJrUUN3ME25MlYxPDhizszN MXjTRW5ITVJ?
VA-ES-BJ MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjHbIltUUN3ME2xNE4xOTR7IN88US=> NYHjS2JiW0GQR1XS
A431 M2nkdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjOVYhKSzVyPUGwMlQzOTJizszN NX;GcWZiW0GQR1XS
LXF-289 M4fLUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3n4ZWlEPTB;MUCuOFU5KM7:TR?= NWnMN3A3W0GQR1XS
SK-MEL-24 NIDpN5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTFyLkiyO|Qh|ryP NX[1TlhJW0GQR1XS
NOS-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTFyLki0O|Ih|ryP NH;K[JdUSU6JRWK=
KNS-62 M3HYcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXQOJBKSzVyPUGxMlI1ODRizszN MknIV2FPT0WU
SK-HEP-1 M{nEfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTFzLkO1Nlch|ryP NEi4RmxUSU6JRWK=
A3-KAW MlTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHmTWM2OD1zMT63NVc5KM7:TR?= M4XGbnNCVkeHUh?=
SK-LU-1 MkDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2e2W2lEPTB;MUKuNlY2PSEQvF2= MVzTRW5ITVJ?
TYK-nu NXWy[YZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrTc3JKSzVyPUGyMlM6OzJizszN NGPrUndUSU6JRWK=
NMC-G1 M3TNNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rRV2lEPTB;MUKuOlA3OiEQvF2= MWPTRW5ITVJ?
BB65-RCC NXPKd5hWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3LclczUUN3ME2xNk44OTZ7IN88US=> NYnaXpBnW0GQR1XS
QIMR-WIL NHrteJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXaeY1KSzVyPUGyMlg5OzNizszN MmLXV2FPT0WU
D-566MG Mnm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3pRXZKSzVyPUGzMlk2PzZizszN Mo\GV2FPT0WU
KYSE-140 NWPOdG9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HtS2lEPTB;MUSuNFc2OyEQvF2= Mn\UV2FPT0WU
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NCI-H526 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELmXZVKSzVyPUK1MlAxOjNizszN NVXwUHg1W0GQR1XS
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HH NFn6bodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPxdJhKSzVyPUK1MlMyQTJizszN MW\TRW5ITVJ?
NCI-H82 M1z2e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLBdFh2UUN3ME2yOU46OzhizszN MX3TRW5ITVJ?
SNU-449 NXzDbIZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTJ5LkKwNVgh|ryP NV\MfW9PW0GQR1XS
COR-L23 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7mTWM2OD1{Nz6yPFE{KM7:TR?= M1raOHNCVkeHUh?=
LOXIMVI MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\5eW5KSzVyPUK3MlM3QCEQvF2= M1mwe3NCVkeHUh?=
GR-ST MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnDfJRKSzVyPUK3MlY4ODZizszN NVOyN|RbW0GQR1XS
NCI-SNU-1 NF:zNWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfjSVRKSzVyPUK3Mlk1PCEQvF2= NFPSdFFUSU6JRWK=
ALL-PO NVPBdWYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXXTWM2OD1{OD6xOlA1KM7:TR?= MV3TRW5ITVJ?
ML-2 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTJ6LkK4NVQh|ryP M4T6NHNCVkeHUh?=
HOP-62 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIqzU29KSzVyPUK4MlcyOyEQvF2= MkHwV2FPT0WU
EGI-1 NWDWfHo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{K0TWlEPTB;MkiuPFg1PSEQvF2= MlnvV2FPT0WU
TCCSUP M1ryXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTJ6LkmyO|Ih|ryP NG\ycHpUSU6JRWK=
LB996-RCC MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTJ7LkW2PFIh|ryP NIS2NYFUSU6JRWK=
LCLC-97TM1 NFvRTXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTN{LkG5OlQh|ryP NWPUcGsxW0GQR1XS
NCI-H1304 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTN{LkOzNFEh|ryP M4LRd3NCVkeHUh?=
KP-N-YS NWDhcmM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvMTWM2OD1|Mj61PVc{KM7:TR?= NI\RUWRUSU6JRWK=
NCI-H1770 MlLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTN|LkG2OFgh|ryP NVHtb2FwW0GQR1XS
EM-2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrWWlNKSzVyPUOzMlY2ODRizszN M4PmRnNCVkeHUh?=
ChaGo-K-1 MknoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTN|LkeyN|Yh|ryP NGXFVJpUSU6JRWK=
ACHN NIHkeolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17KZWlEPTB;M{OuPFM5PSEQvF2= NITFTnlUSU6JRWK=
MN-60 NEHSemtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\Gdm9KSzVyPUOzMlg2PDRizszN NU\YbI1zW0GQR1XS
EW-18 NU\JWYlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTN|Lki5O|Eh|ryP NISzUnVUSU6JRWK=
KGN NET4bmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vkSWlEPTB;M{WuO|I6OiEQvF2= MnvOV2FPT0WU
U031 NXT3NVJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7zTWM2OD1|NT64NVMzKM7:TR?= NXnPepRuW0GQR1XS
HMV-II M1W1bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTN4LkC3O|Qh|ryP Ml\TV2FPT0WU
L-363 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVexcVhpUUN3ME2zO{43PDV3IN88US=> M4excnNCVkeHUh?=
NCI-H1155 NX;JW3NkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jVZ2lEPTB;M{iuNFAyPSEQvF2= NVzNPVNnW0GQR1XS
NCI-H1793 NYXJUJBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HqUWlEPTB;M{iuNVAzPiEQvF2= MnTYV2FPT0WU
P30-OHK M4TzcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTN6LkGzN|Ih|ryP Mn7WV2FPT0WU
AN3-CA NUm3RWN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrYdJdKSzVyPUO4MlE3OTVizszN NX\XWoI6W0GQR1XS
UACC-257 MmTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLXZ4FEUUN3ME2zPE44QSEQvF2= NVK4WG5WW0GQR1XS
MCF7 Mk[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTN7Lki2Nlkh|ryP NGTWbFVUSU6JRWK=
KP-N-YN NY\4b3RvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfKNIFKSzVyPUSwMlQzQDVizszN NEHDV3FUSU6JRWK=
T98G M3HLPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vv[mlEPTB;NECuOFk2PyEQvF2= M1\ZfXNCVkeHUh?=
HGC-27 M3ruS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXPW5BuUUN3ME20N{4zPzRizszN NWDrbWYyW0GQR1XS
NCI-H1092 NVjiWGpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7YOnpKSzVyPUSzMlI5QTVizszN NFru[VRUSU6JRWK=
KARPAS-299 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Tzd2lEPTB;NEOuN|A4OSEQvF2= M4LrfHNCVkeHUh?=
LB1047-RCC M{XwVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvJbIhFUUN3ME20OE46QTV7IN88US=> NFzVeFdUSU6JRWK=
786-0 NHiwbnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTR3Lk[1JO69VQ>? M1;GRXNCVkeHUh?=
HCC2157 M{nmbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfiRlVzUUN3ME20Ok4xOzV7IN88US=> NELHNGRUSU6JRWK=
NY NIrHZXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTR4LkG3O|gh|ryP MkXBV2FPT0WU
EFM-19 NH62T3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnK0TWM2OD12Nj63OVM{KM7:TR?= NH;sNopUSU6JRWK=
EW-16 M2L0PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jhNGlEPTB;NE[uO|gxPiEQvF2= MXrTRW5ITVJ?
UM-UC-3 NF3ubpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrUTWM2OD12Nj64NFU6KM7:TR?= NYHhZ3FFW0GQR1XS
HT-29 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnmzTWM2OD12Nz64O|kzKM7:TR?= NXXNNlZRW0GQR1XS
LN-405 M3;rXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGK2S|RKSzVyPUS4MlA5OjdizszN NVrMbHpuW0GQR1XS
NCI-H727 NIL1NoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vXfmlEPTB;NEiuO|czPiEQvF2= NFrFR2VUSU6JRWK=
D-502MG MmLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG[0fI5KSzVyPUS4Mlk3PzZizszN NUntUJB1W0GQR1XS
GMS-10 NIfCfm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnOSXlKSzVyPUS5MlI6PzRizszN Mnn4V2FPT0WU
MEL-JUSO NIKxZWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4G1XWlEPTB;NEmuN|Q4KM7:TR?= Mnv3V2FPT0WU

... 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
+ 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
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  • 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
+ 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+50% PEG 300+5% Tween 80+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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