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 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

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)
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 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rPSmlEPTB;MD6wO|Q2PyEQvF2= M4TSOXNCVkeHUh?=
EoL-1-cell MofkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTBwMUSxOlYh|ryP NEXxNZNUSU6JRWK=
C32 NUL6V3JDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\WU2lEPTB;MD6xOVE{OSEQvF2= NXXQcHNQW0GQR1XS
M14 M4PEfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3e3VmlEPTB;MD6yNVc2PyEQvF2= MVTTRW5ITVJ?
CP50-MEL-B NWfvbYFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vQXmlEPTB;MD6yPVc5PCEQvF2= NIOyVZlUSU6JRWK=
A101D M{nE[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorQTWM2OD1yLkOyOVg6KM7:TR?= M4TES3NCVkeHUh?=
G-361 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmW5TWM2OD1yLkO0OlM4KM7:TR?= NIHOeo1USU6JRWK=
HT-144 NUPU[ZpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTBwM{[zNlkh|ryP M3q0b3NCVkeHUh?=
ACN MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPoSnhKSzVyPUCuN|g1PzdizszN NWPnNG9JW0GQR1XS
COLO-829 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4D5SWlEPTB;MD6zPFk3QCEQvF2= M2HnR3NCVkeHUh?=
MEL-HO NE[0S4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moi2TWM2OD1yLkSxNVc6KM7:TR?= MVfTRW5ITVJ?
SH-4 NX3rU2VYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnQWYZ3UUN3ME2wMlQyPDJ{IN88US=> M2XnUnNCVkeHUh?=
SK-MEL-3 NVLwUlZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULVbYJuUUN3ME2wMlUyPTZ6IN88US=> Mn;WV2FPT0WU
A375 NY\GUGRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TlO2lEPTB;MD62O|M2QSEQvF2= MYrTRW5ITVJ?
MMAC-SF NILOVYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTBwNki2NVQh|ryP NFnE[ndUSU6JRWK=
BHT-101 MlzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWraPVJPUUN3ME2wMlcxPzB{IN88US=> NUf4RnM1W0GQR1XS
K5 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzV[HdMUUN3ME2wMlc3OTR6IN88US=> NEnjbVRUSU6JRWK=
BV-173 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3TZnJKSzVyPUCuO|k3PDRizszN MlLoV2FPT0WU
RVH-421 M4nuR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHJWWhKUUN3ME2wMlg3Pzl4IN88US=> NVjtdYxMW0GQR1XS
HCC2218 NYLwXFI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYG1SplUUUN3ME2wMlg4QDR2IN88US=> NHLJXHZUSU6JRWK=
WM-115 NHjWN5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfJ[4c6UUN3ME2wMlg5Pjl{IN88US=> MX3TRW5ITVJ?
SK-MEL-28 Ml3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXXSXBWUUN3ME2xMlA1PTZ7IN88US=> Mk\zV2FPT0WU
COLO-679 NGLpVYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXJblZKSzVyPUGuNVA1PjRizszN NHzCZWZUSU6JRWK=
MZ7-mel MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvwcJNKSzVyPUGuNVQ6PjNizszN MXHTRW5ITVJ?
SK-MEL-30 M3zreGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTLT|lPUUN3ME2xMlM{Ozh4IN88US=> NF2yR5pUSU6JRWK=
NCI-H209 NGDMXGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXf3VFlZUUN3ME2xMlYxQDZizszN MmjGV2FPT0WU
HTC-C3 NX3Xe3VyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFL4dFZKSzVyPUGuOlYzQTRizszN M1jJUHNCVkeHUh?=
KARPAS-45 M4jPV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTJwMES5O|gh|ryP NVSwWGNpW0GQR1XS
NCI-SNU-5 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2S2[WlEPTB;Mj6xNVk3QSEQvF2= MkjFV2FPT0WU
KP-4 M{HwUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\IWGlEPTB;Mj6zNFc5PyEQvF2= MnX4V2FPT0WU
PA-1 M{C5S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYG2SG5HUUN3ME2yMlczPjd|IN88US=> NHfvUG5USU6JRWK=
HuO-3N1 Mki1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTJwOEe5OFYh|ryP M4L1dnNCVkeHUh?=
NCI-H358 NF\oZo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPqTWM2OD1{LkmyNlMzKM7:TR?= MUDTRW5ITVJ?
CTB-1 M1rKd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\TNHhKSzVyPUOuOFAyPzZizszN Ml\jV2FPT0WU
697 M3vFUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4mwNWlEPTB;Mz61OVI3PiEQvF2= MmW3V2FPT0WU
CP66-MEL NIradXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTWV3VKSzVyPUSuNVU6OjdizszN NHvsZ5JUSU6JRWK=
NB13 MkLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jyXmlEPTB;ND60PVE4QSEQvF2= MlPSV2FPT0WU
DBTRG-05MG MlLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7qTWM2OD12LkWzN|I2KM7:TR?= MYXTRW5ITVJ?
A2058 NYiyTXJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTRwN{KxOlQh|ryP M1;HVXNCVkeHUh?=
KG-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlntTWM2OD12LkezPVA5KM7:TR?= NELXdlJUSU6JRWK=
8305C MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPPZo9KSzVyPUWuNVg4OyEQvF2= M{TVPXNCVkeHUh?=
RPMI-7951 NF;vNnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTVwOECyPFMh|ryP NGL1ToZUSU6JRWK=
CHL-1 Mlr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLzXIxKSzVyPUWuPVc3ODNizszN Mkn4V2FPT0WU
TI-73 NGP6SFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\6PGlEPTB;Nj6wNFkxOiEQvF2= NW\XfXpyW0GQR1XS
HT-1080 M1rtZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTVd4NlUUN3ME22MlExQTR4IN88US=> Moj5V2FPT0WU
ES5 NGjJNYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTP[mhqUUN3ME22MlE1QTJ2IN88US=> MlfUV2FPT0WU
8-MG-BA NWq5fVBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTGdWtKSzVyPU[uNVgyOjlizszN M1zlOHNCVkeHUh?=
NB7 M{LvXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHt[WtKSzVyPU[uNlE{PzNizszN MnnaV2FPT0WU
H4 NV7LXWVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LXeGlEPTB;Nj6yNlQ6OyEQvF2= NV34[Is6W0GQR1XS
CAL-72 NHLKWGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPaTWM2OD14LkS1OFI{KM7:TR?= NIC2bVdUSU6JRWK=
HCC1806 M3:5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3[2[2lEPTB;Nj64NVk{OSEQvF2= M1KyPHNCVkeHUh?=
BCPAP MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjXWFlQUUN3ME23MlIyPzZ2IN88US=> M{S4[3NCVkeHUh?=
LB2241-RCC NX\xW2lwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTdwM{[5NFch|ryP NX2y[op3W0GQR1XS
COLO-741 NVHj[o1ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\hOGlEPTB;OD6wNVY4QSEQvF2= M3XnUHNCVkeHUh?=
HSC-3 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljrTWM2OD16LkC3NFY5KM7:TR?= NYLvWGNTW0GQR1XS
SW982 MnPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnf3TWM2OD16LkSxOVE3KM7:TR?= NITvNlZUSU6JRWK=
GCT NYnxdI56T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\JXmlEPTB;OD63OVMyPCEQvF2= NYnPcJVlW0GQR1XS
KY821 NHzHS3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfkTWM2OD17LkC1NVc5KM7:TR?= M4DlfXNCVkeHUh?=
JVM-3 NGnUZmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHvR4c2UUN3ME25MlU3QTl7IN88US=> MYDTRW5ITVJ?
RS4-11 MlPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvFTWM2OD17Lk[wOFgh|ryP M3\6e3NCVkeHUh?=
VA-ES-BJ Mof3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTFyLkCxOFkh|ryP MX\TRW5ITVJ?
A431 NVrHT2NDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTFyLkSyNVIh|ryP NF\2cmVUSU6JRWK=
LXF-289 M{LoWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjrXVhGUUN3ME2xNE41PThizszN NXLOW2twW0GQR1XS
SK-MEL-24 M4\uR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\qTWM2OD1zMD64Nlc1KM7:TR?= NHrJZW1USU6JRWK=
NOS-1 NUjNVoFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTZV4xKSzVyPUGwMlg1PzJizszN Moe5V2FPT0WU
KNS-62 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfUU2RpUUN3ME2xNU4zPDB2IN88US=> MXvTRW5ITVJ?
SK-HEP-1 NHXU[2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTFzLkO1Nlch|ryP Ml7YV2FPT0WU
A3-KAW MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnhTFZmUUN3ME2xNU44OTd6IN88US=> MUTTRW5ITVJ?
SK-LU-1 NHztS2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlK0TWM2OD1zMj6yOlU2KM7:TR?= M3LLNnNCVkeHUh?=
TYK-nu NVfTXo1NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLTTWM2OD1zMj6zPVMzKM7:TR?= NW\PVW16W0GQR1XS
NMC-G1 NEf2TVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPjc|ZKSzVyPUGyMlYxPjJizszN MlrFV2FPT0WU
BB65-RCC MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTF{LkexOlkh|ryP NIq5d5hUSU6JRWK=
QIMR-WIL Ml;nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLjTYxKSzVyPUGyMlg5OzNizszN NEXVT4VUSU6JRWK=
D-566MG NUjwc215T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7qTWM2OD1zMz65OVc3KM7:TR?= M1S2XnNCVkeHUh?=
KYSE-140 NFvuPFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\qemlEPTB;MUSuNFc2OyEQvF2= MUHTRW5ITVJ?
SCC-4 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTF2LkOzOVkh|ryP NWjzT25WW0GQR1XS
U251 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTF2Lki0PVIh|ryP M{TPVnNCVkeHUh?=
D-542MG MoHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvEfXZQUUN3ME2xOE46OjJ{IN88US=> NHznUWpUSU6JRWK=
LAMA-84 NHvsU2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXaRm9KSzVyPUG0Mlk6OzJizszN NUS4O|J3W0GQR1XS
NCI-H720 Mmr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LUU2lEPTB;MUWuNlY5PCEQvF2= M4PsW3NCVkeHUh?=
DEL NFryUFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\Ne|ZKSzVyPUG1MlQzQTNizszN MknsV2FPT0WU
SBC-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGD5TFZKSzVyPUG1MlQ{ODVizszN NX72[ZlXW0GQR1XS
ECC10 M3vCXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTF3LkS0OVgh|ryP MnLuV2FPT0WU
Daoy MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTF3Lke2NVYh|ryP NFHuU2tUSU6JRWK=
SCH NXLESIRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTF3Lke4N|Uh|ryP NVO4[WZ4W0GQR1XS
MZ2-MEL NXXLT|B4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTkb4cyUUN3ME2xOk4xPjR4IN88US=> NVTT[nA6W0GQR1XS
CAL-12T MlPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV30b3lJUUN3ME2xOk41QDZ{IN88US=> NWrSUpZkW0GQR1XS
KE-37 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnMeWEyUUN3ME2xOk45OTB5IN88US=> NWj6RohbW0GQR1XS
LS-411N M3;Xdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTF5LkGxPEDPxE1? M1rme3NCVkeHUh?=
NCI-H2228 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nTfmlEPTB;MUeuN|A4OSEQvF2= M{HuR3NCVkeHUh?=
SK-MEL-2 NHjBVVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXVNoFKSzVyPUG3MlQ6PjVizszN MlftV2FPT0WU
HN MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDCUFlKSzVyPUG3MlczPDhizszN MkXjV2FPT0WU
NCI-H1648 MnP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTF5LkixPEDPxE1? M3PmXHNCVkeHUh?=
IA-LM MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fIcmlEPTB;MUiuN|E4OiEQvF2= NE\CbHJUSU6JRWK=
EW-13 M3P1Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvDTWM2OD1zOD61O|A5KM7:TR?= M3[0PHNCVkeHUh?=
YKG-1 NUfDeJE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYiyOGFLUUN3ME2xPU42PzFzIN88US=> MnvoV2FPT0WU
KNS-81-FD MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrLTlgyUUN3ME2xPU42QDV6IN88US=> MXvTRW5ITVJ?
23132-87 M17yXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jYTGlEPTB;MUmuO|Y1OiEQvF2= NGPTRmxUSU6JRWK=
NUGC-3 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2H1WWlEPTB;MUmuPVg5PyEQvF2= MVXTRW5ITVJ?
5637 MmDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHC[FZmUUN3ME2yNE4xPDd6IN88US=> MUjTRW5ITVJ?
NCI-H1755 MkXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXNUpdKSzVyPUKwMlQ4PjRizszN MWLTRW5ITVJ?
RH-18 NH;lfo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofPTWM2OD1{MD61O|Q5KM7:TR?= MWjTRW5ITVJ?
RXF393 NFS3VFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXIeIRKSzVyPUKwMlY4PTZizszN M2rTd3NCVkeHUh?=
LU-134-A Ml;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\WW29KSzVyPUKwMlcxPTZizszN MYLTRW5ITVJ?
TE-12 M3HVS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4[1[WlEPTB;MkCuO|IxOSEQvF2= Ml[zV2FPT0WU
MOLT-4 NEXKW21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXX[29KSzVyPUKxMlE6OTVizszN Mm[wV2FPT0WU
IGR-1 M2nFPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTJzLkO3PVYh|ryP NIP2UoVUSU6JRWK=
HOP-92 NUfidZJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTJzLkS5PFch|ryP NUfBdotRW0GQR1XS
SK-MES-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHS2OGdKSzVyPUKxMlc{QDFizszN NHu0Z3JUSU6JRWK=
LU-65 M4nkd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTkVJV1UUN3ME2yNU45PjJ2IN88US=> NUHOdoZPW0GQR1XS
MS-1 M1vIVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDScI1KSzVyPUKyMlEzODNizszN MVvTRW5ITVJ?
LoVo MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXYTWM2OD1{Mj6yOFQh|ryP MXnTRW5ITVJ?
A704 NV\XRlJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;YWJY5UUN3ME2yNk42OTV3IN88US=> NF3aTlJUSU6JRWK=
HT-1376 NH3QbZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fWOGlEPTB;MkKuOlA2QSEQvF2= NY\xdJpuW0GQR1XS
IST-MEL1 NUDwSmJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\nUWlEPTB;MkKuOlc2OSEQvF2= Mki2V2FPT0WU
Ramos-2G6-4C10 M2HDTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXySIpKSzVyPUKyMlc{PjZizszN M1O0fXNCVkeHUh?=
T47D M3HGR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYizPXNxUUN3ME2yNk44QTd7IN88US=> NIe1c5RUSU6JRWK=
HT-1197 NVi3PHluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2npOWlEPTB;MkOuNFgyPyEQvF2= NUH5T3dFW0GQR1XS
LB2518-MEL M16xWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTJ|Lk[0NVIh|ryP MYLTRW5ITVJ?
J-RT3-T3-5 NXrnepJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXvVGZKSzVyPUK0Mlc2QTVizszN NV\O[Ih5W0GQR1XS
SK-NEP-1 NEe5SWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTJ2Lki3OFQh|ryP MUDTRW5ITVJ?
NCI-H526 MkLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTJ3LkCwNlMh|ryP MmPJV2FPT0WU
IST-SL1 NV[4b3dCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;MU2lEPTB;MkWuNlc2OSEQvF2= NF[2NXRUSU6JRWK=
HH NGPuU3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7yN202UUN3ME2yOU4{OTl{IN88US=> NYTGUJNxW0GQR1XS
NCI-H82 M2PFW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVO1UVZVUUN3ME2yOU46OzhizszN NIHwd2xUSU6JRWK=
SNU-449 NGTBZWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTJ5LkKwNVgh|ryP M2LjNnNCVkeHUh?=
COR-L23 Mkf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M365OWlEPTB;MkeuNlgyOyEQvF2= MlTuV2FPT0WU
LOXIMVI NEP0cm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTJ5LkO2PEDPxE1? NUm4SpY4W0GQR1XS
GR-ST NFjkbmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkD4TWM2OD1{Nz62O|A3KM7:TR?= MW\TRW5ITVJ?
NCI-SNU-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LIbWlEPTB;MkeuPVQ1KM7:TR?= M4HrN3NCVkeHUh?=
ALL-PO MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7tWXZuUUN3ME2yPE4yPjB2IN88US=> M1rkSnNCVkeHUh?=
ML-2 NVXCR|B4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjB[HpKSzVyPUK4MlI5OTRizszN MYfTRW5ITVJ?
HOP-62 NHLEV4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXzTGROUUN3ME2yPE44OTNizszN MoXJV2FPT0WU
EGI-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTJ6Lki4OFUh|ryP NXu1bpFLW0GQR1XS
TCCSUP NVToe|QzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTJ6LkmyO|Ih|ryP MmrKV2FPT0WU
LB996-RCC NX3nNFhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ftNWlEPTB;MkmuOVY5OiEQvF2= NIf6N45USU6JRWK=
LCLC-97TM1 NWXzV2FZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDwTWM2OD1|Mj6xPVY1KM7:TR?= MnLXV2FPT0WU
NCI-H1304 M{HOcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rDS2lEPTB;M{KuN|MxOSEQvF2= M3PwOnNCVkeHUh?=
KP-N-YS M1z5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTN{LkW5O|Mh|ryP M2\IfXNCVkeHUh?=
NCI-H1770 M1voOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYC5TZJpUUN3ME2zN{4yPjR6IN88US=> MUXTRW5ITVJ?
EM-2 NFuxSVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfPepNmUUN3ME2zN{43PTB2IN88US=> M2rDdHNCVkeHUh?=
ChaGo-K-1 NX63V29LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUizenNKUUN3ME2zN{44OjN4IN88US=> MlXDV2FPT0WU
ACHN M1\WU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjLTWM2OD1|Mz64N|g2KM7:TR?= MkLOV2FPT0WU
MN-60 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{e1d2lEPTB;M{OuPFU1PCEQvF2= NYHMV4l1W0GQR1XS
EW-18 NITxdVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXmTWM2OD1|Mz64PVcyKM7:TR?= MXfTRW5ITVJ?
KGN MoHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnCV2xKUUN3ME2zOU44Ojl{IN88US=> NVvrZWkzW0GQR1XS
U031 M1joR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4C3fWlEPTB;M{WuPFE{OiEQvF2= NW\6cJpsW0GQR1XS
HMV-II M370N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nzemlEPTB;M{[uNFc4PCEQvF2= MVTTRW5ITVJ?
L-363 M3zteWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTN5Lk[0OVUh|ryP M1;x[3NCVkeHUh?=
NCI-H1155 M1LofWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\Ne5lCUUN3ME2zPE4xODF3IN88US=> MUfTRW5ITVJ?
NCI-H1793 M{jicGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\0doFrUUN3ME2zPE4yODJ4IN88US=> NXLvR3ZUW0GQR1XS
P30-OHK NYTqcY9WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTseHJKSzVyPUO4MlE{OzJizszN M1uwV3NCVkeHUh?=
AN3-CA MlLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLPZot3UUN3ME2zPE4yPjF3IN88US=> M3zTWHNCVkeHUh?=
UACC-257 M2Dp[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPrTWM2OD1|OD63PUDPxE1? NWHGe5hHW0GQR1XS
MCF7 NUXmcpBtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLacpFKSzVyPUO5Mlg3OjlizszN NFPu[o9USU6JRWK=
KP-N-YN NEXodI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkD2TWM2OD12MD60Nlg2KM7:TR?= MVrTRW5ITVJ?
T98G MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjZUoROUUN3ME20NE41QTV5IN88US=> MlPpV2FPT0WU
HGC-27 MmrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIThVJhKSzVyPUSzMlI4PCEQvF2= NVXxb5pRW0GQR1XS
NCI-H1092 M4e0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGWyTFlKSzVyPUSzMlI5QTVizszN NG\tRYZUSU6JRWK=
KARPAS-299 M1X0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{j6fGlEPTB;NEOuN|A4OSEQvF2= Mm[0V2FPT0WU
LB1047-RCC NIrHOXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vMRWlEPTB;NESuPVk2QSEQvF2= M13zSXNCVkeHUh?=
786-0 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4WyTWlEPTB;NEWuOlUh|ryP NIfhSFNUSU6JRWK=
HCC2157 Mn61S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;KNGdKSzVyPUS2MlA{PTlizszN MoLNV2FPT0WU
NY M3XW[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITNbohKSzVyPUS2MlE4PzhizszN MlTxV2FPT0WU
EFM-19 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGixOpdKSzVyPUS2Mlc2OzNizszN NIPNS3ZUSU6JRWK=
EW-16 Mn21S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTR4Lke4NFYh|ryP NV3QRXZNW0GQR1XS
UM-UC-3 M4rOfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;VPWlEPTB;NE[uPFA2QSEQvF2= NX3xUXNYW0GQR1XS
HT-29 MoD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXleI1QUUN3ME20O{45Pzl{IN88US=> NYK1SIpUW0GQR1XS
LN-405 M2C0d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrq[ldKSzVyPUS4MlA5OjdizszN MlzTV2FPT0WU
NCI-H727 Mly3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVv5bo9CUUN3ME20PE44PzJ4IN88US=> NWSwW|BYW0GQR1XS
D-502MG NYj6[IVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTR6Lkm2O|Yh|ryP NXvWSVh7W0GQR1XS
GMS-10 NH;sTIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rhd2lEPTB;NEmuNlk4PCEQvF2= M4D2R3NCVkeHUh?=
MEL-JUSO MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTR7LkO0O{DPxE1? NFTac2JUSU6JRWK=

... 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 <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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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

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Raf Signaling Pathway Map

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