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.

    (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 NYP2W2g3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HBfWlEPTB;MD6wO|Q2PyEQvF2= NFvheYxUSU6JRWK=
EoL-1-cell M1r5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTNTWM2OD1yLkG0NVY3KM7:TR?= MmLjV2FPT0WU
C32 MoS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rk[mlEPTB;MD6xOVE{OSEQvF2= MYjTRW5ITVJ?
M14 MkXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTBwMkG3OVch|ryP MlTJV2FPT0WU
CP50-MEL-B M13t[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\PPGlEPTB;MD6yPVc5PCEQvF2= MknSV2FPT0WU
A101D MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmi3TWM2OD1yLkOyOVg6KM7:TR?= MnzPV2FPT0WU
G-361 MkjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;ZTWM2OD1yLkO0OlM4KM7:TR?= M2W3fnNCVkeHUh?=
HT-144 NUPHUnVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVOzeGRlUUN3ME2wMlM3OzJ7IN88US=> NEHMN45USU6JRWK=
ACN NGHjbJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTBwM{i0O|ch|ryP MWrTRW5ITVJ?
COLO-829 M4\xNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjLUGVKSzVyPUCuN|g6PjhizszN M3zyfnNCVkeHUh?=
MEL-HO NF7pdopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13VUWlEPTB;MD60NVE4QSEQvF2= M{TFcnNCVkeHUh?=
SH-4 M4\qRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVT1bIF3UUN3ME2wMlQyPDJ{IN88US=> NEThT|JUSU6JRWK=
SK-MEL-3 MkXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTWUVZsUUN3ME2wMlUyPTZ6IN88US=> NV3ySFFUW0GQR1XS
A375 NHv6eINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkX3TWM2OD1yLk[3N|U6KM7:TR?= MoDsV2FPT0WU
MMAC-SF Mmq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1f4XGlEPTB;MD62PFYyPCEQvF2= MYfTRW5ITVJ?
BHT-101 NIflZ2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XoV2lEPTB;MD63NFcxOiEQvF2= NXHUNIRPW0GQR1XS
K5 NIrncpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLre5FKSzVyPUCuO|YyPDhizszN NGfNcXhUSU6JRWK=
BV-173 M{PPXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTBwN{m2OFQh|ryP MV7TRW5ITVJ?
RVH-421 NGG4SnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPiPINSUUN3ME2wMlg3Pzl4IN88US=> Ml\PV2FPT0WU
HCC2218 NInMWmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlm4TWM2OD1yLki3PFQ1KM7:TR?= NI\GOmJUSU6JRWK=
WM-115 NXfOSIpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLYTWM2OD1yLki4OlkzKM7:TR?= MWfTRW5ITVJ?
SK-MEL-28 NHXjdmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX60UZZNUUN3ME2xMlA1PTZ7IN88US=> NXq3TXZIW0GQR1XS
COLO-679 NXvae|NZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTFwMUC0OlQh|ryP NVuzSYsxW0GQR1XS
MZ7-mel NFOwRWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmG4TWM2OD1zLkG0PVY{KM7:TR?= M1nEdXNCVkeHUh?=
SK-MEL-30 NWi0bnpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XtfmlEPTB;MT6zN|M5PiEQvF2= MlnZV2FPT0WU
NCI-H209 NGq2Z5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPXXGc4UUN3ME2xMlYxQDZizszN MlXyV2FPT0WU
HTC-C3 NYTkbIZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\mdIpKSzVyPUGuOlYzQTRizszN NELm[WNUSU6JRWK=
KARPAS-45 M{jwbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPqTWM2OD1{LkC0PVc5KM7:TR?= NG\sZZdUSU6JRWK=
NCI-SNU-5 MnHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYT3T41zUUN3ME2yMlEyQTZ7IN88US=> MV7TRW5ITVJ?
KP-4 NW\STGFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3noTWlEPTB;Mj6zNFc5PyEQvF2= MlO3V2FPT0WU
PA-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;WZYl[UUN3ME2yMlczPjd|IN88US=> NWDTSGltW0GQR1XS
HuO-3N1 MoTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTJwOEe5OFYh|ryP MVnTRW5ITVJ?
NCI-H358 M4DGfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fHSWlEPTB;Mj65NlI{OiEQvF2= NYTkOFlXW0GQR1XS
CTB-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\aSmlEPTB;Mz60NFE4PiEQvF2= NGi1NmhUSU6JRWK=
697 M{Dk[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3S4SmlEPTB;Mz61OVI3PiEQvF2= NXrtWIlYW0GQR1XS
CP66-MEL M{TBcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHsTWhKSzVyPUSuNVU6OjdizszN M3:2RnNCVkeHUh?=
NB13 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlKwTWM2OD12LkS5NVc6KM7:TR?= NGHP[m5USU6JRWK=
DBTRG-05MG NI\mUnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\OTWM2OD12LkWzN|I2KM7:TR?= M3\XPHNCVkeHUh?=
A2058 M4TCZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2L5XmlEPTB;ND63NlE3PCEQvF2= M4PRdXNCVkeHUh?=
KG-1 MnTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTISmZHUUN3ME20Mlc{QTB6IN88US=> Ml7ZV2FPT0WU
8305C NGnLb2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTVwMUi3N{DPxE1? M4nHNXNCVkeHUh?=
RPMI-7951 Mmm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljtTWM2OD13LkiwNlg{KM7:TR?= MmL0V2FPT0WU
CHL-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfhTWM2OD13Lkm3OlA{KM7:TR?= NHjheZRUSU6JRWK=
TI-73 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPPc45KSzVyPU[uNFA6ODJizszN NH;jNZpUSU6JRWK=
HT-1080 NYfyOHVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1e3[mlEPTB;Nj6xNFk1PiEQvF2= MXjTRW5ITVJ?
ES5 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTZwMUS5NlQh|ryP NVXFcZVxW0GQR1XS
8-MG-BA NIXROHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTTNHBKSzVyPU[uNVgyOjlizszN MXfTRW5ITVJ?
NB7 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTZwMkGzO|Mh|ryP NYD1enU1W0GQR1XS
H4 NES0Z4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnWRmliUUN3ME22MlIzPDl|IN88US=> NWD0SnUyW0GQR1XS
CAL-72 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fE[mlEPTB;Nj60OVQzOyEQvF2= Mo\DV2FPT0WU
HCC1806 NYTn[nBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTZwOEG5N|Eh|ryP M1PXdHNCVkeHUh?=
BCPAP MnHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV34XFN5UUN3ME23MlIyPzZ2IN88US=> NEn6WHFUSU6JRWK=
LB2241-RCC M2f6WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTdwM{[5NFch|ryP MY\TRW5ITVJ?
COLO-741 M1ztdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPVTWM2OD16LkCxOlc6KM7:TR?= NULt[3lyW0GQR1XS
HSC-3 Ml\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoO2TWM2OD16LkC3NFY5KM7:TR?= NI\QZ|RUSU6JRWK=
SW982 NXrKZVFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\VPHc6UUN3ME24MlQyPTF4IN88US=> NIX3d|lUSU6JRWK=
GCT MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13VXGlEPTB;OD63OVMyPCEQvF2= NVO5elViW0GQR1XS
KY821 NWjxeHF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYe2bHhjUUN3ME25MlA2OTd6IN88US=> NYDFeGV2W0GQR1XS
JVM-3 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHJTWM2OD17LkW2PVk6KM7:TR?= MUTTRW5ITVJ?
RS4-11 MonhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TaSGlEPTB;OT62NFQ5KM7:TR?= M2K0XHNCVkeHUh?=
VA-ES-BJ M17Cfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzHNXRKSzVyPUGwMlAyPDlizszN NHfxZZpUSU6JRWK=
A431 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M360VmlEPTB;MUCuOFIyOiEQvF2= M1jEOXNCVkeHUh?=
LXF-289 MkeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3VdYk{UUN3ME2xNE41PThizszN M3\lenNCVkeHUh?=
SK-MEL-24 NGHYOJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLnTWM2OD1zMD64Nlc1KM7:TR?= M3e0VHNCVkeHUh?=
NOS-1 MnLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTFyLki0O|Ih|ryP NYDSbWpHW0GQR1XS
KNS-62 NGG4TnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7qO4p4UUN3ME2xNU4zPDB2IN88US=> MXzTRW5ITVJ?
SK-HEP-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzSTWM2OD1zMT6zOVI4KM7:TR?= MmT1V2FPT0WU
A3-KAW MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoOyTWM2OD1zMT63NVc5KM7:TR?= NHyyW29USU6JRWK=
SK-LU-1 NIWzeXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTF{LkK2OVUh|ryP NGH6UmFUSU6JRWK=
TYK-nu MoXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTF{LkO5N|Ih|ryP MWfTRW5ITVJ?
NMC-G1 Mn7XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH[2cHpKSzVyPUGyMlYxPjJizszN MVvTRW5ITVJ?
BB65-RCC NGTZdZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnj4TWM2OD1zMj63NVY6KM7:TR?= M3PUU3NCVkeHUh?=
QIMR-WIL MmXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\DTWlEPTB;MUKuPFg{OyEQvF2= NGXFcJBUSU6JRWK=
D-566MG NUDaOYljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2X1OmlEPTB;MUOuPVU4PiEQvF2= Mn30V2FPT0WU
KYSE-140 M2XnfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGO0bZdKSzVyPUG0MlA4PTNizszN MkLFV2FPT0WU
SCC-4 NHfjOo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXnTWM2OD1zND6zN|U6KM7:TR?= M4m0dHNCVkeHUh?=
U251 M3T6cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTF2Lki0PVIh|ryP M1HLVXNCVkeHUh?=
D-542MG MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTF2LkmyNlIh|ryP NEjYfmRUSU6JRWK=
LAMA-84 Ml:1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3T0SmlEPTB;MUSuPVk{OiEQvF2= MUnTRW5ITVJ?
NCI-H720 MmTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPSTWM2OD1zNT6yOlg1KM7:TR?= NH3xUoFUSU6JRWK=
DEL M4Tubmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHBd|RKSzVyPUG1MlQzQTNizszN NUXnR|FFW0GQR1XS
SBC-1 NFnheHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTF3LkSzNFUh|ryP MWjTRW5ITVJ?
ECC10 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvpTHJKSzVyPUG1MlQ1PThizszN MVLTRW5ITVJ?
Daoy MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fNWGlEPTB;MUWuO|YyPiEQvF2= M2GxSXNCVkeHUh?=
SCH NFTRRpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljnTWM2OD1zNT63PFM2KM7:TR?= M2nqWXNCVkeHUh?=
MZ2-MEL MmT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HwbmlEPTB;MU[uNFY1PiEQvF2= NYG0UphiW0GQR1XS
CAL-12T MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTF4LkS4OlIh|ryP MWTTRW5ITVJ?
KE-37 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nHRmlEPTB;MU[uPFExPyEQvF2= MoPDV2FPT0WU
LS-411N MmjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnsZoJKSzVyPUG3MlEyQCEQvF2= NH7yVHBUSU6JRWK=
NCI-H2228 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXYcoFKSzVyPUG3MlMxPzFizszN NVi2T4k3W0GQR1XS
SK-MEL-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTBTZhKSzVyPUG3MlQ6PjVizszN MX\TRW5ITVJ?
HN NXe5OJZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPYOZYyUUN3ME2xO{44OjR6IN88US=> NWXzeY9uW0GQR1XS
NCI-H1648 NEn2b4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTF5LkixPEDPxE1? NUjhV4ZoW0GQR1XS
IA-LM NE\YNHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrWUG1KSzVyPUG4MlMyPzJizszN NVzVN49bW0GQR1XS
EW-13 NG\yWIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTF6LkW3NFgh|ryP Mlj3V2FPT0WU
YKG-1 NFjXSIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTF7LkW3NVEh|ryP NWXJOWFZW0GQR1XS
KNS-81-FD NWDXTG9tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7QPYNKSzVyPUG5MlU5PThizszN MmHNV2FPT0WU
23132-87 MknQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXhUGtKSzVyPUG5Mlc3PDJizszN NFv0cY1USU6JRWK=
NUGC-3 NXezZYoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUC1OYtQUUN3ME2xPU46QDh5IN88US=> NH:0[4xUSU6JRWK=
5637 NV3ZXIRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\PTWlEPTB;MkCuNFQ4QCEQvF2= M{\OZnNCVkeHUh?=
NCI-H1755 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvzVoQ3UUN3ME2yNE41PzZ2IN88US=> M1:2U3NCVkeHUh?=
RH-18 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\RNWlEPTB;MkCuOVc1QCEQvF2= NU[3WFc1W0GQR1XS
RXF393 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknXTWM2OD1{MD62O|U3KM7:TR?= Mom3V2FPT0WU
LU-134-A NGHZb4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLkTWM2OD1{MD63NFU3KM7:TR?= NF3IS25USU6JRWK=
TE-12 M1mzU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTJyLkeyNFEh|ryP NFHKVIRUSU6JRWK=
MOLT-4 NVnZW3dMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXHTWM2OD1{MT6xPVE2KM7:TR?= NVfmPGdKW0GQR1XS
IGR-1 MnO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTJzLkO3PVYh|ryP M1PQU3NCVkeHUh?=
HOP-92 NYHyS4doT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTJzLkS5PFch|ryP Mk[3V2FPT0WU
SK-MES-1 NFfQSFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTJzLkezPFEh|ryP NUPK[5JlW0GQR1XS
LU-65 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTJzLki2NlQh|ryP M1zLfXNCVkeHUh?=
MS-1 NFnnXodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXMTWM2OD1{Mj6xNlA{KM7:TR?= MlPOV2FPT0WU
LoVo NYDjSVVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLZTWM2OD1{Mj6yOFQh|ryP NFHrc|VUSU6JRWK=
A704 MljKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnOZ2RZUUN3ME2yNk42OTV3IN88US=> NIPWOG5USU6JRWK=
HT-1376 MkK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTJ{Lk[wOVkh|ryP M1XOUHNCVkeHUh?=
IST-MEL1 NFXJTXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PGTGlEPTB;MkKuOlc2OSEQvF2= MWPTRW5ITVJ?
Ramos-2G6-4C10 NHrRTXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJ{LkezOlYh|ryP NHfQdnJUSU6JRWK=
T47D M4fXTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTJ{Lke5O|kh|ryP NIHiPGdUSU6JRWK=
HT-1197 NF3CeXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTJ|LkC4NVch|ryP MU\TRW5ITVJ?
LB2518-MEL MkTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\LUWlEPTB;MkOuOlQyOiEQvF2= MWXTRW5ITVJ?
J-RT3-T3-5 Mk\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7ufIRYUUN3ME2yOE44PTl3IN88US=> MY\TRW5ITVJ?
SK-NEP-1 NIDL[FRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTJ2Lki3OFQh|ryP MUfTRW5ITVJ?
NCI-H526 NX6xc3lpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknFTWM2OD1{NT6wNFI{KM7:TR?= M2jJ[3NCVkeHUh?=
IST-SL1 NFT5NlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTJ3LkK3OVEh|ryP M2fHVHNCVkeHUh?=
HH Mnn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3q4dWlEPTB;MkWuN|E6OiEQvF2= M{PsdHNCVkeHUh?=
NCI-H82 NVHHcItVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo[2TWM2OD1{NT65N|gh|ryP MnvPV2FPT0WU
SNU-449 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTJ5LkKwNVgh|ryP MULTRW5ITVJ?
COR-L23 MmXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJ5LkK4NVMh|ryP NILYeZpUSU6JRWK=
LOXIMVI M17QVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTJ5LkO2PEDPxE1? M{XkOXNCVkeHUh?=
GR-ST NHPUUpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkOyTWM2OD1{Nz62O|A3KM7:TR?= M{K4SXNCVkeHUh?=
NCI-SNU-1 Mmn6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XaSGlEPTB;MkeuPVQ1KM7:TR?= MnTRV2FPT0WU
ALL-PO NGm3e3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWK3OoVyUUN3ME2yPE4yPjB2IN88US=> MlHzV2FPT0WU
ML-2 NFGw[HBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX34NoxyUUN3ME2yPE4zQDF2IN88US=> NV7qbotvW0GQR1XS
HOP-62 Mn7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHj0UYdKSzVyPUK4MlcyOyEQvF2= MXTTRW5ITVJ?
EGI-1 NXLhcY1FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTH[HhyUUN3ME2yPE45QDR3IN88US=> MlrqV2FPT0WU
TCCSUP NVOyU48{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTJ6LkmyO|Ih|ryP MXnTRW5ITVJ?
LB996-RCC NWLxOHZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTJ7LkW2PFIh|ryP MYfTRW5ITVJ?
LCLC-97TM1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjxTWM2OD1|Mj6xPVY1KM7:TR?= NFzwSlhUSU6JRWK=
NCI-H1304 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;je2lEPTB;M{KuN|MxOSEQvF2= NH\0bG1USU6JRWK=
KP-N-YS MmjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfvS4d7UUN3ME2zNk42QTd|IN88US=> MVrTRW5ITVJ?
NCI-H1770 M4D0fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTN|LkG2OFgh|ryP MWDTRW5ITVJ?
EM-2 MoDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHaXpV7UUN3ME2zN{43PTB2IN88US=> NYPRc45YW0GQR1XS
ChaGo-K-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPa[5l2UUN3ME2zN{44OjN4IN88US=> M3H5UnNCVkeHUh?=
ACHN MoLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjSTWM2OD1|Mz64N|g2KM7:TR?= MXnTRW5ITVJ?
MN-60 M4O4V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETjXIFKSzVyPUOzMlg2PDRizszN NIq3[IhUSU6JRWK=
EW-18 MorqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPwUFhKSzVyPUOzMlg6PzFizszN MlLRV2FPT0WU
KGN Mk[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\VSnNKSzVyPUO1MlczQTJizszN Mo\VV2FPT0WU
U031 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTN3LkixN|Ih|ryP MYDTRW5ITVJ?
HMV-II NXPES|BPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTN4LkC3O|Qh|ryP NIfqXIpUSU6JRWK=
L-363 NIfBZWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnOyTWM2OD1|Nz62OFU2KM7:TR?= M362fnNCVkeHUh?=
NCI-H1155 MnvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjtZoZKSzVyPUO4MlAxOTVizszN NVfOeHBVW0GQR1XS
NCI-H1793 NU\UenJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo[2TWM2OD1|OD6xNFI3KM7:TR?= NFroXZpUSU6JRWK=
P30-OHK M2n2[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnLeJAzUUN3ME2zPE4yOzN{IN88US=> MXLTRW5ITVJ?
AN3-CA NXTx[lg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\MTWM2OD1|OD6xOlE2KM7:TR?= MX7TRW5ITVJ?
UACC-257 NIC1O2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHqTWM2OD1|OD63PUDPxE1? NFr4eWNUSU6JRWK=
MCF7 NF7IfINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPO[|RyUUN3ME2zPU45PjJ7IN88US=> NGXUUm5USU6JRWK=
KP-N-YN M4PMR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTRyLkSyPFUh|ryP M3jjbHNCVkeHUh?=
T98G M1f5fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nY[mlEPTB;NECuOFk2PyEQvF2= NETmZo1USU6JRWK=
HGC-27 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzwWW5KSzVyPUSzMlI4PCEQvF2= MVXTRW5ITVJ?
NCI-H1092 MlPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTR|LkK4PVUh|ryP NXXzbJRtW0GQR1XS
KARPAS-299 NF;HZ4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjvV3RKSzVyPUSzMlMxPzFizszN MWfTRW5ITVJ?
LB1047-RCC NFrGWYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTR2Lkm5OVkh|ryP NVzoUHBPW0GQR1XS
786-0 NIH3eI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zPOWlEPTB;NEWuOlUh|ryP M2H0XXNCVkeHUh?=
HCC2157 MmHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nJTWlEPTB;NE[uNFM2QSEQvF2= NH3CbFVUSU6JRWK=
NY Ml7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTR4LkG3O|gh|ryP MVHTRW5ITVJ?
EFM-19 NVj3THVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXG4d|Q6UUN3ME20Ok44PTN|IN88US=> NUeyendlW0GQR1XS
EW-16 M4HBd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETGWWRKSzVyPUS2Mlc5ODZizszN MVPTRW5ITVJ?
UM-UC-3 M{fyV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlryTWM2OD12Nj64NFU6KM7:TR?= NHjDPXFUSU6JRWK=
HT-29 M{HjRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvoSoxXUUN3ME20O{45Pzl{IN88US=> NHn2WZRUSU6JRWK=
LN-405 M3TKPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTR6LkC4Nlch|ryP NIH1UXFUSU6JRWK=
NCI-H727 NUHWb294T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TwdmlEPTB;NEiuO|czPiEQvF2= MVHTRW5ITVJ?
D-502MG NYL0RmJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rLXmlEPTB;NEiuPVY4PiEQvF2= MoT2V2FPT0WU
GMS-10 NInEUVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ry[mlEPTB;NEmuNlk4PCEQvF2= NXzs[lZvW0GQR1XS
MEL-JUSO NVfnc2t6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPFXmxKSzVyPUS5MlM1PyEQvF2= M1HDeXNCVkeHUh?=

... 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 slightly soluble or insoluble
Ethanol slightly soluble or 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
in solvent
Synonyms N/A

Bio Calculators

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID