PLX-4720

製品コードS1152

PLX-4720化学構造

分子量(MW):413.83

PLX-4720は一種の有効で、選択性的なB-RafV600E阻害剤で、無細胞試験でIC50値が13 nMですが、同時にc-Raf-1(Y340DとY341D突然変異型)に有効に作用して、B-RafV600Eに作用する選択性は野生型B-Rafに作用する選択性より10倍が高くなります。

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文献中の引用(46)

カスタマーフィードバック(9)

  • 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.

製品安全説明書

Raf阻害剤の選択性比較

生物活性

製品説明 PLX-4720は一種の有効で、選択性的なB-RafV600E阻害剤で、無細胞試験でIC50値が13 nMですが、同時にc-Raf-1(Y340DとY341D突然変異型)に有効に作用して、B-RafV600Eに作用する選択性は野生型B-Rafに作用する選択性より10倍が高くなります。
靶点
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試験

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 NVTWcW1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHNSFVjUUN3ME2wMlA4PDV5IN88US=> MUPTRW5ITVJ?
EoL-1-cell MmL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTBwMUSxOlYh|ryP Mk\hV2FPT0WU
C32 NUjU[FcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTBwMUWxN|Eh|ryP M4m0XnNCVkeHUh?=
M14 MnjpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTBwMkG3OVch|ryP NF\BdIJUSU6JRWK=
CP50-MEL-B NXjkdWd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1GwRmlEPTB;MD6yPVc5PCEQvF2= MXXTRW5ITVJ?
A101D MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvxTnJMUUN3ME2wMlMzPTh7IN88US=> NHTxdGpUSU6JRWK=
G-361 NUTubWU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3Dfo1KSzVyPUCuN|Q3OzdizszN NILvT|NUSU6JRWK=
HT-144 M{T0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnf5TWM2OD1yLkO2N|I6KM7:TR?= MU\TRW5ITVJ?
ACN NVPsN3pOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7FVHBKSzVyPUCuN|g1PzdizszN MoXhV2FPT0WU
COLO-829 NEDIOIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIO3coJKSzVyPUCuN|g6PjhizszN MWnTRW5ITVJ?
MEL-HO MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHQVHVKSzVyPUCuOFEyPzlizszN NHPuSWdUSU6JRWK=
SH-4 M{jsOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkH3TWM2OD1yLkSxOFIzKM7:TR?= MVTTRW5ITVJ?
SK-MEL-3 MmLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLGTWM2OD1yLkWxOVY5KM7:TR?= NX3TNGhnW0GQR1XS
A375 NF7FcWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTITWM2OD1yLk[3N|U6KM7:TR?= MX\TRW5ITVJ?
MMAC-SF MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYL2NoNFUUN3ME2wMlY5PjF2IN88US=> M3Lqc3NCVkeHUh?=
BHT-101 M3nPTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTBwN{C3NFIh|ryP M{L6VHNCVkeHUh?=
K5 Mn\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTBwN{[xOFgh|ryP Ml\mV2FPT0WU
BV-173 MlrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLN[pZJUUN3ME2wMlc6PjR2IN88US=> MYLTRW5ITVJ?
RVH-421 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H5XmlEPTB;MD64Olc6PiEQvF2= NXvEfndZW0GQR1XS
HCC2218 NYXCTW45T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M363fWlEPTB;MD64O|g1PCEQvF2= M2fuOHNCVkeHUh?=
WM-115 NWO5Spg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTBwOEi2PVIh|ryP NFfyPVJUSU6JRWK=
SK-MEL-28 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTFwMES1Olkh|ryP MWTTRW5ITVJ?
COLO-679 MmjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mke5TWM2OD1zLkGwOFY1KM7:TR?= MYDTRW5ITVJ?
MZ7-mel M2facmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXXVVZKSzVyPUGuNVQ6PjNizszN NF;jdppUSU6JRWK=
SK-MEL-30 M2rISGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrkeI1KSzVyPUGuN|M{QDZizszN Mk\EV2FPT0WU
NCI-H209 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnOVJB1UUN3ME2xMlYxQDZizszN NInI[YpUSU6JRWK=
HTC-C3 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHy4dYJKSzVyPUGuOlYzQTRizszN NIXjbnhUSU6JRWK=
KARPAS-45 Mn;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHkc|ZKSzVyPUKuNFQ6PzhizszN MYXTRW5ITVJ?
NCI-SNU-5 M{HzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTJwMUG5Olkh|ryP MljpV2FPT0WU
KP-4 NHjvV4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlH5TWM2OD1{LkOwO|g4KM7:TR?= NXrENG9UW0GQR1XS
PA-1 MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHCdJFKSzVyPUKuO|I3PzNizszN MUjTRW5ITVJ?
HuO-3N1 NUPwXlB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrCcYJKSzVyPUKuPFc6PDZizszN MW\TRW5ITVJ?
NCI-H358 MkK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfCSHRKSzVyPUKuPVIzOzJizszN MoDSV2FPT0WU
CTB-1 MnLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzrOVVKSzVyPUOuOFAyPzZizszN M1PITXNCVkeHUh?=
697 NE\yb|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XaZmlEPTB;Mz61OVI3PiEQvF2= NUTySGx1W0GQR1XS
CP66-MEL MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTRwMUW5Nlch|ryP MX7TRW5ITVJ?
NB13 NEHPfIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjZUlFKSzVyPUSuOFkyPzlizszN NHvReJFUSU6JRWK=
DBTRG-05MG NXXOZ5JLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELXVYlKSzVyPUSuOVM{OjVizszN NXP4fXlpW0GQR1XS
A2058 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7pTnVKSzVyPUSuO|IyPjRizszN MU\TRW5ITVJ?
KG-1 M13ZNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2W4RWlEPTB;ND63N|kxQCEQvF2= NIjFe4VUSU6JRWK=
8305C NFvicpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PzSGlEPTB;NT6xPFc{KM7:TR?= M3zyVHNCVkeHUh?=
RPMI-7951 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfIPFhZUUN3ME21MlgxOjh|IN88US=> NF;TUmtUSU6JRWK=
CHL-1 MlHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTVwOUe2NFMh|ryP M{HNb3NCVkeHUh?=
TI-73 M1TGNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XwdmlEPTB;Nj6wNFkxOiEQvF2= MXjTRW5ITVJ?
HT-1080 NF36Ro1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLxeVdvUUN3ME22MlExQTR4IN88US=> M1K1VnNCVkeHUh?=
ES5 NFnxS4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTZwMUS5NlQh|ryP NGjPVIdUSU6JRWK=
8-MG-BA MmfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTZwMUixNlkh|ryP NVHvdoE1W0GQR1XS
NB7 MnGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnuxTWM2OD14LkKxN|c{KM7:TR?= NF\HTXhUSU6JRWK=
H4 Ml\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\kdmlEPTB;Nj6yNlQ6OyEQvF2= M{ntVnNCVkeHUh?=
CAL-72 M3Hrfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nvdGlEPTB;Nj60OVQzOyEQvF2= NXnpXnFRW0GQR1XS
HCC1806 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPkTWM2OD14LkixPVMyKM7:TR?= Mo\1V2FPT0WU
BCPAP M1jjNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrOSFdrUUN3ME23MlIyPzZ2IN88US=> MmfXV2FPT0WU
LB2241-RCC MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;0NGlEPTB;Nz6zOlkxPyEQvF2= MUjTRW5ITVJ?
COLO-741 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnH[JhKSzVyPUiuNFE3PzlizszN MoDHV2FPT0WU
HSC-3 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHCb4xKSzVyPUiuNFcxPjhizszN NHj3XmVUSU6JRWK=
SW982 M2DTW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;KUGlEPTB;OD60NVUyPiEQvF2= NXe0SlVbW0GQR1XS
GCT NETpcotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;UTWM2OD16Lke1N|E1KM7:TR?= M1exWXNCVkeHUh?=
KY821 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v0fGlEPTB;OT6wOVE4QCEQvF2= NF72T2VUSU6JRWK=
JVM-3 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlK2TWM2OD17LkW2PVk6KM7:TR?= Ml\vV2FPT0WU
RS4-11 M4D2b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE[2ZZlKSzVyPUmuOlA1QCEQvF2= M{LDTXNCVkeHUh?=
VA-ES-BJ MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkj3TWM2OD1zMD6wNVQ6KM7:TR?= MkH1V2FPT0WU
A431 M2m1Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\MZ2lEPTB;MUCuOFIyOiEQvF2= MmL5V2FPT0WU
LXF-289 M4D5bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;JTWM2OD1zMD60OVgh|ryP NUPPc2M3W0GQR1XS
SK-MEL-24 MnLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{juNmlEPTB;MUCuPFI4PCEQvF2= MmPmV2FPT0WU
NOS-1 MmLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPsTWM2OD1zMD64OFczKM7:TR?= NXfmV5M1W0GQR1XS
KNS-62 NUnaNWhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LGSGlEPTB;MUGuNlQxPCEQvF2= NXfFfJlFW0GQR1XS
SK-HEP-1 NGDpbGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTuOHNRUUN3ME2xNU4{PTJ5IN88US=> Mn6xV2FPT0WU
A3-KAW NH\Bb21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jYbGlEPTB;MUGuO|E4QCEQvF2= NH;TS2hUSU6JRWK=
SK-LU-1 NXfPcFJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVGwXGVEUUN3ME2xNk4zPjV3IN88US=> M{nONHNCVkeHUh?=
TYK-nu MoHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTF{LkO5N|Ih|ryP NHHRN|FUSU6JRWK=
NMC-G1 NV20ZXRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHH0UlNKSzVyPUGyMlYxPjJizszN NILPO2FUSU6JRWK=
BB65-RCC NVPhVFUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfUTWM2OD1zMj63NVY6KM7:TR?= MlXKV2FPT0WU
QIMR-WIL NITlSY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTpUpAyUUN3ME2xNk45QDN|IN88US=> MWLTRW5ITVJ?
D-566MG NWXHWpcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPVW2t[UUN3ME2xN{46PTd4IN88US=> MUnTRW5ITVJ?
KYSE-140 NXTVTI9WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTF2LkC3OVMh|ryP M3TWOXNCVkeHUh?=
SCC-4 M{jHNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTF2LkOzOVkh|ryP MVjTRW5ITVJ?
U251 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTF2Lki0PVIh|ryP NVPERmFrW0GQR1XS
D-542MG NYD1PYx6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HrWWlEPTB;MUSuPVIzOiEQvF2= MWnTRW5ITVJ?
LAMA-84 NXTSXphsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rQVmlEPTB;MUSuPVk{OiEQvF2= M1\JZ3NCVkeHUh?=
NCI-H720 NVfkcos5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrDTWM2OD1zNT6yOlg1KM7:TR?= NHXyWWZUSU6JRWK=
DEL M2jiOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmC4TWM2OD1zNT60Nlk{KM7:TR?= NITJb|JUSU6JRWK=
SBC-1 NHLK[oNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjYTWM2OD1zNT60N|A2KM7:TR?= MV\TRW5ITVJ?
ECC10 Ml;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofoTWM2OD1zNT60OFU5KM7:TR?= MoizV2FPT0WU
Daoy NIjnW5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXzTWM2OD1zNT63OlE3KM7:TR?= MnTqV2FPT0WU
SCH Mk\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;KVotMUUN3ME2xOU44QDN3IN88US=> MV7TRW5ITVJ?
MZ2-MEL NV3ne5BVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fINmlEPTB;MU[uNFY1PiEQvF2= M1XqVnNCVkeHUh?=
CAL-12T MlrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTF4LkS4OlIh|ryP NUXIeGtuW0GQR1XS
KE-37 NVvKOok5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmraTWM2OD1zNj64NVA4KM7:TR?= NED0e4pUSU6JRWK=
LS-411N MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHq2Z5ZKSzVyPUG3MlEyQCEQvF2= MnT2V2FPT0WU
NCI-H2228 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFqzU49KSzVyPUG3MlMxPzFizszN MnTuV2FPT0WU
SK-MEL-2 M4Xkemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITscZpKSzVyPUG3MlQ6PjVizszN NGmwVppUSU6JRWK=
HN M3LieGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPEW|lKSzVyPUG3MlczPDhizszN NHKyTXdUSU6JRWK=
NCI-H1648 M1;PZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTF5LkixPEDPxE1? NYrLU2hRW0GQR1XS
IA-LM M{njTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\NRopKSzVyPUG4MlMyPzJizszN M{fMVnNCVkeHUh?=
EW-13 NFnTNllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTF6LkW3NFgh|ryP NYXw[HVDW0GQR1XS
YKG-1 NVXlRolMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TUUmlEPTB;MUmuOVcyOSEQvF2= NYTh[XJbW0GQR1XS
KNS-81-FD NEfzWpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\qTWM2OD1zOT61PFU5KM7:TR?= NF3wS|VUSU6JRWK=
23132-87 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlS2TWM2OD1zOT63OlQzKM7:TR?= MWLTRW5ITVJ?
NUGC-3 NXLRb3VJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrEd4pxUUN3ME2xPU46QDh5IN88US=> M2PteXNCVkeHUh?=
5637 NXPaXpVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvWTWM2OD1{MD6wOFc5KM7:TR?= MXXTRW5ITVJ?
NCI-H1755 NVLzdIJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTJyLkS3OlQh|ryP NVjpR5dVW0GQR1XS
RH-18 NHvtO4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHTVHhZUUN3ME2yNE42PzR6IN88US=> M4\XSHNCVkeHUh?=
RXF393 MnXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIryeoRKSzVyPUKwMlY4PTZizszN NVjGXWRbW0GQR1XS
LU-134-A M{PFfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTJyLkewOVYh|ryP NWTy[oNQW0GQR1XS
TE-12 NF7peZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDifZpWUUN3ME2yNE44OjBzIN88US=> M1HMTnNCVkeHUh?=
MOLT-4 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTJzLkG5NVUh|ryP NGjUfodUSU6JRWK=
IGR-1 NGP0T25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTJzLkO3PVYh|ryP NYHqd4lGW0GQR1XS
HOP-92 NHrwT|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zN[2lEPTB;MkGuOFk5PyEQvF2= NV7Ne|RQW0GQR1XS
SK-MES-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjEb|dKSzVyPUKxMlc{QDFizszN M2L4NnNCVkeHUh?=
LU-65 MoPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfPeIxKSzVyPUKxMlg3OjRizszN NGrobGVUSU6JRWK=
MS-1 MonKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnkUWNVUUN3ME2yNk4yOjB|IN88US=> MVPTRW5ITVJ?
LoVo MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTJ{LkK0OEDPxE1? Ml3pV2FPT0WU
A704 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHPU49KSzVyPUKyMlUyPTVizszN NHXFd4RUSU6JRWK=
HT-1376 NETjXYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPRWVBKSzVyPUKyMlYxPTlizszN MlTVV2FPT0WU
IST-MEL1 MmfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHZTWM2OD1{Mj62O|UyKM7:TR?= MWHTRW5ITVJ?
Ramos-2G6-4C10 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDO[45KSzVyPUKyMlc{PjZizszN M1nLfnNCVkeHUh?=
T47D NFHrR41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTJ{Lke5O|kh|ryP MoLGV2FPT0WU
HT-1197 M4PCV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXZOW5KSzVyPUKzMlA5OTdizszN MVLTRW5ITVJ?
LB2518-MEL NUTp[HI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zOfGlEPTB;MkOuOlQyOiEQvF2= MlXHV2FPT0WU
J-RT3-T3-5 NVjlUYdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHkUYhKSzVyPUK0Mlc2QTVizszN NIrnR4VUSU6JRWK=
SK-NEP-1 NHrDSIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjGcZpMUUN3ME2yOE45PzR2IN88US=> MoCzV2FPT0WU
NCI-H526 M4HaW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWS4O4lEUUN3ME2yOU4xODJ|IN88US=> M1jrenNCVkeHUh?=
IST-SL1 M4L3Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jFfmlEPTB;MkWuNlc2OSEQvF2= MV3TRW5ITVJ?
HH NEXQRWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYS1SGpPUUN3ME2yOU4{OTl{IN88US=> MlXSV2FPT0WU
NCI-H82 MlTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2H6N2lEPTB;MkWuPVM5KM7:TR?= Ml7xV2FPT0WU
SNU-449 M3\6XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPOU3FUUUN3ME2yO{4zODF6IN88US=> MUfTRW5ITVJ?
COR-L23 NFLEXXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXMVItKSzVyPUK3MlI5OTNizszN M4HLN3NCVkeHUh?=
LOXIMVI M4W2d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\tT2FKSzVyPUK3MlM3QCEQvF2= NYHBTGJpW0GQR1XS
GR-ST MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrUPXlKSzVyPUK3MlY4ODZizszN Ml\zV2FPT0WU
NCI-SNU-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;6W|V6UUN3ME2yO{46PDRizszN Mn7mV2FPT0WU
ALL-PO M1TQT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTJ6LkG2NFQh|ryP MWXTRW5ITVJ?
ML-2 NI\0c4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvoOFBKSzVyPUK4MlI5OTRizszN M1PifXNCVkeHUh?=
HOP-62 NITPPFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13rSGlEPTB;MkiuO|E{KM7:TR?= MlLtV2FPT0WU
EGI-1 MofUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXGTWM2OD1{OD64PFQ2KM7:TR?= MkDKV2FPT0WU
TCCSUP M3;SUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPtTWM2OD1{OD65NlczKM7:TR?= MlTKV2FPT0WU
LB996-RCC MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJ7LkW2PFIh|ryP NUL1OIN1W0GQR1XS
LCLC-97TM1 Mn;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnGWYZKSzVyPUOyMlE6PjRizszN M4X0dXNCVkeHUh?=
NCI-H1304 MlvSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXuxdY1qUUN3ME2zNk4{OzBzIN88US=> MmTVV2FPT0WU
KP-N-YS M{TNZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTN{LkW5O|Mh|ryP NVjib|E2W0GQR1XS
NCI-H1770 M2LLUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTN|LkG2OFgh|ryP M{n5bnNCVkeHUh?=
EM-2 NXu5T412T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3P2VWlEPTB;M{OuOlUxPCEQvF2= MXfTRW5ITVJ?
ChaGo-K-1 M{jqcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPW[FBKSzVyPUOzMlczOzZizszN MV3TRW5ITVJ?
ACHN NF3Ze4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjUUWdKSzVyPUOzMlg{QDVizszN M4r6UHNCVkeHUh?=
MN-60 NWnpWVNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE[5cIlKSzVyPUOzMlg2PDRizszN NVezbpM5W0GQR1XS
EW-18 NGrNbmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NES0N3FKSzVyPUOzMlg6PzFizszN NFPt[IlUSU6JRWK=
KGN MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTN3LkeyPVIh|ryP NYLhbnlpW0GQR1XS
U031 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrScoN{UUN3ME2zOU45OTN{IN88US=> NV3r[nlkW0GQR1XS
HMV-II Ml\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITCXHBKSzVyPUO2MlA4PzRizszN M1jrNnNCVkeHUh?=
L-363 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUT2c41pUUN3ME2zO{43PDV3IN88US=> MnSxV2FPT0WU
NCI-H1155 NHu1O5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LOPWlEPTB;M{iuNFAyPSEQvF2= NU\XeYdjW0GQR1XS
NCI-H1793 NHezb3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDBPFlKSzVyPUO4MlExOjZizszN MWPTRW5ITVJ?
P30-OHK Mlu3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVr3W3NYUUN3ME2zPE4yOzN{IN88US=> MUDTRW5ITVJ?
AN3-CA NF;QW3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTN6LkG2NVUh|ryP MYfTRW5ITVJ?
UACC-257 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTN6Lke5JO69VQ>? NYT1ZVdzW0GQR1XS
MCF7 M4S3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHFOWlQUUN3ME2zPU45PjJ7IN88US=> M1HMTHNCVkeHUh?=
KP-N-YN NViyNZZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWC4Z|JSUUN3ME20NE41Ojh3IN88US=> NEm2[3BUSU6JRWK=
T98G NYrMO49NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXP2Xm9uUUN3ME20NE41QTV5IN88US=> MoL0V2FPT0WU
HGC-27 MoO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGT6V2pKSzVyPUSzMlI4PCEQvF2= M{ixb3NCVkeHUh?=
NCI-H1092 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH30UIRKSzVyPUSzMlI5QTVizszN M3nxdXNCVkeHUh?=
KARPAS-299 M4nQOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFS4R5NKSzVyPUSzMlMxPzFizszN NYO1eXIxW0GQR1XS
LB1047-RCC M3S4cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWKydJFoUUN3ME20OE46QTV7IN88US=> M3jm[nNCVkeHUh?=
786-0 M2\oXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXvUZZnUUN3ME20OU43PSEQvF2= MXHTRW5ITVJ?
HCC2157 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTR4LkCzOVkh|ryP MmP6V2FPT0WU
NY M2LIXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;JNWRKSzVyPUS2MlE4PzhizszN M2j5VXNCVkeHUh?=
EFM-19 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorCTWM2OD12Nj63OVM{KM7:TR?= NFG3[ItUSU6JRWK=
EW-16 NXLGN282T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PuWGlEPTB;NE[uO|gxPiEQvF2= NUP2dI0zW0GQR1XS
UM-UC-3 M2jZUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTR4LkiwOVkh|ryP MlrVV2FPT0WU
HT-29 M1rVeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3q2Z2lEPTB;NEeuPFc6OiEQvF2= MVPTRW5ITVJ?
LN-405 MnvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LCTWlEPTB;NEiuNFgzPyEQvF2= M{e1V3NCVkeHUh?=
NCI-H727 NIWxTWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\0b41KSzVyPUS4Mlc4OjZizszN MX;TRW5ITVJ?
D-502MG M4Tmd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfiRVZzUUN3ME20PE46Pjd4IN88US=> M37FW3NCVkeHUh?=
GMS-10 M1zIOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mni1TWM2OD12OT6yPVc1KM7:TR?= NWLnTHFDW0GQR1XS
MEL-JUSO MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXGwS2RIUUN3ME20PU4{PDdizszN M4[x[3NCVkeHUh?=

... Click to View More Cell Line Experimental Data

In vivo試験 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]

プロトコル(参考用のみ)

キナーゼアッセイ:[1]
+ 展開

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.
細胞アッセイ: [1]
+ 展開
  • 細胞株: COLO205, A375, WM2664, COLO829, HT716, SW620, H460, Calu-6, HCT116, SK-MEL2, SK-MEL3, Lovo, H1299, 1205Lu, and C8161 cells
  • 濃度: Dissolved in DMSO, final concentrations ~1 mM
  • 反応時間: 24, 48, and 72 hours
  • 実験の流れ: 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.
    (参考用のみ)
動物実験:[1]
+ 展開
  • 動物モデル: Female athymic mice (NCr nu/nu) implanted s.c. with COLO205 cells, and SCID mice with 1205Lu or C8161 cells
  • 製剤: Suspended in vehicle (5% DMSO, 1% methylcellulose)
  • 投薬量: 5, 20, or 100 mg/kg
  • 投与方法: Oral gavage once or twice daily
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 83 mg/mL (200.56 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
体内 2% DMSO+50% PEG 300+5% Tween 80+ddH2O 5mg/mL

* <1 mg/mlは製品が微弱に溶解する或いは溶解しないことを示します。
* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 413.83
化学式

C17H14ClF2N3O3S

CAS No. 918505-84-7
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題1:

    What would you recommend to make working solution for intraperitoneal injection into mice?

  • 回答:

    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信号経路図

Raf Inhibitors with Unique Features

相関Raf製品

Tags: PLX-4720を買う | PLX-4720 ic50 | PLX-4720供給者 | PLX-4720を購入する | PLX-4720費用 | PLX-4720生産者 | オーダーPLX-4720 | PLX-4720化学構造 | PLX-4720分子量 | PLX-4720代理店
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID