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。

サイズ 価格(税別)  
JPY 25896.00
JPY 19920.00
JPY 44820.00
JPY 111220.00

文献中の使用例(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。
ターゲット
C-Raf-1 (Y340D/Y341D) [1]
(Cell-free assay)
B-Raf (V600E) [1]
(Cell-free assay)
BRK [1]
(Cell-free assay)
B-Raf [1]
(Cell-free assay)
6.7 nM 13 nM 130 nM 160 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DU-4475 NVjYOJE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTBwMEe0OVch|ryP MV3TRW5ITVJ?
EoL-1-cell NGXrVHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTBwMUSxOlYh|ryP M3[yXnNCVkeHUh?=
C32 NF7DUG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLDTWM2OD1yLkG1NVMyKM7:TR?= NWHj[WIxW0GQR1XS
M14 NIPvXJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjtTWM2OD1yLkKxO|U4KM7:TR?= MWjTRW5ITVJ?
CP50-MEL-B MoH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7YTYtJUUN3ME2wMlI6Pzh2IN88US=> NHm1O3VUSU6JRWK=
A101D NUDSOJpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnT6TWM2OD1yLkOyOVg6KM7:TR?= NFHYeGhUSU6JRWK=
G-361 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{T6VWlEPTB;MD6zOFY{PyEQvF2= NEeyeY5USU6JRWK=
HT-144 MmXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLvOZZKSzVyPUCuN|Y{OjlizszN MVXTRW5ITVJ?
ACN M1jiOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1m4NmlEPTB;MD6zPFQ4PyEQvF2= MmHMV2FPT0WU
COLO-829 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zXcGlEPTB;MD6zPFk3QCEQvF2= NYP2SI5FW0GQR1XS
MEL-HO MlHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NED2UnhKSzVyPUCuOFEyPzlizszN NWPxWmlVW0GQR1XS
SH-4 NFyzcnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwNEG0NlIh|ryP NFTkSIJUSU6JRWK=
SK-MEL-3 NFPLT2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\DT2lEPTB;MD61NVU3QCEQvF2= Mnm5V2FPT0WU
A375 NXW5WVZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTBwNkezOVkh|ryP MkHtV2FPT0WU
MMAC-SF MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;MTWM2OD1yLk[4OlE1KM7:TR?= MVvTRW5ITVJ?
BHT-101 NGfFSIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvSbWxKSzVyPUCuO|A4ODJizszN M3HpU3NCVkeHUh?=
K5 NGi2PI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTBwN{[xOFgh|ryP NWDGNpRnW0GQR1XS
BV-173 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHS2fmRKSzVyPUCuO|k3PDRizszN M2nWXXNCVkeHUh?=
RVH-421 MmXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rkOWlEPTB;MD64Olc6PiEQvF2= NYO3fW9oW0GQR1XS
HCC2218 M1XoTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXLdG5LUUN3ME2wMlg4QDR2IN88US=> NGG0dlBUSU6JRWK=
WM-115 NGLrTpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPtTWM2OD1yLki4OlkzKM7:TR?= MYHTRW5ITVJ?
SK-MEL-28 NHLTdllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTNcpJVUUN3ME2xMlA1PTZ7IN88US=> NX7nTm5bW0GQR1XS
COLO-679 NVPLOGtyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkX5TWM2OD1zLkGwOFY1KM7:TR?= NWDUPJBFW0GQR1XS
MZ7-mel NVnNW2lJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILvfJNKSzVyPUGuNVQ6PjNizszN NYn3XZFHW0GQR1XS
SK-MEL-30 M3\VNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1y3eGlEPTB;MT6zN|M5PiEQvF2= MnTXV2FPT0WU
NCI-H209 MkSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWO4SVRoUUN3ME2xMlYxQDZizszN MorFV2FPT0WU
HTC-C3 M33HW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2qzfGlEPTB;MT62OlI6PCEQvF2= MYrTRW5ITVJ?
KARPAS-45 NHuzXVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYKyb4piUUN3ME2yMlA1QTd6IN88US=> MkLHV2FPT0WU
NCI-SNU-5 NFf6OopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LPTWlEPTB;Mj6xNVk3QSEQvF2= NHPRUmRUSU6JRWK=
KP-4 NYXtdphWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17MdGlEPTB;Mj6zNFc5PyEQvF2= MYfTRW5ITVJ?
PA-1 MnnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTJwN{K2O|Mh|ryP M4OxNXNCVkeHUh?=
HuO-3N1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjuU5dKSzVyPUKuPFc6PDZizszN MULTRW5ITVJ?
NCI-H358 NF\FfXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV74WZAyUUN3ME2yMlkzOjN{IN88US=> MorBV2FPT0WU
CTB-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHhdlBKSzVyPUOuOFAyPzZizszN MWDTRW5ITVJ?
697 MmLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2frWmlEPTB;Mz61OVI3PiEQvF2= MmjkV2FPT0WU
CP66-MEL NYj5PZVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTRwMUW5Nlch|ryP M4rVfHNCVkeHUh?=
NB13 MlnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jlSGlEPTB;ND60PVE4QSEQvF2= NYHXVGRMW0GQR1XS
DBTRG-05MG M4TjZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\BTWM2OD12LkWzN|I2KM7:TR?= NIX0empUSU6JRWK=
A2058 NWTF[VEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TESWlEPTB;ND63NlE3PCEQvF2= M1nnU3NCVkeHUh?=
KG-1 M3Hyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXRTWM2OD12LkezPVA5KM7:TR?= NWHpfWk2W0GQR1XS
8305C MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTVwMUi3N{DPxE1? MoLzV2FPT0WU
RPMI-7951 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTVwOECyPFMh|ryP NYfuPVB4W0GQR1XS
CHL-1 MnzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTVwOUe2NFMh|ryP M4LqSXNCVkeHUh?=
TI-73 M1LjO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\GZYVKSzVyPU[uNFA6ODJizszN MXHTRW5ITVJ?
HT-1080 MoXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTHSpNKSzVyPU[uNVA6PDZizszN NEjsR25USU6JRWK=
ES5 NVm0XnhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmm3TWM2OD14LkG0PVI1KM7:TR?= NWPXZoh4W0GQR1XS
8-MG-BA M1;1[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTZwMUixNlkh|ryP M372XHNCVkeHUh?=
NB7 NHnpWlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTZwMkGzO|Mh|ryP NV7MRlZ{W0GQR1XS
H4 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlOyTWM2OD14LkKyOFk{KM7:TR?= MlLJV2FPT0WU
CAL-72 NHj5dmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXjdmZmUUN3ME22MlQ2PDJ|IN88US=> Mkm2V2FPT0WU
HCC1806 NWDHcY1rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nVO2lEPTB;Nj64NVk{OSEQvF2= NHLUeoxUSU6JRWK=
BCPAP NH3kWm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDqUXpKSzVyPUeuNlE4PjRizszN NV7sW|U6W0GQR1XS
LB2241-RCC NELncXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPVbIpKSzVyPUeuN|Y6ODdizszN Mk\vV2FPT0WU
COLO-741 MorxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3frTmlEPTB;OD6wNVY4QSEQvF2= M{HvVHNCVkeHUh?=
HSC-3 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRThwMEewOlgh|ryP NIXPPGVUSU6JRWK=
SW982 MoTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ToN2lEPTB;OD60NVUyPiEQvF2= M3LE[3NCVkeHUh?=
GCT NVzyfmZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfDTWM2OD16Lke1N|E1KM7:TR?= MlLpV2FPT0WU
KY821 MleyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfoTWM2OD17LkC1NVc5KM7:TR?= NUjURZlMW0GQR1XS
JVM-3 MnHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnYTWM2OD17LkW2PVk6KM7:TR?= MUXTRW5ITVJ?
RS4-11 MmnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnGVlZ2UUN3ME25MlYxPDhizszN M2C3eHNCVkeHUh?=
VA-ES-BJ M2T1WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTFyLkCxOFkh|ryP NVLjZZpWW0GQR1XS
A431 M1\4dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTFyLkSyNVIh|ryP M4HxcXNCVkeHUh?=
LXF-289 NX7tXWZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jHSGlEPTB;MUCuOFU5KM7:TR?= NGHIXHBUSU6JRWK=
SK-MEL-24 NYjKTotkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTFyLkiyO|Qh|ryP M{fRSXNCVkeHUh?=
NOS-1 NYTXZoM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfzbnhbUUN3ME2xNE45PDd{IN88US=> NG\sbXVUSU6JRWK=
KNS-62 NUfHTHVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHrTWM2OD1zMT6yOFA1KM7:TR?= MXzTRW5ITVJ?
SK-HEP-1 M322bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zlWmlEPTB;MUGuN|UzPyEQvF2= MkXPV2FPT0WU
A3-KAW NYDSNIpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTFzLkexO|gh|ryP M1vSXXNCVkeHUh?=
SK-LU-1 M{jCR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn1OIFbUUN3ME2xNk4zPjV3IN88US=> MlrKV2FPT0WU
TYK-nu NFjQfXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\Tb4VKSzVyPUGyMlM6OzJizszN NEH5[GlUSU6JRWK=
NMC-G1 MlLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnoTVhKSzVyPUGyMlYxPjJizszN MXPTRW5ITVJ?
BB65-RCC M{GyZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfuTmVSUUN3ME2xNk44OTZ7IN88US=> MmPQV2FPT0WU
QIMR-WIL M2fYb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTF{Lki4N|Mh|ryP NIHySlBUSU6JRWK=
D-566MG MmnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEWyfnFKSzVyPUGzMlk2PzZizszN NFjscXlUSU6JRWK=
KYSE-140 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HKbGlEPTB;MUSuNFc2OyEQvF2= NWfPfJRRW0GQR1XS
SCC-4 NYHLVmpDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTF2LkOzOVkh|ryP Mnr4V2FPT0WU
U251 NIXMS|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDTTWM2OD1zND64OFkzKM7:TR?= Ml;CV2FPT0WU
D-542MG MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fXZ2lEPTB;MUSuPVIzOiEQvF2= NIjzc4dUSU6JRWK=
LAMA-84 NH;IbIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\0TWM2OD1zND65PVMzKM7:TR?= NG[yWoNUSU6JRWK=
NCI-H720 NFnYPHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TUOGlEPTB;MUWuNlY5PCEQvF2= MVPTRW5ITVJ?
DEL Ml;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWi4T4t[UUN3ME2xOU41Ojl|IN88US=> NITWZoNUSU6JRWK=
SBC-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4ixdWlEPTB;MUWuOFMxPSEQvF2= NH7XPFBUSU6JRWK=
ECC10 M2f4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\BTWM2OD1zNT60OFU5KM7:TR?= NGPobJdUSU6JRWK=
Daoy MnvDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXwTWM2OD1zNT63OlE3KM7:TR?= MX7TRW5ITVJ?
SCH NH7EfGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITQbHVKSzVyPUG1Mlc5OzVizszN MVTTRW5ITVJ?
MZ2-MEL M{PLd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlf1TWM2OD1zNj6wOlQ3KM7:TR?= M1nMcHNCVkeHUh?=
CAL-12T MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jWc2lEPTB;MU[uOFg3OiEQvF2= MX7TRW5ITVJ?
KE-37 MnjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml31TWM2OD1zNj64NVA4KM7:TR?= MYPTRW5ITVJ?
LS-411N NEXM[3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rL[WlEPTB;MUeuNVE5KM7:TR?= NFzkW3JUSU6JRWK=
NCI-H2228 M2jmTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTF5LkOwO|Eh|ryP MlTQV2FPT0WU
SK-MEL-2 M1TDe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTF5LkS5OlUh|ryP MUfTRW5ITVJ?
HN MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LydmlEPTB;MUeuO|I1QCEQvF2= NUjFXYZCW0GQR1XS
NCI-H1648 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrER2pKSzVyPUG3MlgyQCEQvF2= MlHjV2FPT0WU
IA-LM M4TzdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn31TWM2OD1zOD6zNVczKM7:TR?= Moi3V2FPT0WU
EW-13 NVXXcIoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTF6LkW3NFgh|ryP NX7vZ2xXW0GQR1XS
YKG-1 M2TsNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTF7LkW3NVEh|ryP NYi3R3ZuW0GQR1XS
KNS-81-FD M1nJOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfjbFY4UUN3ME2xPU42QDV6IN88US=> MonrV2FPT0WU
23132-87 Mmf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTF7Lke2OFIh|ryP NG\R[WVUSU6JRWK=
NUGC-3 M4ntfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXVTWM2OD1zOT65PFg4KM7:TR?= NUXQbm5XW0GQR1XS
5637 MojJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX64UZM{UUN3ME2yNE4xPDd6IN88US=> NX3L[GN7W0GQR1XS
NCI-H1755 MoX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TXXGlEPTB;MkCuOFc3PCEQvF2= NVXpTY03W0GQR1XS
RH-18 MoH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT1fppKSzVyPUKwMlU4PDhizszN NUHJUoxIW0GQR1XS
RXF393 MorzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTJyLk[3OVYh|ryP NUjZNm9[W0GQR1XS
LU-134-A M3XvZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWD6botIUUN3ME2yNE44ODV4IN88US=> MkLYV2FPT0WU
TE-12 Mn7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXGTWM2OD1{MD63NlAyKM7:TR?= NYP3ZXRLW0GQR1XS
MOLT-4 M3G3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTk[|BKSzVyPUKxMlE6OTVizszN NGPD[WNUSU6JRWK=
IGR-1 NVT2NpBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vx[GlEPTB;MkGuN|c6PiEQvF2= M2L6[XNCVkeHUh?=
HOP-92 Mkf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnZTWM2OD1{MT60PVg4KM7:TR?= Moi4V2FPT0WU
SK-MES-1 NFXGWG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrsWGRrUUN3ME2yNU44OzhzIN88US=> NXr1S5J7W0GQR1XS
LU-65 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfiTYVRUUN3ME2yNU45PjJ2IN88US=> Mkf4V2FPT0WU
MS-1 MoHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTJ{LkGyNFMh|ryP NI\6NFZUSU6JRWK=
LoVo MorWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjxTohKSzVyPUKyMlI1PCEQvF2= MVHTRW5ITVJ?
A704 MoHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDaNG9KSzVyPUKyMlUyPTVizszN M1nRU3NCVkeHUh?=
HT-1376 M2DUZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrFNVRRUUN3ME2yNk43ODV7IN88US=> NHn3VotUSU6JRWK=
IST-MEL1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PkT2lEPTB;MkKuOlc2OSEQvF2= MkHhV2FPT0WU
Ramos-2G6-4C10 M{\SfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fkfWlEPTB;MkKuO|M3PiEQvF2= Ml7UV2FPT0WU
T47D M{nlVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrOTWM2OD1{Mj63PVc6KM7:TR?= NGWw[odUSU6JRWK=
HT-1197 MoXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJ|LkC4NVch|ryP M4X0bnNCVkeHUh?=
LB2518-MEL MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NECyeVdKSzVyPUKzMlY1OTJizszN NVvBWXllW0GQR1XS
J-RT3-T3-5 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLVTWM2OD1{ND63OVk2KM7:TR?= MoTSV2FPT0WU
SK-NEP-1 M1vMVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTJ2Lki3OFQh|ryP MnHaV2FPT0WU
NCI-H526 Ml\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DwbGlEPTB;MkWuNFAzOyEQvF2= NWTUWpN{W0GQR1XS
IST-SL1 NXHDN2JXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTJ3LkK3OVEh|ryP MWLTRW5ITVJ?
HH NX3YUlVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnyOJYzUUN3ME2yOU4{OTl{IN88US=> NE\vUWxUSU6JRWK=
NCI-H82 M4foVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4naWWlEPTB;MkWuPVM5KM7:TR?= M1jtNXNCVkeHUh?=
SNU-449 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTJ5LkKwNVgh|ryP NXTSeYt4W0GQR1XS
COR-L23 NETLVGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\ZTWM2OD1{Nz6yPFE{KM7:TR?= NV3ESJdXW0GQR1XS
LOXIMVI NYnqVXdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTJ5LkO2PEDPxE1? M2TpSXNCVkeHUh?=
GR-ST NVrFcZJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3hdI9DUUN3ME2yO{43PzB4IN88US=> MXPTRW5ITVJ?
NCI-SNU-1 NGDY[GZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTnTWM2OD1{Nz65OFQh|ryP MVzTRW5ITVJ?
ALL-PO MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrDTWM2OD1{OD6xOlA1KM7:TR?= MYfTRW5ITVJ?
ML-2 NYXzZWJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH32W25KSzVyPUK4MlI5OTRizszN MWrTRW5ITVJ?
HOP-62 M3PacGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLYbJNkUUN3ME2yPE44OTNizszN MnjiV2FPT0WU
EGI-1 M1HvOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkKxTWM2OD1{OD64PFQ2KM7:TR?= NV;zWpUyW0GQR1XS
TCCSUP NYDxOINHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LtcWlEPTB;MkiuPVI4OiEQvF2= MY\TRW5ITVJ?
LB996-RCC MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2OzSGlEPTB;MkmuOVY5OiEQvF2= NY\ETGRlW0GQR1XS
LCLC-97TM1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TOTWlEPTB;M{KuNVk3PCEQvF2= Mm\wV2FPT0WU
NCI-H1304 NGO3WnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTN{LkOzNFEh|ryP NFW2NWFUSU6JRWK=
KP-N-YS M2rmTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17xSmlEPTB;M{KuOVk4OyEQvF2= NGDvOZdUSU6JRWK=
NCI-H1770 Mk\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnS3TWM2OD1|Mz6xOlQ5KM7:TR?= MmL6V2FPT0WU
EM-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPW[YxGUUN3ME2zN{43PTB2IN88US=> NVj4S5hXW0GQR1XS
ChaGo-K-1 M3;zZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEn3R4VKSzVyPUOzMlczOzZizszN NELtPVZUSU6JRWK=
ACHN MlLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTN|LkizPFUh|ryP Mn7wV2FPT0WU
MN-60 NV[3UW1GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTBXHBWUUN3ME2zN{45PTR2IN88US=> NFjUSWZUSU6JRWK=
EW-18 MkXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHx[XdKSzVyPUOzMlg6PzFizszN M3XqbHNCVkeHUh?=
KGN NF3lO|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPofoVKSzVyPUO1MlczQTJizszN NVe0TZI1W0GQR1XS
U031 MnewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrxTWM2OD1|NT64NVMzKM7:TR?= NXrpNnBWW0GQR1XS
HMV-II MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoP5TWM2OD1|Nj6wO|c1KM7:TR?= MkTLV2FPT0WU
L-363 NHz6SlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\6OZo1UUN3ME2zO{43PDV3IN88US=> NHS0ToxUSU6JRWK=
NCI-H1155 NYi1cmFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\xOXVwUUN3ME2zPE4xODF3IN88US=> MmOzV2FPT0WU
NCI-H1793 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPQUGtwUUN3ME2zPE4yODJ4IN88US=> M1LIOHNCVkeHUh?=
P30-OHK M2C5Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;DWnFkUUN3ME2zPE4yOzN{IN88US=> NHfEUHBUSU6JRWK=
AN3-CA MnvRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTN6LkG2NVUh|ryP M1Gy[nNCVkeHUh?=
UACC-257 NEXNb3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLGd5ZKSzVyPUO4Mlc6KM7:TR?= MonqV2FPT0WU
MCF7 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLpTWM2OD1|OT64OlI6KM7:TR?= NVexcIdpW0GQR1XS
KP-N-YN MmfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorhTWM2OD12MD60Nlg2KM7:TR?= NXL2fWk2W0GQR1XS
T98G NWe0UnZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PHeWlEPTB;NECuOFk2PyEQvF2= M2KzOXNCVkeHUh?=
HGC-27 MlvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fJbmlEPTB;NEOuNlc1KM7:TR?= NGDaWphUSU6JRWK=
NCI-H1092 M2X5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7lTWM2OD12Mz6yPFk2KM7:TR?= M3HTcHNCVkeHUh?=
KARPAS-299 MlPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoC1TWM2OD12Mz6zNFcyKM7:TR?= Mn3XV2FPT0WU
LB1047-RCC MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrEbmhlUUN3ME20OE46QTV7IN88US=> NX3DcoduW0GQR1XS
786-0 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jueWlEPTB;NEWuOlUh|ryP NHLxOYxUSU6JRWK=
HCC2157 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDCTWM2OD12Nj6wN|U6KM7:TR?= MWTTRW5ITVJ?
NY Mmf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPWcG9WUUN3ME20Ok4yPzd6IN88US=> MYDTRW5ITVJ?
EFM-19 NIe3U3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvTcYpbUUN3ME20Ok44PTN|IN88US=> M3TwNnNCVkeHUh?=
EW-16 NEj4eZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDMO|FKSzVyPUS2Mlc5ODZizszN Mn;XV2FPT0WU
UM-UC-3 NHyweXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3mwe2lEPTB;NE[uPFA2QSEQvF2= M4HCN3NCVkeHUh?=
HT-29 MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvPXo5bUUN3ME20O{45Pzl{IN88US=> NUjtNIZ{W0GQR1XS
LN-405 M2fqd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTSTWM2OD12OD6wPFI4KM7:TR?= NYHpeGJ1W0GQR1XS
NCI-H727 NX[zOIc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fUO2lEPTB;NEiuO|czPiEQvF2= MVPTRW5ITVJ?
D-502MG MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTR6Lkm2O|Yh|ryP NUfWWHFwW0GQR1XS
GMS-10 NVXhRlZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jnVGlEPTB;NEmuNlk4PCEQvF2= MXTTRW5ITVJ?
MEL-JUSO M3\sTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTR7LkO0O{DPxE1? MXrTRW5ITVJ?

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[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.
細胞試験: [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)
動物試験:[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 Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
2% DMSO+50% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 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
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.

Related Antibodies

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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID