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 在庫  
JPY 22462.12 あり
JPY 17278.56 あり
JPY 38876.76 あり
JPY 96471.96 あり

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。
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)
FRK [1]
(Cell-free assay)
6.7 nM 13 nM 130 nM 160 nM 1.3 μM
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 MmSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVe0VXZbUUN3ME2wMlA4PDV5IN88US=> MX7TRW5ITVJ?
EoL-1-cell MoHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXwcIJKSzVyPUCuNVQyPjZizszN NWT1NlluW0GQR1XS
C32 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULod2E1UUN3ME2wMlE2OTNzIN88US=> NIDkcVRUSU6JRWK=
M14 NWCzSWFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\DOmlKSzVyPUCuNlE4PTdizszN MWTTRW5ITVJ?
CP50-MEL-B NX\U[Y5bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjNTWM2OD1yLkK5O|g1KM7:TR?= MWTTRW5ITVJ?
A101D MkX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnmTWM2OD1yLkOyOVg6KM7:TR?= NYjoZWF7W0GQR1XS
G-361 Ml\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX62eWY{UUN3ME2wMlM1PjN5IN88US=> NXzSUINmW0GQR1XS
HT-144 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnEe3lKSzVyPUCuN|Y{OjlizszN MorKV2FPT0WU
ACN NHzoW41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkm0TWM2OD1yLkO4OFc4KM7:TR?= M2X2OXNCVkeHUh?=
COLO-829 M2PpU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTkTWM2OD1yLkO4PVY5KM7:TR?= M3vRbXNCVkeHUh?=
MEL-HO MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXCNpZxUUN3ME2wMlQyOTd7IN88US=> MUPTRW5ITVJ?
SH-4 M4jrVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTBwNEG0NlIh|ryP MkDNV2FPT0WU
SK-MEL-3 NYHvdXM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHJRXVoUUN3ME2wMlUyPTZ6IN88US=> MX3TRW5ITVJ?
A375 NWrrTlhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHGTWM2OD1yLk[3N|U6KM7:TR?= MUXTRW5ITVJ?
MMAC-SF M1XkXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33XWWlEPTB;MD62PFYyPCEQvF2= NVLYOWlSW0GQR1XS
BHT-101 MlvRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\FTWM2OD1yLkewO|AzKM7:TR?= NVGzOWFoW0GQR1XS
K5 NIrNNI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmi5TWM2OD1yLke2NVQ5KM7:TR?= Mm\jV2FPT0WU
BV-173 NEDXTGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\LeWlEPTB;MD63PVY1PCEQvF2= Mo\XV2FPT0WU
RVH-421 M4jkT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHuSWQyUUN3ME2wMlg3Pzl4IN88US=> MnjKV2FPT0WU
HCC2218 MnzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LORmlEPTB;MD64O|g1PCEQvF2= MoLTV2FPT0WU
WM-115 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\xcXVnUUN3ME2wMlg5Pjl{IN88US=> MYLTRW5ITVJ?
SK-MEL-28 NV7xXFdPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXexTlV4UUN3ME2xMlA1PTZ7IN88US=> MYjTRW5ITVJ?
COLO-679 NFrmSIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LkN2lEPTB;MT6xNFQ3PCEQvF2= NYKzSFFyW0GQR1XS
MZ7-mel MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\BW2lEPTB;MT6xOFk3OyEQvF2= NGPlUXlUSU6JRWK=
SK-MEL-30 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFq0N5FKSzVyPUGuN|M{QDZizszN M4jQ[3NCVkeHUh?=
NCI-H209 NUTEOmN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTFwNkC4OkDPxE1? MoLtV2FPT0WU
HTC-C3 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\p[2lEPTB;MT62OlI6PCEQvF2= M1TlR3NCVkeHUh?=
KARPAS-45 M1TPdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1m4fGlEPTB;Mj6wOFk4QCEQvF2= NGCxZYtUSU6JRWK=
NCI-SNU-5 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTJwMUG5Olkh|ryP MWDTRW5ITVJ?
KP-4 M{LRNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvPbHhTUUN3ME2yMlMxPzh5IN88US=> MUTTRW5ITVJ?
PA-1 NUPYT|BYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTJwN{K2O|Mh|ryP NH\1N|dUSU6JRWK=
HuO-3N1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\HS2lEPTB;Mj64O|k1PiEQvF2= NVfSSGpXW0GQR1XS
NCI-H358 NYrQOVJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jSNmlEPTB;Mj65NlI{OiEQvF2= NWj6cpdVW0GQR1XS
CTB-1 NET4flRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnKSZB2UUN3ME2zMlQxOTd4IN88US=> MoXVV2FPT0WU
697 M{D4U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTNwNUWyOlYh|ryP NH7xTpRUSU6JRWK=
CP66-MEL NXviUpc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTRwMUW5Nlch|ryP NIP1[mlUSU6JRWK=
NB13 NEGyR3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17JZmlEPTB;ND60PVE4QSEQvF2= NInO[|NUSU6JRWK=
DBTRG-05MG NUXEVVFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTRwNUOzNlUh|ryP NIj3UYxUSU6JRWK=
A2058 NWG5ZYloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTRwN{KxOlQh|ryP M1nQd3NCVkeHUh?=
KG-1 M175fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nXcWlEPTB;ND63N|kxQCEQvF2= NYnURlJbW0GQR1XS
8305C MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTVwMUi3N{DPxE1? NVvHRWRYW0GQR1XS
RPMI-7951 NYPaZ4VoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzYRVZKSzVyPUWuPFAzQDNizszN M4TGenNCVkeHUh?=
CHL-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTVwOUe2NFMh|ryP NGTUSZBUSU6JRWK=
TI-73 NGPIcXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13Fe2lEPTB;Nj6wNFkxOiEQvF2= MX;TRW5ITVJ?
HT-1080 M3:yU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PKb2lEPTB;Nj6xNFk1PiEQvF2= M4HqTXNCVkeHUh?=
ES5 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvZTIVKSzVyPU[uNVQ6OjRizszN NYnqfItSW0GQR1XS
8-MG-BA MlzvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXNZlJKUUN3ME22MlE5OTJ7IN88US=> NX;Td241W0GQR1XS
NB7 MljwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XtfmlEPTB;Nj6yNVM4OyEQvF2= Mn[wV2FPT0WU
H4 NWXOV|hrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTZwMkK0PVMh|ryP NHu0W4NUSU6JRWK=
CAL-72 MnX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;0N5dKUUN3ME22MlQ2PDJ|IN88US=> M2nqSXNCVkeHUh?=
HCC1806 NX62fYZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7HTm5QUUN3ME22MlgyQTNzIN88US=> M1[4UnNCVkeHUh?=
BCPAP M1:xVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rCeGlEPTB;Nz6yNVc3PCEQvF2= MnPMV2FPT0WU
LB2241-RCC M1L4emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Tt[GlEPTB;Nz6zOlkxPyEQvF2= M2HHeHNCVkeHUh?=
COLO-741 NIDubmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3iyXWlEPTB;OD6wNVY4QSEQvF2= NX:yOnJ4W0GQR1XS
HSC-3 Mm\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPWTWM2OD16LkC3NFY5KM7:TR?= NXHJd2RVW0GQR1XS
SW982 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7YUHVKUUN3ME24MlQyPTF4IN88US=> MYLTRW5ITVJ?
GCT M4PNZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DIXGlEPTB;OD63OVMyPCEQvF2= NF72dJBUSU6JRWK=
KY821 MnnuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTlwMEWxO|gh|ryP MYnTRW5ITVJ?
JVM-3 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1j6PWlEPTB;OT61Olk6QSEQvF2= NIGzZnhUSU6JRWK=
RS4-11 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnGcGlYUUN3ME25MlYxPDhizszN NULE[ItnW0GQR1XS
VA-ES-BJ M3zkRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzRRWRKSzVyPUGwMlAyPDlizszN M{G1enNCVkeHUh?=
A431 NWezVWRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\5NYR5UUN3ME2xNE41OjF{IN88US=> MYTTRW5ITVJ?
LXF-289 MljUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnmcXAzUUN3ME2xNE41PThizszN MlXIV2FPT0WU
SK-MEL-24 NXrqN4lVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTFyLkiyO|Qh|ryP NHzCfVJUSU6JRWK=
NOS-1 NUSwfndOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTwdXVlUUN3ME2xNE45PDd{IN88US=> M122UnNCVkeHUh?=
KNS-62 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmH6TWM2OD1zMT6yOFA1KM7:TR?= MYHTRW5ITVJ?
SK-HEP-1 M{nofWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTFzLkO1Nlch|ryP NGi5[ZRUSU6JRWK=
A3-KAW MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTyNHVKSzVyPUGxMlcyPzhizszN MWrTRW5ITVJ?
SK-LU-1 NEHt[GpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mle4TWM2OD1zMj6yOlU2KM7:TR?= M4HPRnNCVkeHUh?=
TYK-nu NIDhcWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTF{LkO5N|Ih|ryP MXfTRW5ITVJ?
NMC-G1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7lWnlKSzVyPUGyMlYxPjJizszN NV;pbm0{W0GQR1XS
BB65-RCC NX7qNnlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPLZWRKSzVyPUGyMlcyPjlizszN MYLTRW5ITVJ?
QIMR-WIL NEXESFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTF{Lki4N|Mh|ryP MULTRW5ITVJ?
D-566MG MlfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnLSot{UUN3ME2xN{46PTd4IN88US=> MmPWV2FPT0WU
KYSE-140 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTF2LkC3OVMh|ryP MlTlV2FPT0WU
SCC-4 NXi3XIpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTF2LkOzOVkh|ryP MlrwV2FPT0WU
U251 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTF2Lki0PVIh|ryP MWXTRW5ITVJ?
D-542MG M3HRdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjicpBpUUN3ME2xOE46OjJ{IN88US=> MorCV2FPT0WU
LAMA-84 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLkbmtDUUN3ME2xOE46QTN{IN88US=> NVn2R29xW0GQR1XS
NCI-H720 NYjkPIZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrKSo5KSzVyPUG1MlI3QDRizszN NXX2c3lLW0GQR1XS
DEL Ml:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTF3LkSyPVMh|ryP NIDYV|FUSU6JRWK=
SBC-1 NYDLW2twT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvuTWM2OD1zNT60N|A2KM7:TR?= NV\tVoFqW0GQR1XS
ECC10 NW\EOZJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzEVZFrUUN3ME2xOU41PDV6IN88US=> M2r0[HNCVkeHUh?=
Daoy MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHISnlKSzVyPUG1Mlc3OTZizszN M4HiXnNCVkeHUh?=
SCH MmXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXL6e|VOUUN3ME2xOU44QDN3IN88US=> NHXlcWhUSU6JRWK=
MZ2-MEL MoXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTF4LkC2OFYh|ryP M3\1dHNCVkeHUh?=
CAL-12T MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{L5TmlEPTB;MU[uOFg3OiEQvF2= MVzTRW5ITVJ?
KE-37 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XFXWlEPTB;MU[uPFExPyEQvF2= NY\qOVZyW0GQR1XS
LS-411N Mkj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFiyb21KSzVyPUG3MlEyQCEQvF2= NWGw[4U4W0GQR1XS
NCI-H2228 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTF5LkOwO|Eh|ryP Mmj3V2FPT0WU
SK-MEL-2 NYfxdVhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLzfZFKSzVyPUG3MlQ6PjVizszN M1P4NHNCVkeHUh?=
HN M2XtcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTF5LkeyOFgh|ryP M1jCWnNCVkeHUh?=
NCI-H1648 NX73c2Z[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUGxOWw1UUN3ME2xO{45OThizszN M13SUHNCVkeHUh?=
IA-LM MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HmWGlEPTB;MUiuN|E4OiEQvF2= NVWwUJB{W0GQR1XS
EW-13 NFruemZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\RVGlEPTB;MUiuOVcxQCEQvF2= MUnTRW5ITVJ?
YKG-1 MlnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjrXIduUUN3ME2xPU42PzFzIN88US=> MlmzV2FPT0WU
KNS-81-FD MoG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PCZmlEPTB;MUmuOVg2QCEQvF2= NUnES2czW0GQR1XS
23132-87 MmDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTpeW4zUUN3ME2xPU44PjR{IN88US=> NIr3NnNUSU6JRWK=
NUGC-3 NEfVNGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\DcYIxUUN3ME2xPU46QDh5IN88US=> M{PqNXNCVkeHUh?=
5637 NFz6OYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTybY5KSzVyPUKwMlA1PzhizszN NHHa[VhUSU6JRWK=
NCI-H1755 Mn7US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\1c3dKSzVyPUKwMlQ4PjRizszN MkH6V2FPT0WU
RH-18 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXZWI42UUN3ME2yNE42PzR6IN88US=> NWrRXppKW0GQR1XS
RXF393 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEWx[JVKSzVyPUKwMlY4PTZizszN NHPkZZVUSU6JRWK=
LU-134-A NIWzRnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnITWM2OD1{MD63NFU3KM7:TR?= MnnNV2FPT0WU
TE-12 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;sc2lEPTB;MkCuO|IxOSEQvF2= MnnLV2FPT0WU
MOLT-4 Mk\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jvcGlEPTB;MkGuNVkyPSEQvF2= M2npd3NCVkeHUh?=
IGR-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTJzLkO3PVYh|ryP M1PvTXNCVkeHUh?=
HOP-92 Mm\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvWb4dXUUN3ME2yNU41QTh5IN88US=> MUXTRW5ITVJ?
SK-MES-1 MnzvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2D0PGlEPTB;MkGuO|M5OSEQvF2= NFzKSohUSU6JRWK=
LU-65 MmnaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXZS4NKSzVyPUKxMlg3OjRizszN Ml\NV2FPT0WU
MS-1 NUX1dFBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrBTWM2OD1{Mj6xNlA{KM7:TR?= NG[1V3pUSU6JRWK=
LoVo MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zpTWlEPTB;MkKuNlQ1KM7:TR?= Mn;MV2FPT0WU
A704 M1vEfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTJ{LkWxOVUh|ryP Mnr0V2FPT0WU
HT-1376 NWLTSJR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHu0NnhKSzVyPUKyMlYxPTlizszN M4K1NHNCVkeHUh?=
IST-MEL1 M17ldWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4iyU2lEPTB;MkKuOlc2OSEQvF2= NF\TW5JUSU6JRWK=
Ramos-2G6-4C10 MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvJTWM2OD1{Mj63N|Y3KM7:TR?= NIm3OlVUSU6JRWK=
T47D MlPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJ{Lke5O|kh|ryP NHPZUJpUSU6JRWK=
HT-1197 NUXjZmd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3n4eWlEPTB;MkOuNFgyPyEQvF2= M{\yfHNCVkeHUh?=
LB2518-MEL NWGye204T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vvTGlEPTB;MkOuOlQyOiEQvF2= NVjjbpFuW0GQR1XS
J-RT3-T3-5 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnXTWM2OD1{ND63OVk2KM7:TR?= NX[2c5ZMW0GQR1XS
SK-NEP-1 MkLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXW[2FKSzVyPUK0Mlg4PDRizszN NF73VIdUSU6JRWK=
NCI-H526 NVPFUmxFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojSTWM2OD1{NT6wNFI{KM7:TR?= Mn2wV2FPT0WU
IST-SL1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTJ3LkK3OVEh|ryP NUC3UFJ4W0GQR1XS
HH MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTJ3LkOxPVIh|ryP NXzBVYVUW0GQR1XS
NCI-H82 NHnHcY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XHXmlEPTB;MkWuPVM5KM7:TR?= M1XFd3NCVkeHUh?=
SNU-449 NH[zZnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vSUWlEPTB;MkeuNlAyQCEQvF2= NYHXTXhzW0GQR1XS
COR-L23 NYHRWVJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXS1bWMxUUN3ME2yO{4zQDF|IN88US=> MkjvV2FPT0WU
LOXIMVI M4WwNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGL5d|FKSzVyPUK3MlM3QCEQvF2= NVfyZY5QW0GQR1XS
GR-ST NXr1Tpd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjhdHRKSzVyPUK3MlY4ODZizszN M3fNSHNCVkeHUh?=
NCI-SNU-1 MoP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfKTWM2OD1{Nz65OFQh|ryP MX\TRW5ITVJ?
ALL-PO MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjSW2RNUUN3ME2yPE4yPjB2IN88US=> NILHWHNUSU6JRWK=
ML-2 NXLKUXRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFO3XohKSzVyPUK4MlI5OTRizszN M{PScHNCVkeHUh?=
HOP-62 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofzTWM2OD1{OD63NVMh|ryP MnfHV2FPT0WU
EGI-1 NGLXOnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HFXWlEPTB;MkiuPFg1PSEQvF2= NGO5bWhUSU6JRWK=
TCCSUP NGjHd3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7qTWM2OD1{OD65NlczKM7:TR?= NX;p[3F[W0GQR1XS
LB996-RCC MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fNPWlEPTB;MkmuOVY5OiEQvF2= NHP4S|ZUSU6JRWK=
LCLC-97TM1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTN{LkG5OlQh|ryP MX\TRW5ITVJ?
NCI-H1304 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrYfJhKSzVyPUOyMlM{ODFizszN MkntV2FPT0WU
KP-N-YS NFvSbVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDSV2xKSzVyPUOyMlU6PzNizszN NXezbYw2W0GQR1XS
NCI-H1770 MnHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjpfpVKSzVyPUOzMlE3PDhizszN NHfiW5dUSU6JRWK=
EM-2 NXPSV24zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HtUWlEPTB;M{OuOlUxPCEQvF2= NUHBeFNUW0GQR1XS
ChaGo-K-1 M{fNZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;DZVZxUUN3ME2zN{44OjN4IN88US=> NYTvXJNQW0GQR1XS
ACHN M3XyVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfLTWM2OD1|Mz64N|g2KM7:TR?= MoDWV2FPT0WU
MN-60 Ml7DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjo[5l2UUN3ME2zN{45PTR2IN88US=> NYn1U3ZGW0GQR1XS
EW-18 M33MSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDNS2NKSzVyPUOzMlg6PzFizszN M1L4VHNCVkeHUh?=
KGN NWnMOZNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXv3XIZsUUN3ME2zOU44Ojl{IN88US=> M2O2[nNCVkeHUh?=
U031 NEPwPFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TY[GlEPTB;M{WuPFE{OiEQvF2= NVrzT4pRW0GQR1XS
HMV-II MnfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2H0dmlEPTB;M{[uNFc4PCEQvF2= NHjxTYZUSU6JRWK=
L-363 M1uyNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTN5Lk[0OVUh|ryP NV7Q[G9zW0GQR1XS
NCI-H1155 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrwNlZFUUN3ME2zPE4xODF3IN88US=> NXrudXJXW0GQR1XS
NCI-H1793 NF;jR2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4KyVWlEPTB;M{iuNVAzPiEQvF2= NVjVdXFmW0GQR1XS
P30-OHK MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{n0RWlEPTB;M{iuNVM{OiEQvF2= M1LnT3NCVkeHUh?=
AN3-CA M4jaUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTN6LkG2NVUh|ryP MojpV2FPT0WU
UACC-257 MkTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXWTWM2OD1|OD63PUDPxE1? NGDqcGNUSU6JRWK=
MCF7 M2Wwdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDnWWtKSzVyPUO5Mlg3OjlizszN NY\ZSJM5W0GQR1XS
KP-N-YN Mk\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XxcWlEPTB;NECuOFI5PSEQvF2= NEfYZ29USU6JRWK=
T98G M2CzU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\ne2lEPTB;NECuOFk2PyEQvF2= MWrTRW5ITVJ?
HGC-27 NEjzVoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\CTWM2OD12Mz6yO|Qh|ryP NInjT4dUSU6JRWK=
NCI-H1092 M4L6TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrueXRKSzVyPUSzMlI5QTVizszN Mm\xV2FPT0WU
KARPAS-299 M3\J[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33jT2lEPTB;NEOuN|A4OSEQvF2= MVLTRW5ITVJ?
LB1047-RCC NVHMfWt{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIW2OZJKSzVyPUS0Mlk6PTlizszN NFPRbWtUSU6JRWK=
786-0 MnHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7GTWM2OD12NT62OUDPxE1? NGflbYNUSU6JRWK=
HCC2157 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLUd4pKSzVyPUS2MlA{PTlizszN NVrOcFRsW0GQR1XS
NY M1XNOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3ObJpEUUN3ME20Ok4yPzd6IN88US=> NWPIPJgyW0GQR1XS
EFM-19 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTR4Lke1N|Mh|ryP M3vnZ3NCVkeHUh?=
EW-16 MnPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\TfoVKSzVyPUS2Mlc5ODZizszN M2\5NnNCVkeHUh?=
UM-UC-3 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\TTWM2OD12Nj64NFU6KM7:TR?= NH7QPGdUSU6JRWK=
HT-29 NITKfldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7sTWM2OD12Nz64O|kzKM7:TR?= NFPLRmRUSU6JRWK=
LN-405 M1XqNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;oTWM2OD12OD6wPFI4KM7:TR?= NIfXdoVUSU6JRWK=
NCI-H727 MlS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLMcZpKSzVyPUS4Mlc4OjZizszN Ml;QV2FPT0WU
D-502MG MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjETGpKSzVyPUS4Mlk3PzZizszN M1rxOXNCVkeHUh?=
GMS-10 MmHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vmXGlEPTB;NEmuNlk4PCEQvF2= Mo\UV2FPT0WU
MEL-JUSO M4nqR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTR7LkO0O{DPxE1? M3na[3NCVkeHUh?=

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
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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID