PLX-4720 化学構造
分子量: 413.83

高品質保証

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Quality Control & MSDS

製品説明

  • Compare Raf Inhibitors
    Raf製品生物活性の比較
  • 研究分野
  • PLX-4720のメカニズム

製品の説明

生物活性

製品説明 PLX-4720は、B-Raf(V600E)とc-Raf-1(Y340D/Y341D)の「実行中の」形の強力で選択的な阻害剤で、IC50 がそれぞれ 13 nM と 6.7 nMです。
ターゲット B-RafV600E c-Raf-1Y340D/Y341D
IC50 13 nM 6.7 nM [1]
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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
DU-4475 M3P1c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7WTWM2OD1yLkC3OFU4KM7:TR?= M37DOnNCVkeHUh?=
EoL-1-cell M3\0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jM[2lEPTB;MD6xOFE3PiEQvF2= NGPBXXZUSU6JRWK=
C32 NWXUd2V6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTBwMUWxN|Eh|ryP NHuye49USU6JRWK=
M14 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3S1bGlEPTB;MD6yNVc2PyEQvF2= NFLMVHVUSU6JRWK=
CP50-MEL-B Ml7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwMkm3PFQh|ryP MmjCV2FPT0WU
A101D NWHvS2t5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI[1Z5FKSzVyPUCuN|I2QDlizszN NXv2cGdUW0GQR1XS
G-361 NIPXRXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnNbGs2UUN3ME2wMlM1PjN5IN88US=> MXrTRW5ITVJ?
HT-144 NIL6ZoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LZRmlEPTB;MD6zOlMzQSEQvF2= MVzTRW5ITVJ?
ACN NHjhXXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwM{i0O|ch|ryP NYL6dpI4W0GQR1XS
COLO-829 MnnGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlGwTWM2OD1yLkO4PVY5KM7:TR?= NHT0d3RUSU6JRWK=
MEL-HO MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLUV|lKSzVyPUCuOFEyPzlizszN NFH3NZpUSU6JRWK=
SH-4 NVv3dWRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTaTWM2OD1yLkSxOFIzKM7:TR?= MkjhV2FPT0WU
SK-MEL-3 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXCTWM2OD1yLkWxOVY5KM7:TR?= M{X6SHNCVkeHUh?=
A375 NEnjeWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XYRWlEPTB;MD62O|M2QSEQvF2= MkXPV2FPT0WU
MMAC-SF NIHjW|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDjcnlKSzVyPUCuOlg3OTRizszN NF3BZ2pUSU6JRWK=
BHT-101 M17Remdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTBwN{C3NFIh|ryP NVzxdlhlW0GQR1XS
K5 M1zmemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\MUFJKSzVyPUCuO|YyPDhizszN NY\VbGpqW0GQR1XS
BV-173 M2Hnbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfORXk3UUN3ME2wMlc6PjR2IN88US=> NFLoNZBUSU6JRWK=
RVH-421 M4Dmb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHxU4NKSzVyPUCuPFY4QTZizszN M2PWTnNCVkeHUh?=
HCC2218 MlH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvYTWM2OD1yLki3PFQ1KM7:TR?= NIjBTYxUSU6JRWK=
WM-115 NYDXe2h5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTBwOEi2PVIh|ryP M1nxTHNCVkeHUh?=
SK-MEL-28 NGPBdYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[zRmdlUUN3ME2xMlA1PTZ7IN88US=> NVHOV|R5W0GQR1XS
COLO-679 MnLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvwbGFbUUN3ME2xMlExPDZ2IN88US=> MkTJV2FPT0WU
MZ7-mel NVzJNpc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fpPGlEPTB;MT6xOFk3OyEQvF2= NYjvUIx[W0GQR1XS
SK-MEL-30 Mlf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLOTWM2OD1zLkOzN|g3KM7:TR?= M4\GfHNCVkeHUh?=
NCI-H209 MknJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmf3TWM2OD1zLk[wPFYh|ryP MWXTRW5ITVJ?
HTC-C3 M125[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTFwNk[yPVQh|ryP NVHLOlBTW0GQR1XS
KARPAS-45 NFHyOXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmroTWM2OD1{LkC0PVc5KM7:TR?= MYTTRW5ITVJ?
NCI-SNU-5 NEXWRYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWG3XndEUUN3ME2yMlEyQTZ7IN88US=> M2PFdHNCVkeHUh?=
KP-4 M3\JdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\OdW5KSzVyPUKuN|A4QDdizszN NEjve3NUSU6JRWK=
PA-1 Ml3WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2P3NGlEPTB;Mj63NlY4OyEQvF2= NIrnTFZUSU6JRWK=
HuO-3N1 M4\p[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjpOoZuUUN3ME2yMlg4QTR4IN88US=> MXzTRW5ITVJ?
NCI-H358 M4n4cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJwOUKyN|Ih|ryP MmrsV2FPT0WU
CTB-1 NVHzbIljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfyTWM2OD1|LkSwNVc3KM7:TR?= NEfXNWpUSU6JRWK=
697 MmLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTNwNUWyOlYh|ryP NVnTNpdmW0GQR1XS
CP66-MEL M3;zcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTRwMUW5Nlch|ryP MoTVV2FPT0WU
NB13 MkHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\ybFBzUUN3ME20MlQ6OTd7IN88US=> NHr1NGJUSU6JRWK=
DBTRG-05MG NUnFWW9VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvyfWxTUUN3ME20MlU{OzJ3IN88US=> NHnzZXRUSU6JRWK=
A2058 NGrNSmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fsN2lEPTB;ND63NlE3PCEQvF2= MlzHV2FPT0WU
KG-1 MojRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPTUJBKSzVyPUSuO|M6ODhizszN NFvSbmJUSU6JRWK=
8305C NFG4e|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTpN2Z6UUN3ME21MlE5PzNizszN NETX[4VUSU6JRWK=
RPMI-7951 MlnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXW0bGRmUUN3ME21MlgxOjh|IN88US=> M3fGdXNCVkeHUh?=
CHL-1 NWPHe4FNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fiWmlEPTB;NT65O|YxOyEQvF2= M3X6dnNCVkeHUh?=
TI-73 NVS1VXJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTZwMEC5NFIh|ryP MmXJV2FPT0WU
HT-1080 NFvxWZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTZwMUC5OFYh|ryP MmWxV2FPT0WU
ES5 NGTQWVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXlTWM2OD14LkG0PVI1KM7:TR?= MXfTRW5ITVJ?
8-MG-BA NIDrVHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDGSWJIUUN3ME22MlE5OTJ7IN88US=> MlTpV2FPT0WU
NB7 M2Xrb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWG2UZlbUUN3ME22MlIyOzd|IN88US=> NGfMcnNUSU6JRWK=
H4 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2O1bGlEPTB;Nj6yNlQ6OyEQvF2= M1exV3NCVkeHUh?=
CAL-72 NYLpV5U6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHKzSZVKSzVyPU[uOFU1OjNizszN MWnTRW5ITVJ?
HCC1806 NYDqOpFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTjTWM2OD14LkixPVMyKM7:TR?= M{\KcXNCVkeHUh?=
BCPAP MnvsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTdwMkG3OlQh|ryP MnzMV2FPT0WU
LB2241-RCC MmPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHnWI5KSzVyPUeuN|Y6ODdizszN Mk\ZV2FPT0WU
COLO-741 NUnTcHlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRThwMEG2O|kh|ryP Mn3HV2FPT0WU
HSC-3 NIjSfnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jJd2lEPTB;OD6wO|A3QCEQvF2= NYj3[5AxW0GQR1XS
SW982 NXzqRnZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTZXZJKSzVyPUiuOFE2OTZizszN NF7sToZUSU6JRWK=
GCT Mm\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRThwN{WzNVQh|ryP MoDQV2FPT0WU
KY821 NUnkXGZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjW[WxKSzVyPUmuNFUyPzhizszN MlPOV2FPT0WU
JVM-3 NXjVfZFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfPTWM2OD17LkW2PVk6KM7:TR?= MnTFV2FPT0WU
RS4-11 M37sZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGGx[mRKSzVyPUmuOlA1QCEQvF2= NEfXfoxUSU6JRWK=
VA-ES-BJ M1z0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPWNFNJUUN3ME2xNE4xOTR7IN88US=> MlzGV2FPT0WU
A431 NG\2eZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVH6O4FoUUN3ME2xNE41OjF{IN88US=> MmPuV2FPT0WU
LXF-289 MmfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3zd2FlUUN3ME2xNE41PThizszN NVW2b|ZzW0GQR1XS
SK-MEL-24 NVX6VGJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmryTWM2OD1zMD64Nlc1KM7:TR?= MnHuV2FPT0WU
NOS-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXkTWM2OD1zMD64OFczKM7:TR?= MknYV2FPT0WU
KNS-62 M3TNfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmCyTWM2OD1zMT6yOFA1KM7:TR?= NYn0[VZXW0GQR1XS
SK-HEP-1 NVLkeHByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXi1[nVOUUN3ME2xNU4{PTJ5IN88US=> M2LKeXNCVkeHUh?=
A3-KAW NHvrVllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHO2cXdKSzVyPUGxMlcyPzhizszN NHLVRo5USU6JRWK=
SK-LU-1 MlfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHwTWM2OD1zMj6yOlU2KM7:TR?= NELCNJNUSU6JRWK=
TYK-nu MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXydW5pUUN3ME2xNk4{QTN{IN88US=> NIHHcYFUSU6JRWK=
NMC-G1 MlPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUT2R|RZUUN3ME2xNk43ODZ{IN88US=> MVvTRW5ITVJ?
BB65-RCC M2noVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTF{LkexOlkh|ryP MVjTRW5ITVJ?
QIMR-WIL M4i5VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljBTWM2OD1zMj64PFM{KM7:TR?= NEPxZ4dUSU6JRWK=
D-566MG MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfjNWxkUUN3ME2xN{46PTd4IN88US=> NXfh[XZuW0GQR1XS
KYSE-140 NF\LUWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2GwWmlEPTB;MUSuNFc2OyEQvF2= M2TxT3NCVkeHUh?=
SCC-4 NVK3RWRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4myUWlEPTB;MUSuN|M2QSEQvF2= NF7z[XhUSU6JRWK=
U251 NYHUfW1QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrXbo9IUUN3ME2xOE45PDl{IN88US=> MmqzV2FPT0WU
D-542MG MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTF2LkmyNlIh|ryP M{\NSHNCVkeHUh?=
LAMA-84 MkTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVX6fplWUUN3ME2xOE46QTN{IN88US=> NW\K[ZdpW0GQR1XS
NCI-H720 M4frdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvNe3Y2UUN3ME2xOU4zPjh2IN88US=> M4XoZXNCVkeHUh?=
DEL M4TRWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDZTWM2OD1zNT60Nlk{KM7:TR?= NUXCUVJRW0GQR1XS
SBC-1 NH\vNHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDrS5JKSzVyPUG1MlQ{ODVizszN NFz5ZoRUSU6JRWK=
ECC10 NGPHRVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnlWoNKSzVyPUG1MlQ1PThizszN MljHV2FPT0WU
Daoy NVu5NZRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTF3Lke2NVYh|ryP NUXwWlhRW0GQR1XS
SCH MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PVWmlEPTB;MUWuO|g{PSEQvF2= MoroV2FPT0WU
MZ2-MEL NXjKd|Q4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTF4LkC2OFYh|ryP NGTkeotUSU6JRWK=
CAL-12T M{jJOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvsNllJUUN3ME2xOk41QDZ{IN88US=> M33ORXNCVkeHUh?=
KE-37 NYPWbGVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4[0cWlEPTB;MU[uPFExPyEQvF2= NUK3eVBNW0GQR1XS
LS-411N M1Lz[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{[xXmlEPTB;MUeuNVE5KM7:TR?= NELRNW9USU6JRWK=
NCI-H2228 M1PxT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfQTWM2OD1zNz6zNFcyKM7:TR?= M1jRe3NCVkeHUh?=
SK-MEL-2 Mo\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjxVW1QUUN3ME2xO{41QTZ3IN88US=> MUfTRW5ITVJ?
HN MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3qTWM2OD1zNz63NlQ5KM7:TR?= MUTTRW5ITVJ?
NCI-H1648 NIe0c5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPqVGFKSzVyPUG3MlgyQCEQvF2= NVXCZYxMW0GQR1XS
IA-LM NEnQb4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfZZWxKSzVyPUG4MlMyPzJizszN NIWyNVNUSU6JRWK=
EW-13 MkLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILibFZKSzVyPUG4MlU4ODhizszN MnrGV2FPT0WU
YKG-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTSfGk1UUN3ME2xPU42PzFzIN88US=> M3fIWnNCVkeHUh?=
KNS-81-FD MmCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGS2N2VKSzVyPUG5MlU5PThizszN MUXTRW5ITVJ?
23132-87 NULLUFBkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnIfm9KSzVyPUG5Mlc3PDJizszN MV\TRW5ITVJ?
NUGC-3 NWTNNZFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHFbXBSUUN3ME2xPU46QDh5IN88US=> Mlr0V2FPT0WU
5637 M3f2S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Kz[GlEPTB;MkCuNFQ4QCEQvF2= NX2zZZJbW0GQR1XS
NCI-H1755 NXfPcJhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDHTWM2OD1{MD60O|Y1KM7:TR?= NVrXS2xKW0GQR1XS
RH-18 M2PBdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLvVXRwUUN3ME2yNE42PzR6IN88US=> M2Pi[HNCVkeHUh?=
RXF393 MnTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrpdpFYUUN3ME2yNE43PzV4IN88US=> MVrTRW5ITVJ?
LU-134-A NF;k[WtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTJyLkewOVYh|ryP M{fIV3NCVkeHUh?=
TE-12 NV\YSY5zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLKT|FKSzVyPUKwMlczODFizszN NVPuZmhiW0GQR1XS
MOLT-4 NIXrVHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XwZWlEPTB;MkGuNVkyPSEQvF2= NUDYfJZ5W0GQR1XS
IGR-1 MlO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLRcJFMUUN3ME2yNU4{Pzl4IN88US=> M1HSR3NCVkeHUh?=
HOP-92 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\iSmlEPTB;MkGuOFk5PyEQvF2= M2jHdnNCVkeHUh?=
SK-MES-1 M{Xa[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXSPIlrUUN3ME2yNU44OzhzIN88US=> NF\BSlJUSU6JRWK=
LU-65 NYP6XI5tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\BTWM2OD1{MT64OlI1KM7:TR?= NELyUHBUSU6JRWK=
MS-1 NGL3UoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HWUmlEPTB;MkKuNVIxOyEQvF2= NH\n[4NUSU6JRWK=
LoVo MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDwTWM2OD1{Mj6yOFQh|ryP M3vyXnNCVkeHUh?=
A704 NHf6VXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PQNWlEPTB;MkKuOVE2PSEQvF2= MoHOV2FPT0WU
HT-1376 NGXJS3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLZTWM2OD1{Mj62NFU6KM7:TR?= MUTTRW5ITVJ?
IST-MEL1 Ml;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjmTWM2OD1{Mj62O|UyKM7:TR?= MnLJV2FPT0WU
Ramos-2G6-4C10 MofjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37mVWlEPTB;MkKuO|M3PiEQvF2= MV3TRW5ITVJ?
T47D NV[3NnlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTTOnAxUUN3ME2yNk44QTd7IN88US=> MkfIV2FPT0WU
HT-1197 MnnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojqTWM2OD1{Mz6wPFE4KM7:TR?= NVO5fHNXW0GQR1XS
LB2518-MEL MkDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jFd2lEPTB;MkOuOlQyOiEQvF2= MWHTRW5ITVJ?
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HH M{fQc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3ETWM2OD1{NT6zNVkzKM7:TR?= NFjKbW9USU6JRWK=
NCI-H82 M17tN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPvTWM2OD1{NT65N|gh|ryP NIXGfpdUSU6JRWK=
SNU-449 M{LJUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrOcpFKSzVyPUK3MlIxOThizszN NHPEPWNUSU6JRWK=
COR-L23 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3uyd2lEPTB;MkeuNlgyOyEQvF2= MXvTRW5ITVJ?
LOXIMVI MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3j0OmlEPTB;MkeuN|Y5KM7:TR?= M32yPHNCVkeHUh?=
GR-ST NIXqNWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVW5cZV[UUN3ME2yO{43PzB4IN88US=> NXTEPIdZW0GQR1XS
NCI-SNU-1 NFrpeWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTJ5Lkm0OEDPxE1? NYjOVoJLW0GQR1XS
ALL-PO Mmi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTJ6LkG2NFQh|ryP M3Xz[XNCVkeHUh?=
ML-2 MoezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoX1TWM2OD1{OD6yPFE1KM7:TR?= MnL3V2FPT0WU
HOP-62 M2jBemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;EZWlEPTB;MkiuO|E{KM7:TR?= MmTnV2FPT0WU
EGI-1 M3jzRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH71dWxKSzVyPUK4Mlg5PDVizszN MYHTRW5ITVJ?
TCCSUP MkfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4j1OWlEPTB;MkiuPVI4OiEQvF2= NGjFenFUSU6JRWK=
LB996-RCC NX7TfJBVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTJ7LkW2PFIh|ryP MY\TRW5ITVJ?
LCLC-97TM1 M2CwXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXxTWM2OD1|Mj6xPVY1KM7:TR?= M4ixXHNCVkeHUh?=
NCI-H1304 NWrDOpZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPaNGJKSzVyPUOyMlM{ODFizszN NXf1NFdrW0GQR1XS
KP-N-YS NGDOdXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLiNWVKSzVyPUOyMlU6PzNizszN NVTVd4toW0GQR1XS
NCI-H1770 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIKzdHhKSzVyPUOzMlE3PDhizszN MXzTRW5ITVJ?
EM-2 MlK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7ZOZVKSzVyPUOzMlY2ODRizszN NFKycJhUSU6JRWK=
ChaGo-K-1 MmTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn74TWM2OD1|Mz63NlM3KM7:TR?= NHfpUotUSU6JRWK=
ACHN MmTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\aTWM2OD1|Mz64N|g2KM7:TR?= NETtSVJUSU6JRWK=
MN-60 Mn7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTN|Lki1OFQh|ryP MoHHV2FPT0WU
EW-18 NIXjcVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7QTWM2OD1|Mz64PVcyKM7:TR?= NF7y[XVUSU6JRWK=
KGN NIK0W5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\0dmlEPTB;M{WuO|I6OiEQvF2= NXWwU2g1W0GQR1XS
U031 NEHre4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\E[XBVUUN3ME2zOU45OTN{IN88US=> NInwXnJUSU6JRWK=
HMV-II MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjzZYRKSzVyPUO2MlA4PzRizszN MoW3V2FPT0WU
L-363 M3vOOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkS5TWM2OD1|Nz62OFU2KM7:TR?= M4i4[XNCVkeHUh?=
NCI-H1155 M3;KeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\2TW1KSzVyPUO4MlAxOTVizszN M2fwTXNCVkeHUh?=
NCI-H1793 NFzCT|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\EcINKSzVyPUO4MlExOjZizszN NUDISYJEW0GQR1XS
P30-OHK M4j5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3qwe2lEPTB;M{iuNVM{OiEQvF2= NVK1dodnW0GQR1XS
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T98G M2TrO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTRyLkS5OVch|ryP M2LRUHNCVkeHUh?=
HGC-27 NWLTUFJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH[5UXhKSzVyPUSzMlI4PCEQvF2= MXPTRW5ITVJ?
NCI-H1092 NHX2e5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTR|LkK4PVUh|ryP M4fPZnNCVkeHUh?=
KARPAS-299 Ml\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;xbGlEPTB;NEOuN|A4OSEQvF2= NF7DTFRUSU6JRWK=
LB1047-RCC M2DkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTR2Lkm5OVkh|ryP M{HXWnNCVkeHUh?=
786-0 M4fsSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTR3Lk[1JO69VQ>? NWfTTIVXW0GQR1XS
HCC2157 NEHYPJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\rTWM2OD12Nj6wN|U6KM7:TR?= MULTRW5ITVJ?
NY NGrT[GpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIO1UY1KSzVyPUS2MlE4PzhizszN M2PteHNCVkeHUh?=
EFM-19 NEfVbWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHxTWM2OD12Nj63OVM{KM7:TR?= MVfTRW5ITVJ?
EW-16 NFG0RohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2G5PWlEPTB;NE[uO|gxPiEQvF2= NFrJVmFUSU6JRWK=
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HT-29 NEe4NYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3exVWlEPTB;NEeuPFc6OiEQvF2= NV7vR3ViW0GQR1XS
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NCI-H727 NVjkfnhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfiUIdCUUN3ME20PE44PzJ4IN88US=> MmXMV2FPT0WU
D-502MG NV3ncZJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HxUGlEPTB;NEiuPVY4PiEQvF2= NIq1cXVUSU6JRWK=
GMS-10 M{izXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moq2TWM2OD12OT6yPVc1KM7:TR?= NHu4XHBUSU6JRWK=
MEL-JUSO MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTR7LkO0O{DPxE1? M3jSTnNCVkeHUh?=

... 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]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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]

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.

動物実験: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download PLX-4720 SDF
分子量 413.83
化学式

C17H14ClF2N3O3S

CAS No. 918505-84-7
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 83 mg/mL (200.56 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 2% DMSO+50% PEG 300+5% Tween 80+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 N-(3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide

文献中の引用 (45)

Frequently Asked Questions

  • Question 1
    What would you recommend to make working solution for intraperitoneal injection into mice?

    Answer: 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.

技術サポート&よくある質問(FAQ)

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他の質問がある場合は、お気軽くお問合せください。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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