PLX-4720 化学構造
分子量: 413.83

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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 NVTRZZRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfVTWM2OD1yLkC3OFU4KM7:TR?= NEH2dVhUSU6JRWK=
EoL-1-cell M1PWU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLETWM2OD1yLkG0NVY3KM7:TR?= NI[wc5FUSU6JRWK=
C32 M4LEfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnuemJJUUN3ME2wMlE2OTNzIN88US=> NF23VnNUSU6JRWK=
M14 M3LFTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXafGV[UUN3ME2wMlIyPzV5IN88US=> NF;wT4xUSU6JRWK=
CP50-MEL-B MnTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXr[JpKSzVyPUCuNlk4QDRizszN NGPzUlZUSU6JRWK=
A101D MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TifGlEPTB;MD6zNlU5QSEQvF2= M3jm[3NCVkeHUh?=
G-361 NXfI[W1LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHz3TZJKSzVyPUCuN|Q3OzdizszN M3;OfHNCVkeHUh?=
HT-144 NFGyeGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTBwM{[zNlkh|ryP MnvEV2FPT0WU
ACN NUXVUWh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnGzTWM2OD1yLkO4OFc4KM7:TR?= NFH4WItUSU6JRWK=
COLO-829 MkTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jFcWlEPTB;MD6zPFk3QCEQvF2= MXfTRW5ITVJ?
MEL-HO M1TJdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHNcmJQUUN3ME2wMlQyOTd7IN88US=> MnTsV2FPT0WU
SH-4 NU\FdIRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTBwNEG0NlIh|ryP M334U3NCVkeHUh?=
SK-MEL-3 Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLITWM2OD1yLkWxOVY5KM7:TR?= NWeweoNFW0GQR1XS
A375 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13oZWlEPTB;MD62O|M2QSEQvF2= Ml3XV2FPT0WU
MMAC-SF MoX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fEfGlEPTB;MD62PFYyPCEQvF2= NX3ybllOW0GQR1XS
BHT-101 MoP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nsRWlEPTB;MD63NFcxOiEQvF2= MlPIV2FPT0WU
K5 M3HwTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rrVmlEPTB;MD63OlE1QCEQvF2= MVzTRW5ITVJ?
BV-173 Mn;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPvTWM2OD1yLke5OlQ1KM7:TR?= MnrWV2FPT0WU
RVH-421 NH3kdZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXyTWM2OD1yLki2O|k3KM7:TR?= M2fJUHNCVkeHUh?=
HCC2218 M2jhV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Ow[2lEPTB;MD64O|g1PCEQvF2= NYG4W3VQW0GQR1XS
WM-115 NEPCVZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTBwOEi2PVIh|ryP MUHTRW5ITVJ?
SK-MEL-28 NXjoW|ZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTFwMES1Olkh|ryP NV\EOVVQW0GQR1XS
COLO-679 NEK5PGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3OW|BFUUN3ME2xMlExPDZ2IN88US=> NH6xUYpUSU6JRWK=
MZ7-mel NYfGRlZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkm0TWM2OD1zLkG0PVY{KM7:TR?= MlnjV2FPT0WU
SK-MEL-30 MnPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH72eoNKSzVyPUGuN|M{QDZizszN Mn7mV2FPT0WU
NCI-H209 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7ETWM2OD1zLk[wPFYh|ryP MXjTRW5ITVJ?
HTC-C3 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HIeGlEPTB;MT62OlI6PCEQvF2= MojQV2FPT0WU
KARPAS-45 MnO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rUUGlEPTB;Mj6wOFk4QCEQvF2= NVTFWFlyW0GQR1XS
NCI-SNU-5 M1zGWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3OwcmlEPTB;Mj6xNVk3QSEQvF2= NVn2VG9HW0GQR1XS
KP-4 NF;GO5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTJwM{C3PFch|ryP MXfTRW5ITVJ?
PA-1 NHz4fW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLJTWM2OD1{LkeyOlc{KM7:TR?= Mo\OV2FPT0WU
HuO-3N1 NHXBUndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvVTWM2OD1{Lki3PVQ3KM7:TR?= NX7oOlFiW0GQR1XS
NCI-H358 Mon1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXvfW9zUUN3ME2yMlkzOjN{IN88US=> MoPIV2FPT0WU
CTB-1 M4fGO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXTV2xKSzVyPUOuOFAyPzZizszN MVrTRW5ITVJ?
697 M1n6WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3H2SWlEPTB;Mz61OVI3PiEQvF2= Mnr1V2FPT0WU
CP66-MEL MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3GycWlEPTB;ND6xOVkzPyEQvF2= NHXrXHJUSU6JRWK=
NB13 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoD5TWM2OD12LkS5NVc6KM7:TR?= MkfXV2FPT0WU
DBTRG-05MG M{DxcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTRwNUOzNlUh|ryP MlHiV2FPT0WU
A2058 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvWTWM2OD12LkeyNVY1KM7:TR?= Ml7GV2FPT0WU
KG-1 M{\iRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEezWoRKSzVyPUSuO|M6ODhizszN Mni5V2FPT0WU
8305C M1Liemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfTTWM2OD13LkG4O|Mh|ryP NWHqZ4FzW0GQR1XS
RPMI-7951 NWXyNYkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjRNWR4UUN3ME21MlgxOjh|IN88US=> M37yVnNCVkeHUh?=
CHL-1 NEDZOotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37BZ2lEPTB;NT65O|YxOyEQvF2= MXPTRW5ITVJ?
TI-73 NIXWTlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TaU2lEPTB;Nj6wNFkxOiEQvF2= Mo\oV2FPT0WU
HT-1080 NF[xO|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTl[5NKSzVyPU[uNVA6PDZizszN MUDTRW5ITVJ?
ES5 MnzvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnGV4pOUUN3ME22MlE1QTJ2IN88US=> MVXTRW5ITVJ?
8-MG-BA MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Tw[2lEPTB;Nj6xPFEzQSEQvF2= MoThV2FPT0WU
NB7 M2jDcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnxUndoUUN3ME22MlIyOzd|IN88US=> NEniW45USU6JRWK=
H4 NFPIcm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1flZ2lEPTB;Nj6yNlQ6OyEQvF2= MYTTRW5ITVJ?
CAL-72 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXP0fYIyUUN3ME22MlQ2PDJ|IN88US=> Mnf4V2FPT0WU
HCC1806 MmrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PTSmlEPTB;Nj64NVk{OSEQvF2= MmDrV2FPT0WU
BCPAP NEHIWpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTdwMkG3OlQh|ryP NUTZT5poW0GQR1XS
LB2241-RCC M{TwU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYX4c3kzUUN3ME23MlM3QTB5IN88US=> NY\oN2R7W0GQR1XS
COLO-741 Mlf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzqSYdTUUN3ME24MlAyPjd7IN88US=> NGC5XFFUSU6JRWK=
HSC-3 MmXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33ZRmlEPTB;OD6wO|A3QCEQvF2= M1[xTXNCVkeHUh?=
SW982 NFPJTlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PYVmlEPTB;OD60NVUyPiEQvF2= M2fsPXNCVkeHUh?=
GCT NGP0OnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;PTWM2OD16Lke1N|E1KM7:TR?= MXjTRW5ITVJ?
KY821 NYO5NWsyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3uU|FkUUN3ME25MlA2OTd6IN88US=> MnvVV2FPT0WU
JVM-3 M{W1cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVL5V|VQUUN3ME25MlU3QTl7IN88US=> MnnMV2FPT0WU
RS4-11 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHsdHdKSzVyPUmuOlA1QCEQvF2= M3XTZXNCVkeHUh?=
VA-ES-BJ NVfu[ZNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzaXpZKSzVyPUGwMlAyPDlizszN NWTMPJZZW0GQR1XS
A431 M1HwN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTFyLkSyNVIh|ryP NUjiWVB5W0GQR1XS
LXF-289 NUP1V|NwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moi4TWM2OD1zMD60OVgh|ryP NFnzeZBUSU6JRWK=
SK-MEL-24 M3;RU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTFyLkiyO|Qh|ryP MVfTRW5ITVJ?
NOS-1 NFmwOohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLSPXZKSzVyPUGwMlg1PzJizszN MXzTRW5ITVJ?
KNS-62 NULPVJNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLpeVBKSzVyPUGxMlI1ODRizszN NYixe3hZW0GQR1XS
SK-HEP-1 MoPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULXemZJUUN3ME2xNU4{PTJ5IN88US=> MX;TRW5ITVJ?
A3-KAW MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTFzLkexO|gh|ryP M13HNnNCVkeHUh?=
SK-LU-1 M1vFOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzNVW1TUUN3ME2xNk4zPjV3IN88US=> Mn\5V2FPT0WU
TYK-nu NUG2eW1tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fZ[WlEPTB;MUKuN|k{OiEQvF2= MVjTRW5ITVJ?
NMC-G1 NEXrNW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\sTWM2OD1zMj62NFYzKM7:TR?= M3q5UXNCVkeHUh?=
BB65-RCC M4PqRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPwTWM2OD1zMj63NVY6KM7:TR?= NFHkZ49USU6JRWK=
QIMR-WIL NYKzPIQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTF{Lki4N|Mh|ryP MonqV2FPT0WU
D-566MG MkS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3SxN2lEPTB;MUOuPVU4PiEQvF2= NXG2UY5PW0GQR1XS
KYSE-140 NWXHSWVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fCOGlEPTB;MUSuNFc2OyEQvF2= M{jmbHNCVkeHUh?=
SCC-4 M3vHdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTF2LkOzOVkh|ryP MorSV2FPT0WU
U251 NF\XeotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPYV2V5UUN3ME2xOE45PDl{IN88US=> NFLiVnhUSU6JRWK=
D-542MG NGOzXZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\hb5dKSzVyPUG0MlkzOjJizszN Mo\sV2FPT0WU
LAMA-84 M4TqRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrxVndKSzVyPUG0Mlk6OzJizszN M4TyPHNCVkeHUh?=
NCI-H720 NEC2SHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPSTnB5UUN3ME2xOU4zPjh2IN88US=> MmDGV2FPT0WU
DEL MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vvV2lEPTB;MUWuOFI6OyEQvF2= M{LEeXNCVkeHUh?=
SBC-1 NXzOS4VHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nodWlEPTB;MUWuOFMxPSEQvF2= MlTUV2FPT0WU
ECC10 Ml\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTF3LkS0OVgh|ryP M{fmWHNCVkeHUh?=
Daoy NV7tOZZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHTTWM2OD1zNT63OlE3KM7:TR?= MYfTRW5ITVJ?
SCH M4\FU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M16xSmlEPTB;MUWuO|g{PSEQvF2= NIO4Wo1USU6JRWK=
MZ2-MEL M4DQPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHURWJrUUN3ME2xOk4xPjR4IN88US=> NX3iVFBoW0GQR1XS
CAL-12T MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnyO3dKSzVyPUG2MlQ5PjJizszN NIi0d45USU6JRWK=
KE-37 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnoWJZbUUN3ME2xOk45OTB5IN88US=> MmTrV2FPT0WU
LS-411N NILRTIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlO5TWM2OD1zNz6xNVgh|ryP NIj1[m1USU6JRWK=
NCI-H2228 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTGUIJKSzVyPUG3MlMxPzFizszN NV;5U|JEW0GQR1XS
SK-MEL-2 MlzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTF5LkS5OlUh|ryP NGrKNVFUSU6JRWK=
HN NX\XWm9QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLmcpFKSzVyPUG3MlczPDhizszN NF7ZZVhUSU6JRWK=
NCI-H1648 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4X3ZWlEPTB;MUeuPFE5KM7:TR?= NIXsWGJUSU6JRWK=
IA-LM MkDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\ZcmlEPTB;MUiuN|E4OiEQvF2= M1HKbXNCVkeHUh?=
EW-13 NYX5d3F1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3v6OmlEPTB;MUiuOVcxQCEQvF2= NX3zdVNCW0GQR1XS
YKG-1 MnfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTiTWM2OD1zOT61O|EyKM7:TR?= M{X0UXNCVkeHUh?=
KNS-81-FD M2TtXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTF7LkW4OVgh|ryP NHjvXJdUSU6JRWK=
23132-87 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTF7Lke2OFIh|ryP Moq5V2FPT0WU
NUGC-3 NInIb4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPzTWM2OD1zOT65PFg4KM7:TR?= MVHTRW5ITVJ?
5637 M13FUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTJyLkC0O|gh|ryP NEjueZRUSU6JRWK=
NCI-H1755 MnPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTJyLkS3OlQh|ryP M17TbnNCVkeHUh?=
RH-18 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3P5XmlEPTB;MkCuOVc1QCEQvF2= NHjufINUSU6JRWK=
RXF393 NV[xOHA4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTJyLk[3OVYh|ryP NInOOYNUSU6JRWK=
LU-134-A M3LRbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHsTWM2OD1{MD63NFU3KM7:TR?= MVzTRW5ITVJ?
TE-12 MoTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXwTWM2OD1{MD63NlAyKM7:TR?= NHSwU2JUSU6JRWK=
MOLT-4 M2rvc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIG2b25KSzVyPUKxMlE6OTVizszN NGSxZ29USU6JRWK=
IGR-1 NYLa[nE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PZdGlEPTB;MkGuN|c6PiEQvF2= MXzTRW5ITVJ?
HOP-92 M2CyV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3W2UGlEPTB;MkGuOFk5PyEQvF2= NFLuXI1USU6JRWK=
SK-MES-1 NXKze5F[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXndYhKSzVyPUKxMlc{QDFizszN NVLVU|JFW0GQR1XS
LU-65 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HQUGlEPTB;MkGuPFYzPCEQvF2= MmnQV2FPT0WU
MS-1 M1\tcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPKfFdKSzVyPUKyMlEzODNizszN NXr4[I1OW0GQR1XS
LoVo M1zheWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfqVXlKSzVyPUKyMlI1PCEQvF2= NUD4cHZLW0GQR1XS
A704 M2fiWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWH6XpRFUUN3ME2yNk42OTV3IN88US=> MkTvV2FPT0WU
HT-1376 M1;4Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvjTWM2OD1{Mj62NFU6KM7:TR?= MYnTRW5ITVJ?
IST-MEL1 NGmzeXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnnUIdKSzVyPUKyMlY4PTFizszN MXnTRW5ITVJ?
Ramos-2G6-4C10 NXHSTnlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnToTWM2OD1{Mj63N|Y3KM7:TR?= NGXYSWtUSU6JRWK=
T47D NVfmeHNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PLSWlEPTB;MkKuO|k4QSEQvF2= NF\K[ndUSU6JRWK=
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IST-SL1 NYPKTY5xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjIRplGUUN3ME2yOU4zPzVzIN88US=> MmSwV2FPT0WU
HH MnLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJ3LkOxPVIh|ryP NYjpe4VzW0GQR1XS
NCI-H82 NYfCb3hHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnr6TWM2OD1{NT65N|gh|ryP NFLVVFBUSU6JRWK=
SNU-449 M1HpfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTJ5LkKwNVgh|ryP NI\N[JlUSU6JRWK=
COR-L23 M1TseWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LsOmlEPTB;MkeuNlgyOyEQvF2= MWHTRW5ITVJ?
LOXIMVI MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDvVXBKSzVyPUK3MlM3QCEQvF2= NH3hW5VUSU6JRWK=
GR-ST NETtPIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M335W2lEPTB;MkeuOlcxPiEQvF2= M3ruN3NCVkeHUh?=
NCI-SNU-1 M1rNeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDne2pwUUN3ME2yO{46PDRizszN NV:zeWFFW0GQR1XS
ALL-PO NH3QV3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzpWY91UUN3ME2yPE4yPjB2IN88US=> Mo\3V2FPT0WU
ML-2 NWOyflJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rIfmlEPTB;MkiuNlgyPCEQvF2= NWmxSmN1W0GQR1XS
HOP-62 NU\l[41wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[4TWM2OD1{OD63NVMh|ryP MVzTRW5ITVJ?
EGI-1 NGXpfIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzGO5ZWUUN3ME2yPE45QDR3IN88US=> NFfVe4JUSU6JRWK=
TCCSUP MorXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTJ6LkmyO|Ih|ryP NVnWTGtkW0GQR1XS
LB996-RCC M4f0cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTJ7LkW2PFIh|ryP NFr4eJhUSU6JRWK=
LCLC-97TM1 MkDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PxXmlEPTB;M{KuNVk3PCEQvF2= MoLOV2FPT0WU
NCI-H1304 MkCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTN{LkOzNFEh|ryP NFjxV5JUSU6JRWK=
KP-N-YS MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTN{LkW5O|Mh|ryP MkjrV2FPT0WU
NCI-H1770 MonsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;rRWlEPTB;M{OuNVY1QCEQvF2= M2XTe3NCVkeHUh?=
EM-2 NX2ydnBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvwcms4UUN3ME2zN{43PTB2IN88US=> MlXrV2FPT0WU
ChaGo-K-1 NFvzOJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfubY1KSzVyPUOzMlczOzZizszN NUXp[WQ1W0GQR1XS
ACHN M1;PPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTN|LkizPFUh|ryP NECzW3lUSU6JRWK=
MN-60 M3vPPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTN|Lki1OFQh|ryP NFPsWXhUSU6JRWK=
EW-18 MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TaU2lEPTB;M{OuPFk4OSEQvF2= M3[weHNCVkeHUh?=
KGN MnzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTNSGxWUUN3ME2zOU44Ojl{IN88US=> M4DvcnNCVkeHUh?=
U031 MoTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7oTWM2OD1|NT64NVMzKM7:TR?= MWXTRW5ITVJ?
HMV-II NXTzb4Y2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTN4LkC3O|Qh|ryP NIPW[ZFUSU6JRWK=
L-363 M164dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTN5Lk[0OVUh|ryP NIW0fXRUSU6JRWK=
NCI-H1155 NEDzfVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnz0TWM2OD1|OD6wNFE2KM7:TR?= MWrTRW5ITVJ?
NCI-H1793 M4DnVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTN6LkGwNlYh|ryP MlzLV2FPT0WU
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KP-N-YN MmjrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTRyLkSyPFUh|ryP NUfIenJTW0GQR1XS
T98G MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLBNmNoUUN3ME20NE41QTV5IN88US=> NIXtdJBUSU6JRWK=
HGC-27 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETjXGNKSzVyPUSzMlI4PCEQvF2= NFTid5dUSU6JRWK=
NCI-H1092 NXr3TVJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LXOWlEPTB;NEOuNlg6PSEQvF2= MWXTRW5ITVJ?
KARPAS-299 MlvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjvZmZWUUN3ME20N{4{ODdzIN88US=> M{nF[3NCVkeHUh?=
LB1047-RCC MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnWzTWM2OD12ND65PVU6KM7:TR?= MVzTRW5ITVJ?
786-0 NXfpNXhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\6TWM2OD12NT62OUDPxE1? MnXnV2FPT0WU
HCC2157 NVLEN|BpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPMOYNKSzVyPUS2MlA{PTlizszN NV3td5RKW0GQR1XS
NY MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPZTWM2OD12Nj6xO|c5KM7:TR?= MlixV2FPT0WU
EFM-19 NES3SpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLqeJdMUUN3ME20Ok44PTN|IN88US=> NFfXSWlUSU6JRWK=
EW-16 NEnHcnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm[3TWM2OD12Nj63PFA3KM7:TR?= MmfPV2FPT0WU
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HT-29 NETIXYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEP1Z|ZKSzVyPUS3Mlg4QTJizszN M4fGRXNCVkeHUh?=
LN-405 NVjN[Yw5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnYSXlWUUN3ME20PE4xQDJ5IN88US=> M3vK[HNCVkeHUh?=
NCI-H727 M3K3fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEW2RXZKSzVyPUS4Mlc4OjZizszN MlvUV2FPT0WU
D-502MG MlLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPQTWM2OD12OD65Olc3KM7:TR?= MXjTRW5ITVJ?
GMS-10 NV\IVHozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWqyd4xHUUN3ME20PU4zQTd2IN88US=> NF3Pd2VUSU6JRWK=
MEL-JUSO M1PmeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELvU4VKSzVyPUS5MlM1PyEQvF2= MVzTRW5ITVJ?

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 83 mg/mL (200.56 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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)

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。

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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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