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 NIrldllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknDTWM2OD1yLkC3OFU4KM7:TR?= NXzVVHdUW0GQR1XS
EoL-1-cell MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIWxT3FKSzVyPUCuNVQyPjZizszN MVTTRW5ITVJ?
C32 Mo\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LsXmlEPTB;MD6xOVE{OSEQvF2= MYLTRW5ITVJ?
M14 M3\qTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3nd3JLUUN3ME2wMlIyPzV5IN88US=> MXPTRW5ITVJ?
CP50-MEL-B NHmzfpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVew[WV2UUN3ME2wMlI6Pzh2IN88US=> Ml\rV2FPT0WU
A101D MnzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwM{K1PFkh|ryP NYnOV2QzW0GQR1XS
G-361 NX7iXFZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjKeXJjUUN3ME2wMlM1PjN5IN88US=> M{ToS3NCVkeHUh?=
HT-144 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\lTWM2OD1yLkO2N|I6KM7:TR?= NWDPeJJyW0GQR1XS
ACN NUDrb2V4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH[yRmZKSzVyPUCuN|g1PzdizszN M4PuTHNCVkeHUh?=
COLO-829 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rXSmlEPTB;MD6zPFk3QCEQvF2= M2qwd3NCVkeHUh?=
MEL-HO NX3PSGlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTBwNEGxO|kh|ryP MkPYV2FPT0WU
SH-4 NVvkd4U1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDQU2FOUUN3ME2wMlQyPDJ{IN88US=> NF[xZ4xUSU6JRWK=
SK-MEL-3 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTBwNUG1Olgh|ryP NXfNW5pvW0GQR1XS
A375 M1[0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnJXWYyUUN3ME2wMlY4OzV7IN88US=> NXHMT2hEW0GQR1XS
MMAC-SF MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTBwNki2NVQh|ryP MoiwV2FPT0WU
BHT-101 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIS3e3RKSzVyPUCuO|A4ODJizszN MUXTRW5ITVJ?
K5 NIP3TWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\PcoxKSzVyPUCuO|YyPDhizszN Ml3WV2FPT0WU
BV-173 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzxZo92UUN3ME2wMlc6PjR2IN88US=> MmXmV2FPT0WU
RVH-421 NYXNR3RIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTBwOE[3PVYh|ryP MYDTRW5ITVJ?
HCC2218 M2fUcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTZTWM2OD1yLki3PFQ1KM7:TR?= MnrQV2FPT0WU
WM-115 M3H6PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHoXY5KSzVyPUCuPFg3QTJizszN MVfTRW5ITVJ?
SK-MEL-28 NHrTOIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTFwMES1Olkh|ryP NGXEWHhUSU6JRWK=
COLO-679 NGPOOFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\JTWM2OD1zLkGwOFY1KM7:TR?= MWjTRW5ITVJ?
MZ7-mel M3[2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;5WGRKSzVyPUGuNVQ6PjNizszN M4Ttd3NCVkeHUh?=
SK-MEL-30 Moe5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITRSJhKSzVyPUGuN|M{QDZizszN M{\t[HNCVkeHUh?=
NCI-H209 M1qzPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYX2[ZJIUUN3ME2xMlYxQDZizszN NG\1WGlUSU6JRWK=
HTC-C3 MoPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjvTWM2OD1zLk[2Nlk1KM7:TR?= NWjZdXRCW0GQR1XS
KARPAS-45 M1jRWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7zTWM2OD1{LkC0PVc5KM7:TR?= M3W4VXNCVkeHUh?=
NCI-SNU-5 NVPyfYF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTJwMUG5Olkh|ryP NVz3[Wx{W0GQR1XS
KP-4 MnS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTJwM{C3PFch|ryP MmnXV2FPT0WU
PA-1 NXjLPZJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnz6TWM2OD1{LkeyOlc{KM7:TR?= MXXTRW5ITVJ?
HuO-3N1 NIDJOpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTJwOEe5OFYh|ryP NEjHO4dUSU6JRWK=
NCI-H358 NXqxb4xbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTJwOUKyN|Ih|ryP NH3PZ5BUSU6JRWK=
CTB-1 M2GzdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWqzfnhPUUN3ME2zMlQxOTd4IN88US=> MULTRW5ITVJ?
697 NVjXTZNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXn3SWFpUUN3ME2zMlU2OjZ4IN88US=> M4PLTnNCVkeHUh?=
CP66-MEL NX7STGd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHGV2RKSzVyPUSuNVU6OjdizszN M1vGbnNCVkeHUh?=
NB13 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDZ[3o2UUN3ME20MlQ6OTd7IN88US=> MUHTRW5ITVJ?
DBTRG-05MG MkTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfHbmdZUUN3ME20MlU{OzJ3IN88US=> NHqwPFBUSU6JRWK=
A2058 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rQSGlEPTB;ND63NlE3PCEQvF2= NG\ROlRUSU6JRWK=
KG-1 Mm[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTRwN{O5NFgh|ryP NE\hfppUSU6JRWK=
8305C MlH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHKPXd6UUN3ME21MlE5PzNizszN Mme5V2FPT0WU
RPMI-7951 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfRPFVIUUN3ME21MlgxOjh|IN88US=> MV7TRW5ITVJ?
CHL-1 MnLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzu[XU3UUN3ME21Mlk4PjB|IN88US=> MX7TRW5ITVJ?
TI-73 MnzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXZXHREUUN3ME22MlAxQTB{IN88US=> M4XVN3NCVkeHUh?=
HT-1080 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnGd3NKSzVyPU[uNVA6PDZizszN NEfQfodUSU6JRWK=
ES5 M4DCZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGWySJZKSzVyPU[uNVQ6OjRizszN NHLjUWhUSU6JRWK=
8-MG-BA MoTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\4ZWlEPTB;Nj6xPFEzQSEQvF2= NFX0bFlUSU6JRWK=
NB7 MmfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fIcGlEPTB;Nj6yNVM4OyEQvF2= MUDTRW5ITVJ?
H4 NELKcFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjkXpNKSzVyPU[uNlI1QTNizszN MkPqV2FPT0WU
CAL-72 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEe1O5BKSzVyPU[uOFU1OjNizszN NILDSpBUSU6JRWK=
HCC1806 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknITWM2OD14LkixPVMyKM7:TR?= MWDTRW5ITVJ?
BCPAP NWftRm5QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTdwMkG3OlQh|ryP Moj4V2FPT0WU
LB2241-RCC NFu0W25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLETWM2OD15LkO2PVA4KM7:TR?= MlizV2FPT0WU
COLO-741 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRThwMEG2O|kh|ryP MXHTRW5ITVJ?
HSC-3 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfu[2hKSzVyPUiuNFcxPjhizszN NWPWUIpKW0GQR1XS
SW982 M4nkc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRThwNEG1NVYh|ryP NVTxfpV5W0GQR1XS
GCT Ml7OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDwV3NVUUN3ME24Mlc2OzF2IN88US=> Mo\uV2FPT0WU
KY821 MoT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fCS2lEPTB;OT6wOVE4QCEQvF2= NGHNZZNUSU6JRWK=
JVM-3 NXm1SHlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTtXIlWUUN3ME25MlU3QTl7IN88US=> Mlf1V2FPT0WU
RS4-11 Mm\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml20TWM2OD17Lk[wOFgh|ryP NXzOWVNQW0GQR1XS
VA-ES-BJ M4P6U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fn[mlEPTB;MUCuNFE1QSEQvF2= M4XrW3NCVkeHUh?=
A431 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjVV2RKSzVyPUGwMlQzOTJizszN M1fpWHNCVkeHUh?=
LXF-289 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTFyLkS1PEDPxE1? MoDpV2FPT0WU
SK-MEL-24 MnHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\SdWlEPTB;MUCuPFI4PCEQvF2= NYn1W|BkW0GQR1XS
NOS-1 NYTPfm1KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTFyLki0O|Ih|ryP MmT5V2FPT0WU
KNS-62 M2ey[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmO5TWM2OD1zMT6yOFA1KM7:TR?= M{LYUXNCVkeHUh?=
SK-HEP-1 MnrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTxeXBvUUN3ME2xNU4{PTJ5IN88US=> MYnTRW5ITVJ?
A3-KAW M3jIPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrCTWM2OD1zMT63NVc5KM7:TR?= MnrLV2FPT0WU
SK-LU-1 MlL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\XV2lEPTB;MUKuNlY2PSEQvF2= NWrNcGtjW0GQR1XS
TYK-nu MlLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLaTWM2OD1zMj6zPVMzKM7:TR?= M3r3Z3NCVkeHUh?=
NMC-G1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFGyU2FKSzVyPUGyMlYxPjJizszN MYDTRW5ITVJ?
BB65-RCC M2[zO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW[5epdJUUN3ME2xNk44OTZ7IN88US=> MnzOV2FPT0WU
QIMR-WIL M1KzSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHCTWM2OD1zMj64PFM{KM7:TR?= Mn20V2FPT0WU
D-566MG MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTF|Lkm1O|Yh|ryP MXXTRW5ITVJ?
KYSE-140 NHjze|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGq3SpRKSzVyPUG0MlA4PTNizszN MmiwV2FPT0WU
SCC-4 NHXtSnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\4fVNzUUN3ME2xOE4{OzV7IN88US=> NG\TXo1USU6JRWK=
U251 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTF2Lki0PVIh|ryP NHnDN5VUSU6JRWK=
D-542MG MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTF2LkmyNlIh|ryP MWfTRW5ITVJ?
LAMA-84 MkTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTHTWM2OD1zND65PVMzKM7:TR?= MXXTRW5ITVJ?
NCI-H720 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTF3LkK2PFQh|ryP NFHkRZpUSU6JRWK=
DEL Mk\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTGXIFNUUN3ME2xOU41Ojl|IN88US=> MYDTRW5ITVJ?
SBC-1 NHfRbmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTF3LkSzNFUh|ryP NX;yUopHW0GQR1XS
ECC10 M3vTbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTF3LkS0OVgh|ryP NYPjRmRwW0GQR1XS
Daoy NFvmSpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTF3Lke2NVYh|ryP M4\2VHNCVkeHUh?=
SCH MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFi2eWxKSzVyPUG1Mlc5OzVizszN NX\nXIk4W0GQR1XS
MZ2-MEL NFjK[ZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTF4LkC2OFYh|ryP M4XKenNCVkeHUh?=
CAL-12T MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTF4LkS4OlIh|ryP M{XrdnNCVkeHUh?=
KE-37 NFW1ZWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4T1OWlEPTB;MU[uPFExPyEQvF2= NIqySJRUSU6JRWK=
LS-411N NFfSSVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NImxO2NKSzVyPUG3MlEyQCEQvF2= NXfETI43W0GQR1XS
NCI-H2228 Mm\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPqeW5KSzVyPUG3MlMxPzFizszN MmLHV2FPT0WU
SK-MEL-2 MlPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTF5LkS5OlUh|ryP NEnN[pVUSU6JRWK=
HN NEPNdmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\1eWlEPTB;MUeuO|I1QCEQvF2= NIO3OmVUSU6JRWK=
NCI-H1648 NITHcHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\t[mlEPTB;MUeuPFE5KM7:TR?= NFj2dXFUSU6JRWK=
IA-LM NHfsfJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnN[lhKSzVyPUG4MlMyPzJizszN M2GzZnNCVkeHUh?=
EW-13 MmXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITyXoVKSzVyPUG4MlU4ODhizszN MVzTRW5ITVJ?
YKG-1 NVv5RZhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGn1bmtKSzVyPUG5MlU4OTFizszN MYnTRW5ITVJ?
KNS-81-FD M3H5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHhVlhIUUN3ME2xPU42QDV6IN88US=> MXHTRW5ITVJ?
23132-87 MnTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHRb4ZuUUN3ME2xPU44PjR{IN88US=> MVPTRW5ITVJ?
NUGC-3 NWHGdm12T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPrVGs6UUN3ME2xPU46QDh5IN88US=> NV3GZ4djW0GQR1XS
5637 NVyxPJA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTJyLkC0O|gh|ryP M2G1UHNCVkeHUh?=
NCI-H1755 M3vhPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTJyLkS3OlQh|ryP MVfTRW5ITVJ?
RH-18 Mnj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLoTWM2OD1{MD61O|Q5KM7:TR?= MoH6V2FPT0WU
RXF393 M2Hu[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\WTWM2OD1{MD62O|U3KM7:TR?= NHfoSodUSU6JRWK=
LU-134-A NGr2RWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\JdFRKSzVyPUKwMlcxPTZizszN NXS1bII1W0GQR1XS
TE-12 NILVRmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPo[YZvUUN3ME2yNE44OjBzIN88US=> M{O5bnNCVkeHUh?=
MOLT-4 M3\uTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlv4TWM2OD1{MT6xPVE2KM7:TR?= NUjoPWpqW0GQR1XS
IGR-1 M3nQWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTJzLkO3PVYh|ryP MUTTRW5ITVJ?
HOP-92 M{DHVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzWVndEUUN3ME2yNU41QTh5IN88US=> MV\TRW5ITVJ?
SK-MES-1 NITmfXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7GTpM5UUN3ME2yNU44OzhzIN88US=> NI[5R|ZUSU6JRWK=
LU-65 MoPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mln3TWM2OD1{MT64OlI1KM7:TR?= MXjTRW5ITVJ?
MS-1 MnPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjXTWM2OD1{Mj6xNlA{KM7:TR?= MkD2V2FPT0WU
LoVo MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPJTWM2OD1{Mj6yOFQh|ryP MX\TRW5ITVJ?
A704 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTJ{LkWxOVUh|ryP NH3BUYRUSU6JRWK=
HT-1376 NUTjcI1uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVmzOXE6UUN3ME2yNk43ODV7IN88US=> M1P5WnNCVkeHUh?=
IST-MEL1 M2[3NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTJ{Lk[3OVEh|ryP NXOzT|Q{W0GQR1XS
Ramos-2G6-4C10 M2\K[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mly1TWM2OD1{Mj63N|Y3KM7:TR?= NIPZXFRUSU6JRWK=
T47D NYjB[4ZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTJ{Lke5O|kh|ryP Mn7CV2FPT0WU
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NY MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTR4LkG3O|gh|ryP NFnleIVUSU6JRWK=
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... 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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