PLX-4720

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。

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電話番号: + 81 3-5632-9610mail@cosmobio.co.jp

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 MoiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGe4cI1KSzVyPUCuNFc1PTdizszN NH2wU4VUSU6JRWK=
EoL-1-cell MlToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjsVVRKSzVyPUCuNVQyPjZizszN MoXEV2FPT0WU
C32 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHv4OYtKSzVyPUCuNVUyOzFizszN MojJV2FPT0WU
M14 NGT2epFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTBwMkG3OVch|ryP NXHaUlJlW0GQR1XS
CP50-MEL-B MnSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTBwMkm3PFQh|ryP MVrTRW5ITVJ?
A101D NUTqbY0zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3lWnR4UUN3ME2wMlMzPTh7IN88US=> M4O5c3NCVkeHUh?=
G-361 MojHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rPTWlEPTB;MD6zOFY{PyEQvF2= Mn[3V2FPT0WU
HT-144 NYrrRmp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HPc2lEPTB;MD6zOlMzQSEQvF2= M2HEOnNCVkeHUh?=
ACN MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHoTWM2OD1yLkO4OFc4KM7:TR?= NH3BNplUSU6JRWK=
COLO-829 NYDVTXo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTaR4dqUUN3ME2wMlM5QTZ6IN88US=> MXHTRW5ITVJ?
MEL-HO M{LVbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnsbIlKSzVyPUCuOFEyPzlizszN MVfTRW5ITVJ?
SH-4 NYHKd4hKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHQeFU5UUN3ME2wMlQyPDJ{IN88US=> MmrFV2FPT0WU
SK-MEL-3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYS4d4hmUUN3ME2wMlUyPTZ6IN88US=> NYnocJU{W0GQR1XS
A375 NIDuWpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIG3RnRKSzVyPUCuOlc{PTlizszN MXvTRW5ITVJ?
MMAC-SF MlnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTBwNki2NVQh|ryP NV3NeYJHW0GQR1XS
BHT-101 NFfMZ3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;PdGlEPTB;MD63NFcxOiEQvF2= MUXTRW5ITVJ?
K5 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHTeoE3UUN3ME2wMlc3OTR6IN88US=> NFO1eWhUSU6JRWK=
BV-173 NFnu[nVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfMTWM2OD1yLke5OlQ1KM7:TR?= NH24bmlUSU6JRWK=
RVH-421 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlG2TWM2OD1yLki2O|k3KM7:TR?= NIjxfG5USU6JRWK=
HCC2218 MoPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PFS2lEPTB;MD64O|g1PCEQvF2= NXv1TVl{W0GQR1XS
WM-115 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{exUGlEPTB;MD64PFY6OiEQvF2= MknYV2FPT0WU
SK-MEL-28 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jTS2lEPTB;MT6wOFU3QSEQvF2= MmewV2FPT0WU
COLO-679 NXnSfWVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTFwMUC0OlQh|ryP M3qyeHNCVkeHUh?=
MZ7-mel NU\aV4I{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDRWo9KSzVyPUGuNVQ6PjNizszN NEH3NXJUSU6JRWK=
SK-MEL-30 Mm\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV32NGlnUUN3ME2xMlM{Ozh4IN88US=> NYCxOJhzW0GQR1XS
NCI-H209 NU\MXWVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF2yXnZKSzVyPUGuOlA5PiEQvF2= NFTB[WtUSU6JRWK=
HTC-C3 NUj1dpVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnyb5FVUUN3ME2xMlY3Ojl2IN88US=> NYfHRotYW0GQR1XS
KARPAS-45 MnPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1O0bmlEPTB;Mj6wOFk4QCEQvF2= NW\QWFVGW0GQR1XS
NCI-SNU-5 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3:0O2lEPTB;Mj6xNVk3QSEQvF2= MlnWV2FPT0WU
KP-4 MmLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nBOWlEPTB;Mj6zNFc5PyEQvF2= NXHRV5g4W0GQR1XS
PA-1 M{LHR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIT3dY9KSzVyPUKuO|I3PzNizszN NELOUJhUSU6JRWK=
HuO-3N1 NUTESItqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTJwOEe5OFYh|ryP MYHTRW5ITVJ?
NCI-H358 MoLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVz5VWtUUUN3ME2yMlkzOjN{IN88US=> MoO1V2FPT0WU
CTB-1 NVPaSWhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXSd2U{UUN3ME2zMlQxOTd4IN88US=> MlfZV2FPT0WU
697 NVz3NJM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHyxdVlKSzVyPUOuOVUzPjZizszN M1zUd3NCVkeHUh?=
CP66-MEL NYPmdnRCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\3TWM2OD12LkG1PVI4KM7:TR?= NXvWe45FW0GQR1XS
NB13 MnzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvZWVRWUUN3ME20MlQ6OTd7IN88US=> NFftXVlUSU6JRWK=
DBTRG-05MG NEXEdnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTRwNUOzNlUh|ryP NWXMdohTW0GQR1XS
A2058 NEKwe|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\5TWM2OD12LkeyNVY1KM7:TR?= M4GwdnNCVkeHUh?=
KG-1 M4DMfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTRwN{O5NFgh|ryP MV\TRW5ITVJ?
8305C MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUm0SlcyUUN3ME21MlE5PzNizszN NFf2emRUSU6JRWK=
RPMI-7951 NXzYSoRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFOzOG1KSzVyPUWuPFAzQDNizszN MlL3V2FPT0WU
CHL-1 NWe4XHRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXUTWM2OD13Lkm3OlA{KM7:TR?= MU\TRW5ITVJ?
TI-73 M4LnV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDDTWM2OD14LkCwPVAzKM7:TR?= MmLzV2FPT0WU
HT-1080 MmKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPzTWM2OD14LkGwPVQ3KM7:TR?= MWLTRW5ITVJ?
ES5 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWW2bZBFUUN3ME22MlE1QTJ2IN88US=> M13nZ3NCVkeHUh?=
8-MG-BA MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjjSYJFUUN3ME22MlE5OTJ7IN88US=> NVrhVGJOW0GQR1XS
NB7 Mor5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHoTWM2OD14LkKxN|c{KM7:TR?= MUjTRW5ITVJ?
H4 MmnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjqRY1UUUN3ME22MlIzPDl|IN88US=> M1u2SnNCVkeHUh?=
CAL-72 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrBR4FCUUN3ME22MlQ2PDJ|IN88US=> MnPXV2FPT0WU
HCC1806 NV:xTHRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;w[5FyUUN3ME22MlgyQTNzIN88US=> M2nmWXNCVkeHUh?=
BCPAP MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXkTWM2OD15LkKxO|Y1KM7:TR?= NX7h[lRiW0GQR1XS
LB2241-RCC NIPreYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHWzOmtKSzVyPUeuN|Y6ODdizszN MU\TRW5ITVJ?
COLO-741 MmfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHsTWM2OD16LkCxOlc6KM7:TR?= NEjUXGNUSU6JRWK=
HSC-3 NVPFeXFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXVTWM2OD16LkC3NFY5KM7:TR?= M1HIZXNCVkeHUh?=
SW982 NV34V5VkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHu2TmNKSzVyPUiuOFE2OTZizszN NX\YPFF3W0GQR1XS
GCT NV7rWmltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPkPW5KSzVyPUiuO|U{OTRizszN MlTrV2FPT0WU
KY821 NYX3UJlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTlwMEWxO|gh|ryP MoPwV2FPT0WU
JVM-3 NVmyTJdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTlwNU[5PVkh|ryP MX7TRW5ITVJ?
RS4-11 MoXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnewTWM2OD17Lk[wOFgh|ryP M2PjeXNCVkeHUh?=
VA-ES-BJ NWnKOZJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHf1W5hKSzVyPUGwMlAyPDlizszN M2T5enNCVkeHUh?=
A431 NVS3cGp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDRS5dKSzVyPUGwMlQzOTJizszN M1vOd3NCVkeHUh?=
LXF-289 NI[zbZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF75NZBKSzVyPUGwMlQ2QCEQvF2= M4fxOXNCVkeHUh?=
SK-MEL-24 Mn3CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7mSVhDUUN3ME2xNE45Ojd2IN88US=> NW\DUXZEW0GQR1XS
NOS-1 NULwbItDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTFyLki0O|Ih|ryP NYLQR5hJW0GQR1XS
KNS-62 Mn7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTFzLkK0NFQh|ryP Mn7pV2FPT0WU
SK-HEP-1 MoriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojETWM2OD1zMT6zOVI4KM7:TR?= M3fQUnNCVkeHUh?=
A3-KAW M{SyfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGqxUmdKSzVyPUGxMlcyPzhizszN M3;HNXNCVkeHUh?=
SK-LU-1 NXXRflU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnHW|BNUUN3ME2xNk4zPjV3IN88US=> M33uenNCVkeHUh?=
TYK-nu Mn[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTF{LkO5N|Ih|ryP MXLTRW5ITVJ?
NMC-G1 MnXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHyyXoVKSzVyPUGyMlYxPjJizszN MojIV2FPT0WU
BB65-RCC NV7QcYlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37PbGlEPTB;MUKuO|E3QSEQvF2= MVzTRW5ITVJ?
QIMR-WIL NGrVcXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV:1VmdtUUN3ME2xNk45QDN|IN88US=> NYm2U3c{W0GQR1XS
D-566MG M2rIbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHH2UWtKSzVyPUGzMlk2PzZizszN NGnsSGRUSU6JRWK=
KYSE-140 NHPmcHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTF2LkC3OVMh|ryP NVfMXVJjW0GQR1XS
SCC-4 M{H4OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTF2LkOzOVkh|ryP MUnTRW5ITVJ?
U251 Mlr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTF2Lki0PVIh|ryP MV\TRW5ITVJ?
D-542MG NF\kWVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHlTWM2OD1zND65NlIzKM7:TR?= MnHOV2FPT0WU
LAMA-84 MoLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTF2Lkm5N|Ih|ryP NXL5OIpiW0GQR1XS
NCI-H720 MoLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDuWYlSUUN3ME2xOU4zPjh2IN88US=> NHjSRndUSU6JRWK=
DEL MkPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDLWHNKSzVyPUG1MlQzQTNizszN NFrVUpFUSU6JRWK=
SBC-1 NHnifFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7rTWM2OD1zNT60N|A2KM7:TR?= NHnXZ41USU6JRWK=
ECC10 NGn5[olIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\4WVVwUUN3ME2xOU41PDV6IN88US=> NUDMV5NvW0GQR1XS
Daoy MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPUTWM2OD1zNT63OlE3KM7:TR?= M1nnNHNCVkeHUh?=
SCH NGq4XmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn64TWM2OD1zNT63PFM2KM7:TR?= MlHtV2FPT0WU
MZ2-MEL NV7wW5MzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkP2TWM2OD1zNj6wOlQ3KM7:TR?= M{jqe3NCVkeHUh?=
CAL-12T Mlm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn:1TWM2OD1zNj60PFYzKM7:TR?= MXTTRW5ITVJ?
KE-37 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\iTWM2OD1zNj64NVA4KM7:TR?= NH;mV3NUSU6JRWK=
LS-411N MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHybHV1UUN3ME2xO{4yOThizszN NG\4Uo5USU6JRWK=
NCI-H2228 MkXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTF5LkOwO|Eh|ryP NWm3W3FoW0GQR1XS
SK-MEL-2 M4\sS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\sT2lEPTB;MUeuOFk3PSEQvF2= NFrlN2RUSU6JRWK=
HN MmfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTF5LkeyOFgh|ryP MmjzV2FPT0WU
NCI-H1648 MknMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPwTWM2OD1zNz64NVgh|ryP M17wUnNCVkeHUh?=
IA-LM MojIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFS3TYJKSzVyPUG4MlMyPzJizszN Ml3SV2FPT0WU
EW-13 MknNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULD[o1uUUN3ME2xPE42PzB6IN88US=> NWLyNG5FW0GQR1XS
YKG-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\QemlKSzVyPUG5MlU4OTFizszN M{LaOnNCVkeHUh?=
KNS-81-FD MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\aSI5KSzVyPUG5MlU5PThizszN MnXVV2FPT0WU
23132-87 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrhSphKSzVyPUG5Mlc3PDJizszN NWTEeGI2W0GQR1XS
NUGC-3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;NUmRVUUN3ME2xPU46QDh5IN88US=> NEe1flJUSU6JRWK=
5637 MnfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2j3OGlEPTB;MkCuNFQ4QCEQvF2= NF7hXIhUSU6JRWK=
NCI-H1755 Mn3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\4O4dKSzVyPUKwMlQ4PjRizszN NULQfm1vW0GQR1XS
RH-18 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fZZWlEPTB;MkCuOVc1QCEQvF2= NUn1dZp1W0GQR1XS
RXF393 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXTTWM2OD1{MD62O|U3KM7:TR?= NXvhXmt{W0GQR1XS
LU-134-A M1TVcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDvTWM2OD1{MD63NFU3KM7:TR?= NU\0ZYM6W0GQR1XS
TE-12 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;ocmI3UUN3ME2yNE44OjBzIN88US=> M3;5cHNCVkeHUh?=
MOLT-4 NXT4cIJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTJzLkG5NVUh|ryP NXHLcVZ3W0GQR1XS
IGR-1 NYmwRWs4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPwSXlKSzVyPUKxMlM4QTZizszN NWTtc5ZZW0GQR1XS
HOP-92 MoWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDxSGFKSzVyPUKxMlQ6QDdizszN MnzGV2FPT0WU
SK-MES-1 NWewS4NkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlqzTWM2OD1{MT63N|gyKM7:TR?= NVHiWZd7W0GQR1XS
LU-65 M3TNWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnBT5p3UUN3ME2yNU45PjJ2IN88US=> NW\vU|B5W0GQR1XS
MS-1 M1TzWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjQcVdKSzVyPUKyMlEzODNizszN MmntV2FPT0WU
LoVo M376Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHXSIFIUUN3ME2yNk4zPDRizszN MWLTRW5ITVJ?
A704 NWe2RpBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;UPXgyUUN3ME2yNk42OTV3IN88US=> Mm\FV2FPT0WU
HT-1376 M2O4PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moj2TWM2OD1{Mj62NFU6KM7:TR?= NWH6fYJrW0GQR1XS
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NCI-H526 NFnjc2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrDTWM2OD1{NT6wNFI{KM7:TR?= M2DXb3NCVkeHUh?=
IST-SL1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXt[lJKSzVyPUK1MlI4PTFizszN MWfTRW5ITVJ?
HH NXjnOHFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrlRo54UUN3ME2yOU4{OTl{IN88US=> NXTyTnBFW0GQR1XS
NCI-H82 MmrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NESy[5dKSzVyPUK1Mlk{QCEQvF2= NYS1VZZOW0GQR1XS
SNU-449 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTJ5LkKwNVgh|ryP NIfITWdUSU6JRWK=
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LOXIMVI NXfLR2xUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTJ5LkO2PEDPxE1? MYTTRW5ITVJ?
GR-ST MoL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnftTWM2OD1{Nz62O|A3KM7:TR?= M{DFNHNCVkeHUh?=
NCI-SNU-1 M{G3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjIZ4ptUUN3ME2yO{46PDRizszN MkXIV2FPT0WU
ALL-PO MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnDeIpKSzVyPUK4MlE3ODRizszN MonGV2FPT0WU
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HOP-62 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{T2VmlEPTB;MkiuO|E{KM7:TR?= NH;3cXRUSU6JRWK=
EGI-1 NHjlWldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDFRXBTUUN3ME2yPE45QDR3IN88US=> MVPTRW5ITVJ?
TCCSUP M2L1fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL2TWM2OD1{OD65NlczKM7:TR?= NU\rTmFCW0GQR1XS
LB996-RCC NUnZOohJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NET6WJhKSzVyPUK5MlU3QDJizszN NG[4SVFUSU6JRWK=
LCLC-97TM1 MoXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTN{LkG5OlQh|ryP MmrJV2FPT0WU
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KP-N-YS NH\iOHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33MNWlEPTB;M{KuOVk4OyEQvF2= NHLxbVRUSU6JRWK=
NCI-H1770 NH\PT4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUT1[VBOUUN3ME2zN{4yPjR6IN88US=> NHSwR41USU6JRWK=
EM-2 NUC1UIg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2j1VmlEPTB;M{OuOlUxPCEQvF2= MW\TRW5ITVJ?
ChaGo-K-1 NHHsPYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLJVYpKSzVyPUOzMlczOzZizszN MonyV2FPT0WU
ACHN MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjOSWhzUUN3ME2zN{45Ozh3IN88US=> NV[yd2FIW0GQR1XS
MN-60 MnT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zXRWlEPTB;M{OuPFU1PCEQvF2= MVPTRW5ITVJ?
EW-18 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHqTlNUUUN3ME2zN{45QTdzIN88US=> NVjoVHFFW0GQR1XS
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U031 NU\tcXB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTN3LkixN|Ih|ryP NWHlZm46W0GQR1XS
HMV-II MoX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlznTWM2OD1|Nj6wO|c1KM7:TR?= NGLsNFlUSU6JRWK=
L-363 MnvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorBTWM2OD1|Nz62OFU2KM7:TR?= NWfSUXY3W0GQR1XS
NCI-H1155 MknnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrVZZlMUUN3ME2zPE4xODF3IN88US=> NGXtbHRUSU6JRWK=
NCI-H1793 NUW3cWdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\pcHpKSzVyPUO4MlExOjZizszN NVi5UoVKW0GQR1XS
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HGC-27 NIXJ[JNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPPb2FKSzVyPUSzMlI4PCEQvF2= NXruN25KW0GQR1XS
NCI-H1092 NILF[pdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;pfohCUUN3ME20N{4zQDl3IN88US=> MYHTRW5ITVJ?
KARPAS-299 NV7zSIlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1n2fGlEPTB;NEOuN|A4OSEQvF2= NX;GUo5HW0GQR1XS
LB1047-RCC Ml\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTR2Lkm5OVkh|ryP NXXORnlrW0GQR1XS
786-0 NHG4dHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7MTWM2OD12NT62OUDPxE1? MXPTRW5ITVJ?
HCC2157 M4ntUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrhTWM2OD12Nj6wN|U6KM7:TR?= MXjTRW5ITVJ?
NY NGfIWHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjPTWM2OD12Nj6xO|c5KM7:TR?= M2D6fnNCVkeHUh?=
EFM-19 NUX1V2ppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTR4Lke1N|Mh|ryP M17DfXNCVkeHUh?=
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HT-29 MnvXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTR5Lki3PVIh|ryP NV\2XldTW0GQR1XS
LN-405 NYXVSI5JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\IVWlEPTB;NEiuNFgzPyEQvF2= NGnISplUSU6JRWK=
NCI-H727 NW\Kb2llT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTR6Lke3NlYh|ryP MYXTRW5ITVJ?
D-502MG NUHjPVZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTSTWM2OD12OD65Olc3KM7:TR?= NVfIVZNxW0GQR1XS
GMS-10 MoXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmO0TWM2OD12OT6yPVc1KM7:TR?= NIPjXmFUSU6JRWK=
MEL-JUSO NWDleopST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDHb2FKSzVyPUS5MlM1PyEQvF2= MUjTRW5ITVJ?

... 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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