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 MlvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fPS2lEPTB;MD6wO|Q2PyEQvF2= M{PWdXNCVkeHUh?=
EoL-1-cell NIfPXnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwMUSxOlYh|ryP NYHNUlBuW0GQR1XS
C32 NUiydXBmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPu[lBmUUN3ME2wMlE2OTNzIN88US=> M1HOb3NCVkeHUh?=
M14 M4n6[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHZXodKSzVyPUCuNlE4PTdizszN NEfHdWZUSU6JRWK=
CP50-MEL-B M{XXTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nvbmlEPTB;MD6yPVc5PCEQvF2= NGfvdpdUSU6JRWK=
A101D M{D2W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmruTWM2OD1yLkOyOVg6KM7:TR?= MlLpV2FPT0WU
G-361 MoDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzKNG5KSzVyPUCuN|Q3OzdizszN M2K0U3NCVkeHUh?=
HT-144 M2PmPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVi2[5ZHUUN3ME2wMlM3OzJ7IN88US=> NVPPdYppW0GQR1XS
ACN MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnsUGZoUUN3ME2wMlM5PDd5IN88US=> M3rFUHNCVkeHUh?=
COLO-829 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fEc2lEPTB;MD6zPFk3QCEQvF2= NWXiZ21NW0GQR1XS
MEL-HO NXzCN4hMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTBwNEGxO|kh|ryP NHXzU2JUSU6JRWK=
SH-4 MmDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHBd4xWUUN3ME2wMlQyPDJ{IN88US=> MojpV2FPT0WU
SK-MEL-3 M1GyNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljETWM2OD1yLkWxOVY5KM7:TR?= MVrTRW5ITVJ?
A375 NYfKVpVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7oTWM2OD1yLk[3N|U6KM7:TR?= NXvqZVVzW0GQR1XS
MMAC-SF NGDHe|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTVPFhKSzVyPUCuOlg3OTRizszN NFfXOG9USU6JRWK=
BHT-101 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LnN2lEPTB;MD63NFcxOiEQvF2= M3zmVHNCVkeHUh?=
K5 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkm1TWM2OD1yLke2NVQ5KM7:TR?= MU\TRW5ITVJ?
BV-173 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPRb|BrUUN3ME2wMlc6PjR2IN88US=> NELnN3FUSU6JRWK=
RVH-421 NUK4T5pMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;YTWM2OD1yLki2O|k3KM7:TR?= MojIV2FPT0WU
HCC2218 NXvSZotrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jMTGlEPTB;MD64O|g1PCEQvF2= M{f0eHNCVkeHUh?=
WM-115 Mk[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\sTWM2OD1yLki4OlkzKM7:TR?= MVXTRW5ITVJ?
SK-MEL-28 NV;3NYVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFuzRpFKSzVyPUGuNFQ2PjlizszN NVX4cWxRW0GQR1XS
COLO-679 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYS4U|FLUUN3ME2xMlExPDZ2IN88US=> NV\mZlhRW0GQR1XS
MZ7-mel NXuwZYx6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;aTWM2OD1zLkG0PVY{KM7:TR?= NUPnS4NPW0GQR1XS
SK-MEL-30 NH3mTHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3MTW1KSzVyPUGuN|M{QDZizszN MWnTRW5ITVJ?
NCI-H209 Mnz6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUH5Nlh1UUN3ME2xMlYxQDZizszN NX3rd5kyW0GQR1XS
HTC-C3 Ml;RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTFwNk[yPVQh|ryP M{KwcnNCVkeHUh?=
KARPAS-45 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTJwMES5O|gh|ryP MnXkV2FPT0WU
NCI-SNU-5 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3iZVJKSzVyPUKuNVE6PjlizszN NX3YSm06W0GQR1XS
KP-4 MofoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLhTWM2OD1{LkOwO|g4KM7:TR?= MnzEV2FPT0WU
PA-1 NXflUXhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjvdZBKUUN3ME2yMlczPjd|IN88US=> NWGz[G1XW0GQR1XS
HuO-3N1 M3n6dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEizVpRKSzVyPUKuPFc6PDZizszN M4XYTXNCVkeHUh?=
NCI-H358 M1LWdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTJwOUKyN|Ih|ryP Mn7LV2FPT0WU
CTB-1 NYn5OVYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7Pb2dKSzVyPUOuOFAyPzZizszN M3fUTnNCVkeHUh?=
697 M1TLdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDvdmFKSzVyPUOuOVUzPjZizszN NW[weJRjW0GQR1XS
CP66-MEL MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mon0TWM2OD12LkG1PVI4KM7:TR?= M162TnNCVkeHUh?=
NB13 M2nRO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2[z[WlEPTB;ND60PVE4QSEQvF2= NHjheHhUSU6JRWK=
DBTRG-05MG M4\QRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXSzS21SUUN3ME20MlU{OzJ3IN88US=> NUPVOnE3W0GQR1XS
A2058 MnvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3QSXlQUUN3ME20MlczOTZ2IN88US=> Mm[yV2FPT0WU
KG-1 NH;YWo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\UbW5sUUN3ME20Mlc{QTB6IN88US=> NHXIeWxUSU6JRWK=
8305C NGrHSZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTVwMUi3N{DPxE1? NVXX[5FyW0GQR1XS
RPMI-7951 MljpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTVwOECyPFMh|ryP NX2wUnRxW0GQR1XS
CHL-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTVwOUe2NFMh|ryP NInTXJdUSU6JRWK=
TI-73 NXWzS4dsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPUTWM2OD14LkCwPVAzKM7:TR?= NFjN[YRUSU6JRWK=
HT-1080 NYXYVW4zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFP3bXpKSzVyPU[uNVA6PDZizszN NH3TeGZUSU6JRWK=
ES5 NVvTZ4VMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XTV2lEPTB;Nj6xOFkzPCEQvF2= M4DNW3NCVkeHUh?=
8-MG-BA MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\TZZdEUUN3ME22MlE5OTJ7IN88US=> M1f6[3NCVkeHUh?=
NB7 NIqyc4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XqcmlEPTB;Nj6yNVM4OyEQvF2= NYXYOVJEW0GQR1XS
H4 MoDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkO4TWM2OD14LkKyOFk{KM7:TR?= MlTIV2FPT0WU
CAL-72 NVPXb4VDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTZwNEW0NlMh|ryP NXTjO4NNW0GQR1XS
HCC1806 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7yU5RKSzVyPU[uPFE6OzFizszN NVr2VFJHW0GQR1XS
BCPAP MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1njcmlEPTB;Nz6yNVc3PCEQvF2= NWn0XnZsW0GQR1XS
LB2241-RCC MlziS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETQRVBKSzVyPUeuN|Y6ODdizszN M4TGTHNCVkeHUh?=
COLO-741 M2jiZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRThwMEG2O|kh|ryP Mn3OV2FPT0WU
HSC-3 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHyO3dKSzVyPUiuNFcxPjhizszN NV;rdYVGW0GQR1XS
SW982 MnW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInYSmdKSzVyPUiuOFE2OTZizszN M331PHNCVkeHUh?=
GCT MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRThwN{WzNVQh|ryP NF\4VpVUSU6JRWK=
KY821 NXrIe2ZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYm3VFJUUUN3ME25MlA2OTd6IN88US=> MX;TRW5ITVJ?
JVM-3 NXnFRWtCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTlwNU[5PVkh|ryP NHvIT|JUSU6JRWK=
RS4-11 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rUcmlEPTB;OT62NFQ5KM7:TR?= MlHiV2FPT0WU
VA-ES-BJ NHnmdndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFiwbpBKSzVyPUGwMlAyPDlizszN MlvIV2FPT0WU
A431 NIrqbG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rBXWlEPTB;MUCuOFIyOiEQvF2= M1jDS3NCVkeHUh?=
LXF-289 NGrLSXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jDeWlEPTB;MUCuOFU5KM7:TR?= M{LKRXNCVkeHUh?=
SK-MEL-24 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfCTWM2OD1zMD64Nlc1KM7:TR?= NHPaWFlUSU6JRWK=
NOS-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoD3TWM2OD1zMD64OFczKM7:TR?= NY[3PHdYW0GQR1XS
KNS-62 NEfMRmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PNUGlEPTB;MUGuNlQxPCEQvF2= MYXTRW5ITVJ?
SK-HEP-1 NYjGc3A4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTFzLkO1Nlch|ryP M4XKVXNCVkeHUh?=
A3-KAW M4PsVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zmfGlEPTB;MUGuO|E4QCEQvF2= NFTHW2xUSU6JRWK=
SK-LU-1 Ml\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTETWM2OD1zMj6yOlU2KM7:TR?= NGP0XGtUSU6JRWK=
TYK-nu NEHvRoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTF{LkO5N|Ih|ryP NVuzNm0{W0GQR1XS
NMC-G1 NG\1V|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjiTWM2OD1zMj62NFYzKM7:TR?= MkTEV2FPT0WU
BB65-RCC MnrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTqVIlqUUN3ME2xNk44OTZ7IN88US=> MVzTRW5ITVJ?
QIMR-WIL NV7nb|JDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFu5RWFKSzVyPUGyMlg5OzNizszN NFHJZ4NUSU6JRWK=
D-566MG M2rJVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\X[IlpUUN3ME2xN{46PTd4IN88US=> MVTTRW5ITVJ?
KYSE-140 M1HmWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGj0XVRKSzVyPUG0MlA4PTNizszN MWLTRW5ITVJ?
SCC-4 NXzvVmg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTF2LkOzOVkh|ryP NIrIcJhUSU6JRWK=
U251 NVrVV4FFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTF2Lki0PVIh|ryP NVrST4h2W0GQR1XS
D-542MG NV3FbZgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlq3TWM2OD1zND65NlIzKM7:TR?= M2KyNnNCVkeHUh?=
LAMA-84 M{fYZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;3OGlEPTB;MUSuPVk{OiEQvF2= NGLzbVlUSU6JRWK=
NCI-H720 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vPdmlEPTB;MUWuNlY5PCEQvF2= M4n0fnNCVkeHUh?=
DEL MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzLUI1oUUN3ME2xOU41Ojl|IN88US=> M12yOXNCVkeHUh?=
SBC-1 NH3uWFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13icWlEPTB;MUWuOFMxPSEQvF2= MmG2V2FPT0WU
ECC10 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYC1SXZjUUN3ME2xOU41PDV6IN88US=> NHvrdnFUSU6JRWK=
Daoy NVfQZoJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrrdXVIUUN3ME2xOU44PjF4IN88US=> M1\UUXNCVkeHUh?=
SCH MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjrWIlKSzVyPUG1Mlc5OzVizszN NYH1TZNGW0GQR1XS
MZ2-MEL NVrV[VJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDYToxQUUN3ME2xOk4xPjR4IN88US=> NGjVVXNUSU6JRWK=
CAL-12T MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTF4LkS4OlIh|ryP Mm\CV2FPT0WU
KE-37 M1fDWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LlOWlEPTB;MU[uPFExPyEQvF2= M{LtW3NCVkeHUh?=
LS-411N MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\MTWlEPTB;MUeuNVE5KM7:TR?= M3\ve3NCVkeHUh?=
NCI-H2228 Ml[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTF5LkOwO|Eh|ryP NE\tcZdUSU6JRWK=
SK-MEL-2 NEnMZpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTF5LkS5OlUh|ryP NH;GRppUSU6JRWK=
HN M1iybGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2r2emlEPTB;MUeuO|I1QCEQvF2= NVLONHJGW0GQR1XS
NCI-H1648 NH3GPGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nSXmlEPTB;MUeuPFE5KM7:TR?= Ml;LV2FPT0WU
IA-LM MlP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrvTWM2OD1zOD6zNVczKM7:TR?= MnPJV2FPT0WU
EW-13 NE\UeXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXOTWM2OD1zOD61O|A5KM7:TR?= NEDlTVlUSU6JRWK=
YKG-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1K3NmlEPTB;MUmuOVcyOSEQvF2= MnTPV2FPT0WU
KNS-81-FD MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjPPHo1UUN3ME2xPU42QDV6IN88US=> M4LiWnNCVkeHUh?=
23132-87 M2H3V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTF7Lke2OFIh|ryP NVPXW5V[W0GQR1XS
NUGC-3 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2ryZmlEPTB;MUmuPVg5PyEQvF2= M1rmNHNCVkeHUh?=
5637 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PieWlEPTB;MkCuNFQ4QCEQvF2= NEeyO4tUSU6JRWK=
NCI-H1755 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnIZXFJUUN3ME2yNE41PzZ2IN88US=> MlLwV2FPT0WU
RH-18 MkDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLZRot1UUN3ME2yNE42PzR6IN88US=> M3TjWHNCVkeHUh?=
RXF393 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HyVmlEPTB;MkCuOlc2PiEQvF2= NUn4UXRSW0GQR1XS
LU-134-A NXz6N49ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33KdWlEPTB;MkCuO|A2PiEQvF2= M3GzOnNCVkeHUh?=
TE-12 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTJyLkeyNFEh|ryP NUPlXIxlW0GQR1XS
MOLT-4 MkD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnOR3dKSzVyPUKxMlE6OTVizszN M3HYVHNCVkeHUh?=
IGR-1 M4X2NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTJzLkO3PVYh|ryP M2r5dXNCVkeHUh?=
HOP-92 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTJzLkS5PFch|ryP NVHxNnJJW0GQR1XS
SK-MES-1 NGrwb2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfVTWM2OD1{MT63N|gyKM7:TR?= NUHz[2d[W0GQR1XS
LU-65 NVKzdoNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVKxWZV6UUN3ME2yNU45PjJ2IN88US=> MULTRW5ITVJ?
MS-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjl[4VtUUN3ME2yNk4yOjB|IN88US=> M{fSdXNCVkeHUh?=
LoVo MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;t[JNKSzVyPUKyMlI1PCEQvF2= MUHTRW5ITVJ?
A704 NGftWXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjwdJFKSzVyPUKyMlUyPTVizszN Mnz1V2FPT0WU
HT-1376 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTJ{Lk[wOVkh|ryP NIm2b|VUSU6JRWK=
IST-MEL1 NXG0V2JsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIm5dnBKSzVyPUKyMlY4PTFizszN NEHRRpJUSU6JRWK=
Ramos-2G6-4C10 NV3GdodVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PzOmlEPTB;MkKuO|M3PiEQvF2= MXzTRW5ITVJ?
T47D MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJ{Lke5O|kh|ryP NHHnSHFUSU6JRWK=
HT-1197 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknTTWM2OD1{Mz6wPFE4KM7:TR?= MWLTRW5ITVJ?
LB2518-MEL M1rofmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzMTWM2OD1{Mz62OFEzKM7:TR?= NV33UoJpW0GQR1XS
J-RT3-T3-5 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rYOGlEPTB;MkSuO|U6PSEQvF2= NVHnflYyW0GQR1XS
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NCI-H526 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHBb3pKSzVyPUK1MlAxOjNizszN MXjTRW5ITVJ?
IST-SL1 MkTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTBTWM2OD1{NT6yO|UyKM7:TR?= NEfueGdUSU6JRWK=
HH MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jiTWlEPTB;MkWuN|E6OiEQvF2= M2rvPXNCVkeHUh?=
NCI-H82 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzNNYZKSzVyPUK1Mlk{QCEQvF2= NVL1cnpqW0GQR1XS
SNU-449 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXTTWM2OD1{Nz6yNFE5KM7:TR?= NFrSUYZUSU6JRWK=
COR-L23 M3y3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTJ5LkK4NVMh|ryP M3ji[nNCVkeHUh?=
LOXIMVI MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDWT3o3UUN3ME2yO{4{PjhizszN NVz5UZBZW0GQR1XS
GR-ST NIjBVGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETw[5RKSzVyPUK3MlY4ODZizszN MX;TRW5ITVJ?
NCI-SNU-1 NX[3R3pST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\vTWM2OD1{Nz65OFQh|ryP M4jZbHNCVkeHUh?=
ALL-PO NWDrPY5zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XzdGlEPTB;MkiuNVYxPCEQvF2= NGLxdoZUSU6JRWK=
ML-2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHOW2VKSzVyPUK4MlI5OTRizszN MmHKV2FPT0WU
HOP-62 NXjKN|Z6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37XTmlEPTB;MkiuO|E{KM7:TR?= NXizbVN1W0GQR1XS
EGI-1 NF;RcFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTJ6Lki4OFUh|ryP MVrTRW5ITVJ?
TCCSUP MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDyTWM2OD1{OD65NlczKM7:TR?= MkewV2FPT0WU
LB996-RCC MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vmdGlEPTB;MkmuOVY5OiEQvF2= NXO3WHkyW0GQR1XS
LCLC-97TM1 Ml7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rCNGlEPTB;M{KuNVk3PCEQvF2= NFrheGhUSU6JRWK=
NCI-H1304 M4T1d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfQbHdKSzVyPUOyMlM{ODFizszN MnTMV2FPT0WU
KP-N-YS M{XldWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTN{LkW5O|Mh|ryP M2i1UHNCVkeHUh?=
NCI-H1770 NX;SbVZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTN|LkG2OFgh|ryP NYjpVIRvW0GQR1XS
EM-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlWyTWM2OD1|Mz62OVA1KM7:TR?= MoW1V2FPT0WU
ChaGo-K-1 MoTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXITWM2OD1|Mz63NlM3KM7:TR?= M2nMNnNCVkeHUh?=
ACHN NXi2[2J1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTN|LkizPFUh|ryP NGf5ZVZUSU6JRWK=
MN-60 NYHzZm92T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rWUmlEPTB;M{OuPFU1PCEQvF2= MoWzV2FPT0WU
EW-18 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7aNldKSzVyPUOzMlg6PzFizszN NH3uPFRUSU6JRWK=
KGN NETDe3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnWyTWM2OD1|NT63NlkzKM7:TR?= M37FeXNCVkeHUh?=
U031 NIm4UGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LsT2lEPTB;M{WuPFE{OiEQvF2= NXnZNZZFW0GQR1XS
HMV-II NVLvSlV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\oR|JmUUN3ME2zOk4xPzd2IN88US=> M2T4fXNCVkeHUh?=
L-363 NFHJNGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zvdmlEPTB;M{euOlQ2PSEQvF2= MXvTRW5ITVJ?
NCI-H1155 NXzFWY01T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\VZ2lEPTB;M{iuNFAyPSEQvF2= MX3TRW5ITVJ?
NCI-H1793 NGnlZmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHY[ZFKSzVyPUO4MlExOjZizszN NEWwZ4JUSU6JRWK=
P30-OHK MmfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnKXZkyUUN3ME2zPE4yOzN{IN88US=> NYrrWFZ{W0GQR1XS
AN3-CA NELURY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnCc2VKSzVyPUO4MlE3OTVizszN NWDIR4VZW0GQR1XS
UACC-257 NILvcmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknKTWM2OD1|OD63PUDPxE1? NH3uTldUSU6JRWK=
MCF7 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTETWM2OD1|OT64OlI6KM7:TR?= NILMUY1USU6JRWK=
KP-N-YN MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTRyLkSyPFUh|ryP NVTqZm15W0GQR1XS
T98G NEPidZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;ZTWM2OD12MD60PVU4KM7:TR?= MYDTRW5ITVJ?
HGC-27 NXvuOotNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIq2O2NKSzVyPUSzMlI4PCEQvF2= MYTTRW5ITVJ?
NCI-H1092 NWfORoNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3:5OmlEPTB;NEOuNlg6PSEQvF2= NHTkNmhUSU6JRWK=
KARPAS-299 MonBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvOSG1KSzVyPUSzMlMxPzFizszN M1i1[HNCVkeHUh?=
LB1047-RCC NGnURVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoOxTWM2OD12ND65PVU6KM7:TR?= Mk\HV2FPT0WU
786-0 NVToTlhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[0TWM2OD12NT62OUDPxE1? M2X2[XNCVkeHUh?=
HCC2157 NEj4R4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTR4LkCzOVkh|ryP MkDoV2FPT0WU
NY NW\5VnpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzOT3I5UUN3ME20Ok4yPzd6IN88US=> MYfTRW5ITVJ?
EFM-19 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPxdXo{UUN3ME20Ok44PTN|IN88US=> MofZV2FPT0WU
EW-16 NHPxfZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPmVWlKSzVyPUS2Mlc5ODZizszN NFm1bIpUSU6JRWK=
UM-UC-3 M4\2SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4ruO2lEPTB;NE[uPFA2QSEQvF2= M4PN[nNCVkeHUh?=
HT-29 NYrvXFNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\FTWM2OD12Nz64O|kzKM7:TR?= NEfLVoVUSU6JRWK=
LN-405 NFPoN4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XaNmlEPTB;NEiuNFgzPyEQvF2= NHfycI1USU6JRWK=
NCI-H727 NIXofGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\NeplvUUN3ME20PE44PzJ4IN88US=> MYTTRW5ITVJ?
D-502MG MlLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2[wU2lEPTB;NEiuPVY4PiEQvF2= MoLuV2FPT0WU
GMS-10 NUSwVZdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\ZVmlEPTB;NEmuNlk4PCEQvF2= NH3VdHVUSU6JRWK=
MEL-JUSO NYH6V3N4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTR7LkO0O{DPxE1? NEfHcmRUSU6JRWK=

... 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 1% CMC+0.5% Tween-80 30 mg/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

カスタマーフィードバック (9)


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Rating
Source Cancer Discov, 2013, 3, 350-62. PLX-4720 purchased from Selleck
Method Western blot
Cell Lines A375 cells
Concentrations 1 uM
Incubation Time 16 h
Results Associated with the increased RAS-GTP, it's observed a concomitant increase in C-RAF activation, as measured by phosphorylation of Ser338. Under conditions of combined C-RAF/NF1 knockdown, ERK phosphorylation was inhibited more effectively compared to knockdown of NF1 alone. Moreover, whereas cyclin D1 levels were inhibited by PLX4720 in A375 cells, but NF1 silencing partially alleviated this effect.

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Rating
Source Genes Dev, 2012, 26, 1055-69. PLX-4720 purchased from Selleck
Method Western blot
Cell Lines Melanoma cell lines
Concentrations 1, 2, 3 uM
Incubation Time 4 h, 3 days
Results Treatment with Pi-103 and PLX4720 (a BRAFV600E inhibitor) inhibited the activity of AKT and ERK, respectively (D). More importantly, Pi-103 treatment profoundly cooperated with PLX4720 of inhibition in dose response curves(E).

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Rating
Source Proc Natl Acad Sci USA , 2011, 108, 6067-6072. PLX-4720 purchased from Selleck
Method Western blotting
Cell Lines Cells overexpressing myc-CRAF and BRAF
Concentrations 10/50 µM
Incubation Time 1/2 h
Results GDC0879 but not PLX4720 induced BRAF/CRAF dimer formation (Fig. A). However, both drugs induced complexes between KSR1 and CRAF and enhanced interactions between KSR1 and BRAF (Fig. B and C), which suggested that KSR1/RAF complexes induced by the drug might explain the effects ofthe type I BRAF specific inhibitors. As reported previously, treatment of wild-type cells with either drug strongly induced ERK activation at low to intermediate doses but inhibited ERK activation at higher doses (Fig. D and E). Similar results were obtained with cells expressing constitutively active RAS (Fig. D and E) or after serum treatment. Strikingly, in KSR deficient cells, ERK activation was significantly attenuated after PLX4720 or GDC0879 treatment (Fig. D and E), which demonstrates that the ability of PLX4720 and GDC0879 to activate ERK requires the presence of KSR1. We found that, when KSR1 was overexpressed withCRAF, MEK activation was induced by PLX4720 or GDC0879 treatment (Fig. F). this result suggested that induction of the CRAF/KSR1 complex might be important in the activation of MEK. In vitro kinase activity toward MEK was detected but only after drug treatment (Fig. G), which suggests KSR1/CRAF complex formation kinase activity toward MEK.

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Rating
Source Cancer Res , 2011, 71, 2750-2760. PLX-4720 purchased from Selleck
Method Western blotting, MTT assay, flow cytometry
Cell Lines PTEN+/ PTEN- melanoma cell lines
Concentrations 0.001-10 µmol/L
Incubation Time 48 h
Results The PTEN+ cell lines had lower constitutive levels of pAKT (Ser473) compared with the PTEN(Fig. A). Similar levels of pAKT (Thr308) were observed in the PTEN and PTEN þ cell lines. Analysis of the growth inhibitory effects of PLX4720 by the MTT and Alamar Blue assays (Fig. B) did not reveal any statistically significant differences in the GI 50 values between the PTEN+/ PTEN- cell lines. We observed that following PLX4720 treatment (3 and 10 µmol/L, 48 hours), the PTEN-melanoma cell lines showed significantly less apoptosis than the PTEN+ (P < 0.05: Fig. C)

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Rating
Source Cancer Res , 2011, 71, 2750-2760. PLX-4720 purchased from Selleck
Method Western blotting
Cell Lines PTEN+/ PTEN- melanoma cell lines
Concentrations 0.03-3 µmol/L
Incubation Time 24 h
Results Treatment of the PTEN+/ PTEN- cell line panels with PLX4720 increased pPDK1andpAKTsignaling only in the melanoma cell lines lacking PTEN expression (Fig. A). Addition of PLX4720 also led to the inhibition of mTOR activity in the PTEN+ cell lines only (Fig. A). The requirement for PTEN in the increased AKT signaling was confirmed by studies showing that PLX4720 stimulated pAKT in WM35 cells (PTEN+) when PTEN was knocked down by siRNA (Fig. B). The effects of PLX4720 upon pAKT signaling were BRAF specific, with BRAF siRNA knockdown found to increase pAKT in PTEN- cells only (Fig. C).

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Rating
Source Cancer Res, 2011, 71, 2750-2760. PLX-4720 purchased from Selleck
Method Western blot, Immunofluorescence staining, flow cytometry
Cell Lines 1205Lu cells
Concentrations 3 µmol/L
Incubation Time 48 h
Results Combined PI3K and BRAF inhibition increased the level of BIM expression in both Western blot and immunofluorescence studies (Fig. A). Consistent with a role for increased AKT signaling suppressing BIM expression in PTEN- cells, dual BRAF and PI3K inhibition increased nuclear FOXO3a localization in the PTEN- cell lines (Fig. B) and enhanced the level of BIM mRNA (Fig. B). the combination of PLX4720 with the PI3K inhibitor GDC-0941 significantly enhanced the levels of apoptosis observed in PTEN melanoma cell lines compared to either the BRAF or PI3K inhibitor alone (Fig. C). Similar results were also observed in a 3D spheroid assay, where combined PLX4720 (3 µmol/L) and LY294002 (10 µmol/L) treatment prevented the recovery of cell growth observed when melanoma spheroids were treated with either drug alone (Fig. D).

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Rating
Source Cancer Res , 2011, 71, 2750-2760. PLX-4720 purchased from Selleck
Method LC-MRM analysis, Western blotting, immunofluorescence staining
Cell Lines PTEN+/ PTEN- melanoma cell lines
Concentrations 3/10 µmol/L
Incubation Time 0-48 h
Results We next used LC-MRM to quantify the PLX4720-induced changes in the expression of 17 members of the Bcl-2 protein family (Fig. A shows results for 9 proteins). The only proapoptotic protein to demonstrate significant differences between the PTEN+/ PTEN- cell lines was BIM (Fig. A). Western blots and immunofluorescence staining confirmed the LC-MRM data and showed a greater degree of PLX4720-induced BIM expression in the PTEN+ cell lines compared to PTEN- cell lines (Fig. B,C). In parallel, we observed that PLX4720 also increased the inactivation of BAD (as shown by increased phospho-BAD) in the PTEN- cells (Fig. D) and that overexpression of BAD in the PTEN- cells enhanced PLX4720-mediated apoptosis (Fig. D).

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Rating
Source Dr. Jong-In Park of Medical College of Wisconsin. PLX-4720 purchased from Selleck
Method Western blot
Cell Lines SK-MEL-28 cell line
Concentrations 0-1 µM
Incubation Time 4/22 h
Results 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

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Rating
Source Dr. Daniel C.Cho of Harvard Medical School. PLX-4720 purchased from Selleck
Method MTT assay, Western blotting
Cell Lines A375 melanoma cells
Concentrations 0-1000 nM
Incubation Time
Results 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.

文献中の引用 (44)

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    Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.

  • Sorafenib Tosylate

    Sorafenib Tosylateは、Raf-1、B-RafとVEGFR-2のマルチキナーゼ阻害剤で、IC50 がそれぞれ 6 nM、 22 nM、90 nMです。

  • TAK-632

    TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf, respectively, showing less or no inhibition against other tested kinases.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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