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 NFTYRppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUKzXIFtUUN3ME2wMlA4PDV5IN88US=> MWTTRW5ITVJ?
EoL-1-cell NXHXeYJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwMUSxOlYh|ryP NWfGSHdzW0GQR1XS
C32 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPSO2pKSzVyPUCuNVUyOzFizszN Mnm1V2FPT0WU
M14 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLZcYxKSzVyPUCuNlE4PTdizszN M2HnSHNCVkeHUh?=
CP50-MEL-B MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfpZnRKSzVyPUCuNlk4QDRizszN NEfuXnVUSU6JRWK=
A101D NH;yfIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwM{K1PFkh|ryP M4jVU3NCVkeHUh?=
G-361 M4O2Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLCUFVKSzVyPUCuN|Q3OzdizszN MXXTRW5ITVJ?
HT-144 M1XvO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFW0d|BKSzVyPUCuN|Y{OjlizszN MlHUV2FPT0WU
ACN NYnQSnZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYD1eHN2UUN3ME2wMlM5PDd5IN88US=> NXPnfnhkW0GQR1XS
COLO-829 NInQd3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLPOndKSzVyPUCuN|g6PjhizszN MorMV2FPT0WU
MEL-HO MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvDUXpKSzVyPUCuOFEyPzlizszN M{H1NXNCVkeHUh?=
SH-4 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwNEG0NlIh|ryP M122ZnNCVkeHUh?=
SK-MEL-3 NVLDVXZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTBwNUG1Olgh|ryP M3mybnNCVkeHUh?=
A375 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TheWlEPTB;MD62O|M2QSEQvF2= M1zJXXNCVkeHUh?=
MMAC-SF NXu1PJhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2j3TGlEPTB;MD62PFYyPCEQvF2= MVjTRW5ITVJ?
BHT-101 NUTuVJUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LCSWlEPTB;MD63NFcxOiEQvF2= NIjSRohUSU6JRWK=
K5 NF3MPZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFP6fXlKSzVyPUCuO|YyPDhizszN M1T1ZXNCVkeHUh?=
BV-173 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[4TWM2OD1yLke5OlQ1KM7:TR?= MVrTRW5ITVJ?
RVH-421 NVXoR5hDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXFXI1KSzVyPUCuPFY4QTZizszN Mn:xV2FPT0WU
HCC2218 NVzmTIVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\ZSYdsUUN3ME2wMlg4QDR2IN88US=> NUTXcZRHW0GQR1XS
WM-115 NYDZNHBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPDXFRIUUN3ME2wMlg5Pjl{IN88US=> Mn\LV2FPT0WU
SK-MEL-28 NXTWTYpqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LrXmlEPTB;MT6wOFU3QSEQvF2= MY\TRW5ITVJ?
COLO-679 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnnTWM2OD1zLkGwOFY1KM7:TR?= MnjSV2FPT0WU
MZ7-mel MoC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moj4TWM2OD1zLkG0PVY{KM7:TR?= MVPTRW5ITVJ?
SK-MEL-30 MnSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTFwM{OzPFYh|ryP NFPSN2xUSU6JRWK=
NCI-H209 M4HZNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTFwNkC4OkDPxE1? NUTJSXRtW0GQR1XS
HTC-C3 NWDiUoNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\NTWM2OD1zLk[2Nlk1KM7:TR?= NHfY[pNUSU6JRWK=
KARPAS-45 NWDjd2J{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTJwMES5O|gh|ryP NVLrVIIxW0GQR1XS
NCI-SNU-5 NUfnXXBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3VN3NMUUN3ME2yMlEyQTZ7IN88US=> M3vW[3NCVkeHUh?=
KP-4 M2LpR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\3Rox{UUN3ME2yMlMxPzh5IN88US=> MYjTRW5ITVJ?
PA-1 NU[3ZodbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LNSWlEPTB;Mj63NlY4OyEQvF2= MUHTRW5ITVJ?
HuO-3N1 NXnXOYVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PXTmlEPTB;Mj64O|k1PiEQvF2= Mnq3V2FPT0WU
NCI-H358 M1\D[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWf1TVZJUUN3ME2yMlkzOjN{IN88US=> Mn\xV2FPT0WU
CTB-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoKyTWM2OD1|LkSwNVc3KM7:TR?= MVjTRW5ITVJ?
697 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTNwNUWyOlYh|ryP NX7O[WJiW0GQR1XS
CP66-MEL NVu0WZp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{X3NmlEPTB;ND6xOVkzPyEQvF2= MVrTRW5ITVJ?
NB13 M4W4cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\P[ohrUUN3ME20MlQ6OTd7IN88US=> M1LIeHNCVkeHUh?=
DBTRG-05MG NInTV3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTRwNUOzNlUh|ryP NGHzVIlUSU6JRWK=
A2058 M1XGWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTRwN{KxOlQh|ryP M1j6XnNCVkeHUh?=
KG-1 MnToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPPU5lDUUN3ME20Mlc{QTB6IN88US=> NYLX[YJpW0GQR1XS
8305C MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXtdZE1UUN3ME21MlE5PzNizszN MnXnV2FPT0WU
RPMI-7951 Ml\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1W2ZWlEPTB;NT64NFI5OyEQvF2= NXnKO29nW0GQR1XS
CHL-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{GxS2lEPTB;NT65O|YxOyEQvF2= M3;0[nNCVkeHUh?=
TI-73 M3nRZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH22cHlKSzVyPU[uNFA6ODJizszN NHG0UmhUSU6JRWK=
HT-1080 NVnQfIxUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHFRoFKSzVyPU[uNVA6PDZizszN M4W0SXNCVkeHUh?=
ES5 M3X2bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHvT41DUUN3ME22MlE1QTJ2IN88US=> MnzzV2FPT0WU
8-MG-BA NFvIOXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTZwMUixNlkh|ryP NFL6OlZUSU6JRWK=
NB7 NHnSVmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjiTWM2OD14LkKxN|c{KM7:TR?= MoLqV2FPT0WU
H4 M{nrXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTZwMkK0PVMh|ryP NUm2c3VkW0GQR1XS
CAL-72 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTZwNEW0NlMh|ryP MVnTRW5ITVJ?
HCC1806 NWDPNIZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnmTWM2OD14LkixPVMyKM7:TR?= MVnTRW5ITVJ?
BCPAP MorCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnzW5N[UUN3ME23MlIyPzZ2IN88US=> MV3TRW5ITVJ?
LB2241-RCC M4Xsb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nQUWlEPTB;Nz6zOlkxPyEQvF2= MY\TRW5ITVJ?
COLO-741 NFjSV4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHezXVhKSzVyPUiuNFE3PzlizszN MofRV2FPT0WU
HSC-3 MoD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPG[VRKSzVyPUiuNFcxPjhizszN MWjTRW5ITVJ?
SW982 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV:yVpZDUUN3ME24MlQyPTF4IN88US=> M{HweHNCVkeHUh?=
GCT MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnkXmt[UUN3ME24Mlc2OzF2IN88US=> NXKwUGRMW0GQR1XS
KY821 NXy0bWJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4raXWlEPTB;OT6wOVE4QCEQvF2= NHTtcVVUSU6JRWK=
JVM-3 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTlwNU[5PVkh|ryP MlTSV2FPT0WU
RS4-11 NHLsd2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH2zV2hKSzVyPUmuOlA1QCEQvF2= NXn2RYtnW0GQR1XS
VA-ES-BJ NVHNc5NpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7zTWM2OD1zMD6wNVQ6KM7:TR?= MoX4V2FPT0WU
A431 M1fz[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDvV|dKSzVyPUGwMlQzOTJizszN M{HV[3NCVkeHUh?=
LXF-289 Mn;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXj1O2NZUUN3ME2xNE41PThizszN NFO4PWtUSU6JRWK=
SK-MEL-24 MknSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTFyLkiyO|Qh|ryP NF;pXlhUSU6JRWK=
NOS-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEm2UYdKSzVyPUGwMlg1PzJizszN NFf3co9USU6JRWK=
KNS-62 NYLoWIplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Ww[WlEPTB;MUGuNlQxPCEQvF2= M4Pa[3NCVkeHUh?=
SK-HEP-1 MoLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HhVmlEPTB;MUGuN|UzPyEQvF2= M4LEfnNCVkeHUh?=
A3-KAW NXrnfpc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfuTWM2OD1zMT63NVc5KM7:TR?= MYXTRW5ITVJ?
SK-LU-1 NHf1U4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXi3TYNJUUN3ME2xNk4zPjV3IN88US=> M4P6fHNCVkeHUh?=
TYK-nu M2[2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTF{LkO5N|Ih|ryP NEKyeFlUSU6JRWK=
NMC-G1 NYX3[IN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXK3PGdtUUN3ME2xNk43ODZ{IN88US=> NGLQOWNUSU6JRWK=
BB65-RCC NGXzfGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXnTWM2OD1zMj63NVY6KM7:TR?= NUnoNGF6W0GQR1XS
QIMR-WIL M1jVfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTF{Lki4N|Mh|ryP M2PWTHNCVkeHUh?=
D-566MG MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrEeJJQUUN3ME2xN{46PTd4IN88US=> MmrNV2FPT0WU
KYSE-140 M3;JVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XiXmlEPTB;MUSuNFc2OyEQvF2= M2rxSHNCVkeHUh?=
SCC-4 NXLIR|NMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\1cWlEPTB;MUSuN|M2QSEQvF2= MVvTRW5ITVJ?
U251 NHrFbHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXnfIRKSzVyPUG0Mlg1QTJizszN NVHWRYpLW0GQR1XS
D-542MG MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\udXRKSzVyPUG0MlkzOjJizszN NEPQPHBUSU6JRWK=
LAMA-84 NEXNeWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFK3eYNKSzVyPUG0Mlk6OzJizszN M{PvfHNCVkeHUh?=
NCI-H720 NUDpOIFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVK4[Vl3UUN3ME2xOU4zPjh2IN88US=> MlXZV2FPT0WU
DEL M{DFTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrpeXVvUUN3ME2xOU41Ojl|IN88US=> MYnTRW5ITVJ?
SBC-1 M1rlNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLhUHkxUUN3ME2xOU41OzB3IN88US=> NGLOOHpUSU6JRWK=
ECC10 MkmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELVPGdKSzVyPUG1MlQ1PThizszN NGLPflhUSU6JRWK=
Daoy NF7XWoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPTTWM2OD1zNT63OlE3KM7:TR?= MnfJV2FPT0WU
SCH NXPjRplZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTF3Lke4N|Uh|ryP NETzeHJUSU6JRWK=
MZ2-MEL NXT5XJN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTI[FVoUUN3ME2xOk4xPjR4IN88US=> M3PLUXNCVkeHUh?=
CAL-12T MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkH3TWM2OD1zNj60PFYzKM7:TR?= NI\QU5VUSU6JRWK=
KE-37 M37BSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvDTWM2OD1zNj64NVA4KM7:TR?= M3v1NnNCVkeHUh?=
LS-411N NIK5TlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nESWlEPTB;MUeuNVE5KM7:TR?= MXPTRW5ITVJ?
NCI-H2228 Mn3ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTQTIlYUUN3ME2xO{4{ODdzIN88US=> NFTVNWxUSU6JRWK=
SK-MEL-2 M3\3N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1X2XmlEPTB;MUeuOFk3PSEQvF2= M3G1fXNCVkeHUh?=
HN MomzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LQ[WlEPTB;MUeuO|I1QCEQvF2= MUfTRW5ITVJ?
NCI-H1648 M2nlRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;LdJJ3UUN3ME2xO{45OThizszN NWSzT4hxW0GQR1XS
IA-LM MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\STWM2OD1zOD6zNVczKM7:TR?= M3[4SHNCVkeHUh?=
EW-13 NEn3OZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XiUGlEPTB;MUiuOVcxQCEQvF2= M{jXNHNCVkeHUh?=
YKG-1 NV[xcY1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTF7LkW3NVEh|ryP NVS2cZhZW0GQR1XS
KNS-81-FD NW\WOJIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnWzTWM2OD1zOT61PFU5KM7:TR?= NG\pcHRUSU6JRWK=
23132-87 MkjtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTF7Lke2OFIh|ryP MYrTRW5ITVJ?
NUGC-3 NHv1WHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zWfmlEPTB;MUmuPVg5PyEQvF2= NH21RoRUSU6JRWK=
5637 M3TP[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzq[JZWUUN3ME2yNE4xPDd6IN88US=> NHvxT5hUSU6JRWK=
NCI-H1755 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPJTWM2OD1{MD60O|Y1KM7:TR?= NI[4OVFUSU6JRWK=
RH-18 NF21RnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjkTWM2OD1{MD61O|Q5KM7:TR?= MXfTRW5ITVJ?
RXF393 NWTlbVBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInVd2dKSzVyPUKwMlY4PTZizszN NVz1eZF1W0GQR1XS
LU-134-A MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTJyLkewOVYh|ryP M1jQenNCVkeHUh?=
TE-12 M4\xTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPwWW1KSzVyPUKwMlczODFizszN MoHxV2FPT0WU
MOLT-4 M1:wUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjVUpRKSzVyPUKxMlE6OTVizszN M{DDVnNCVkeHUh?=
IGR-1 MkHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTJzLkO3PVYh|ryP NWnCPVJxW0GQR1XS
HOP-92 M4LpXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1myWmlEPTB;MkGuOFk5PyEQvF2= MnXBV2FPT0WU
SK-MES-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3RTWM2OD1{MT63N|gyKM7:TR?= M1LYNXNCVkeHUh?=
LU-65 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTJzLki2NlQh|ryP MXzTRW5ITVJ?
MS-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITSbmVKSzVyPUKyMlEzODNizszN NWj6XlE5W0GQR1XS
LoVo NVfJO3h{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrCTWM2OD1{Mj6yOFQh|ryP MYDTRW5ITVJ?
A704 M2S3[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDnTWM2OD1{Mj61NVU2KM7:TR?= NV\VdXh1W0GQR1XS
HT-1376 NI[zfo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj1eHVXUUN3ME2yNk43ODV7IN88US=> MXjTRW5ITVJ?
IST-MEL1 MmTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULWWngzUUN3ME2yNk43PzVzIN88US=> M3;nRXNCVkeHUh?=
Ramos-2G6-4C10 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUGyT|R[UUN3ME2yNk44OzZ4IN88US=> NYe4OWc4W0GQR1XS
T47D M2DSRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPiTWM2OD1{Mj63PVc6KM7:TR?= Mm\sV2FPT0WU
HT-1197 NUjsbYVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1H5R2lEPTB;MkOuNFgyPyEQvF2= M2LXTXNCVkeHUh?=
LB2518-MEL Mo[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTJ|Lk[0NVIh|ryP M2DRT3NCVkeHUh?=
J-RT3-T3-5 NWDofXhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPLcGxKSzVyPUK0Mlc2QTVizszN M2K4[HNCVkeHUh?=
SK-NEP-1 M{TSSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWf0XGtxUUN3ME2yOE45PzR2IN88US=> MnPEV2FPT0WU
NCI-H526 M4jZT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXy0dGFXUUN3ME2yOU4xODJ|IN88US=> MkLpV2FPT0WU
IST-SL1 NIj1OohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTJ3LkK3OVEh|ryP NUXVOmFLW0GQR1XS
HH M3\pcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTmNpFKSzVyPUK1MlMyQTJizszN MUDTRW5ITVJ?
NCI-H82 MmPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEW0XndKSzVyPUK1Mlk{QCEQvF2= MVHTRW5ITVJ?
SNU-449 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnFTWM2OD1{Nz6yNFE5KM7:TR?= NY\PdlVRW0GQR1XS
COR-L23 MljYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTJ5LkK4NVMh|ryP NXnZWWk6W0GQR1XS
LOXIMVI NYPGcVJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTufWlPUUN3ME2yO{4{PjhizszN MoPGV2FPT0WU
GR-ST MlzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXv5THBLUUN3ME2yO{43PzB4IN88US=> M3nmTnNCVkeHUh?=
NCI-SNU-1 NWnJb3g5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HPPGlEPTB;MkeuPVQ1KM7:TR?= M3;ZUXNCVkeHUh?=
ALL-PO NVTIfXBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTJ6LkG2NFQh|ryP Moj1V2FPT0WU
ML-2 NVPSXIlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTJ6LkK4NVQh|ryP MljSV2FPT0WU
HOP-62 NVH4W4x1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlexTWM2OD1{OD63NVMh|ryP MYHTRW5ITVJ?
EGI-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXWTWM2OD1{OD64PFQ2KM7:TR?= NIjifIhUSU6JRWK=
TCCSUP NHvMWnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXkRnVsUUN3ME2yPE46Ojd{IN88US=> M2f4SnNCVkeHUh?=
LB996-RCC NVezTGhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGX0d25KSzVyPUK5MlU3QDJizszN NFu0XpNUSU6JRWK=
LCLC-97TM1 NVvqPHJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXwU2ZKSzVyPUOyMlE6PjRizszN MmfBV2FPT0WU
NCI-H1304 MnjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjqfXFKSzVyPUOyMlM{ODFizszN NGPRUVlUSU6JRWK=
KP-N-YS NILBXWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYGzV4pDUUN3ME2zNk42QTd|IN88US=> MkT5V2FPT0WU
NCI-H1770 M2fjXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHO0WHJKSzVyPUOzMlE3PDhizszN M{TJVHNCVkeHUh?=
EM-2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTN|Lk[1NFQh|ryP MorRV2FPT0WU
ChaGo-K-1 NF;hXYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\wU4VKSzVyPUOzMlczOzZizszN NEm4d2pUSU6JRWK=
ACHN MlL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7XT2tpUUN3ME2zN{45Ozh3IN88US=> NIXvUlVUSU6JRWK=
MN-60 NE\BZmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHHTWM2OD1|Mz64OVQ1KM7:TR?= MUjTRW5ITVJ?
EW-18 Mkm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXe4UpRmUUN3ME2zN{45QTdzIN88US=> NYHlTllmW0GQR1XS
KGN MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTN3LkeyPVIh|ryP NHHhWZBUSU6JRWK=
U031 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[zRWlEPTB;M{WuPFE{OiEQvF2= M4\u[HNCVkeHUh?=
HMV-II Ml30S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvyRWpKSzVyPUO2MlA4PzRizszN MkSwV2FPT0WU
L-363 M2\ORWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTN5Lk[0OVUh|ryP M{LQcHNCVkeHUh?=
NCI-H1155 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnwOldRUUN3ME2zPE4xODF3IN88US=> NVzHb4l2W0GQR1XS
NCI-H1793 NGT5XVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTN6LkGwNlYh|ryP Mn\xV2FPT0WU
P30-OHK NWq0d2djT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXTb3hKSzVyPUO4MlE{OzJizszN NWf5WXFGW0GQR1XS
AN3-CA NU[yWmsyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTN6LkG2NVUh|ryP NXWwbpF5W0GQR1XS
UACC-257 M3np[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTN6Lke5JO69VQ>? MkHEV2FPT0WU
MCF7 MmK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfGN4lKSzVyPUO5Mlg3OjlizszN MnvmV2FPT0WU
KP-N-YN MofMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTRyLkSyPFUh|ryP MUjTRW5ITVJ?
T98G MlS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HVe2lEPTB;NECuOFk2PyEQvF2= M2rIPXNCVkeHUh?=
HGC-27 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH60boJKSzVyPUSzMlI4PCEQvF2= M1fL[HNCVkeHUh?=
NCI-H1092 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTR|LkK4PVUh|ryP Mn\OV2FPT0WU
KARPAS-299 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYL1VIlVUUN3ME20N{4{ODdzIN88US=> Mn[wV2FPT0WU
LB1047-RCC MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfUTWM2OD12ND65PVU6KM7:TR?= M{jnTHNCVkeHUh?=
786-0 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXRTWM2OD12NT62OUDPxE1? NGLtNYxUSU6JRWK=
HCC2157 M1TqWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTR4LkCzOVkh|ryP M1TWeHNCVkeHUh?=
NY NF;KOHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFr0UGxKSzVyPUS2MlE4PzhizszN NUfSTVZHW0GQR1XS
EFM-19 M4rpeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvTfFhKSzVyPUS2Mlc2OzNizszN MnLCV2FPT0WU
EW-16 NGWzRZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfUToZTUUN3ME20Ok44QDB4IN88US=> Mn:2V2FPT0WU
UM-UC-3 NGTGNlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fyTmlEPTB;NE[uPFA2QSEQvF2= NHezbHJUSU6JRWK=
HT-29 MmnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzyUnVKSzVyPUS3Mlg4QTJizszN NGX6U45USU6JRWK=
LN-405 MnjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfuTWM2OD12OD6wPFI4KM7:TR?= NUDmVHN7W0GQR1XS
NCI-H727 M3X1VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTR6Lke3NlYh|ryP MWPTRW5ITVJ?
D-502MG MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[3ZmlEPTB;NEiuPVY4PiEQvF2= M3XKcHNCVkeHUh?=
GMS-10 MkexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjDOXp5UUN3ME20PU4zQTd2IN88US=> M4H4O3NCVkeHUh?=
MEL-JUSO NYGzOGJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HNdGlEPTB;NEmuN|Q4KM7:TR?= NIPLRpNUSU6JRWK=

... 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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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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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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    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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