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 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHvPFVzUUN3ME2wMlA4PDV5IN88US=> MVvTRW5ITVJ?
EoL-1-cell NED2XGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\VeWlEPTB;MD6xOFE3PiEQvF2= Ml7FV2FPT0WU
C32 NYWzV25HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnL4TWM2OD1yLkG1NVMyKM7:TR?= MoWwV2FPT0WU
M14 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTBwMkG3OVch|ryP NWTmZopiW0GQR1XS
CP50-MEL-B NEj0R4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnUTWM2OD1yLkK5O|g1KM7:TR?= MXHTRW5ITVJ?
A101D M1LNVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfLXHplUUN3ME2wMlMzPTh7IN88US=> NET6R3dUSU6JRWK=
G-361 M4LnTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTBwM{S2N|ch|ryP NYDT[ndtW0GQR1XS
HT-144 NX3tUXJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17ib2lEPTB;MD6zOlMzQSEQvF2= M{fV[nNCVkeHUh?=
ACN NUTOXmt2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTBwM{i0O|ch|ryP M1TSVXNCVkeHUh?=
COLO-829 NIPL[pJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3tTWM2OD1yLkO4PVY5KM7:TR?= MmPIV2FPT0WU
MEL-HO M{\XPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwNEGxO|kh|ryP M4K0d3NCVkeHUh?=
SH-4 NIHsd45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTBTWM2OD1yLkSxOFIzKM7:TR?= M1rEWnNCVkeHUh?=
SK-MEL-3 NYPKTW9UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEX1WJNKSzVyPUCuOVE2PjhizszN NFHUOVBUSU6JRWK=
A375 Mlu0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M360e2lEPTB;MD62O|M2QSEQvF2= M1fhOnNCVkeHUh?=
MMAC-SF MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTHcIpKSzVyPUCuOlg3OTRizszN M4DXWHNCVkeHUh?=
BHT-101 NF7WRplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoK2TWM2OD1yLkewO|AzKM7:TR?= M1XoNXNCVkeHUh?=
K5 NEX1SYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTBwN{[xOFgh|ryP NXG3W21DW0GQR1XS
BV-173 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHm1VJJKSzVyPUCuO|k3PDRizszN MmHHV2FPT0WU
RVH-421 NYHz[WJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXCTWM2OD1yLki2O|k3KM7:TR?= NGC0NY5USU6JRWK=
HCC2218 M2T2[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PR[2lEPTB;MD64O|g1PCEQvF2= NF\keVFUSU6JRWK=
WM-115 M1PiS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Tnb2lEPTB;MD64PFY6OiEQvF2= MWPTRW5ITVJ?
SK-MEL-28 M17kd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTFwMES1Olkh|ryP Ml:xV2FPT0WU
COLO-679 NXjxXnRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTFwMUC0OlQh|ryP MVXTRW5ITVJ?
MZ7-mel NVzUcW1wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvBTWM2OD1zLkG0PVY{KM7:TR?= NFOxXZNUSU6JRWK=
SK-MEL-30 Mn7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDIW3JKSzVyPUGuN|M{QDZizszN MWHTRW5ITVJ?
NCI-H209 NHviR4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrrTWM2OD1zLk[wPFYh|ryP M4Xqd3NCVkeHUh?=
HTC-C3 NFfyS4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjzTWM2OD1zLk[2Nlk1KM7:TR?= MX7TRW5ITVJ?
KARPAS-45 M4T0eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE[xe3FKSzVyPUKuNFQ6PzhizszN MXLTRW5ITVJ?
NCI-SNU-5 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTCTWM2OD1{LkGxPVY6KM7:TR?= MUHTRW5ITVJ?
KP-4 M1nySGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fRVmlEPTB;Mj6zNFc5PyEQvF2= NIHhNGlUSU6JRWK=
PA-1 M1\5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoC3TWM2OD1{LkeyOlc{KM7:TR?= MVXTRW5ITVJ?
HuO-3N1 M4X3bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3zTWM2OD1{Lki3PVQ3KM7:TR?= M4H5PXNCVkeHUh?=
NCI-H358 NHm2S2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHQTWM2OD1{LkmyNlMzKM7:TR?= NEHBVIxUSU6JRWK=
CTB-1 NXPqfJl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVSzfWw1UUN3ME2zMlQxOTd4IN88US=> MXLTRW5ITVJ?
697 NX36UVBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4e3dmlEPTB;Mz61OVI3PiEQvF2= MW\TRW5ITVJ?
CP66-MEL MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\vTWM2OD12LkG1PVI4KM7:TR?= M1HuU3NCVkeHUh?=
NB13 M4DD[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHn3SW9KSzVyPUSuOFkyPzlizszN NXzlfXhxW0GQR1XS
DBTRG-05MG Mnn5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjNXFVSUUN3ME20MlU{OzJ3IN88US=> M1K1WXNCVkeHUh?=
A2058 NVm3WIVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MomwTWM2OD12LkeyNVY1KM7:TR?= NHzHSpBUSU6JRWK=
KG-1 M2\seGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\seGRKSzVyPUSuO|M6ODhizszN MkLHV2FPT0WU
8305C MnyyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3wfIoxUUN3ME21MlE5PzNizszN MVTTRW5ITVJ?
RPMI-7951 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfWTWM2OD13LkiwNlg{KM7:TR?= MYLTRW5ITVJ?
CHL-1 MlPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPwTWM2OD13Lkm3OlA{KM7:TR?= NILTSmZUSU6JRWK=
TI-73 MnvIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\xemlEPTB;Nj6wNFkxOiEQvF2= NX;p[Yg6W0GQR1XS
HT-1080 NHr3emdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPKZY9EUUN3ME22MlExQTR4IN88US=> M4raOXNCVkeHUh?=
ES5 NInNRVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vEXWlEPTB;Nj6xOFkzPCEQvF2= MkTOV2FPT0WU
8-MG-BA MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LkTGlEPTB;Nj6xPFEzQSEQvF2= NXvYXpZ6W0GQR1XS
NB7 NXjpeoM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LTVmlEPTB;Nj6yNVM4OyEQvF2= MYHTRW5ITVJ?
H4 NEHGe2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTZwMkK0PVMh|ryP MX7TRW5ITVJ?
CAL-72 NFrXcZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTZwNEW0NlMh|ryP M17JTnNCVkeHUh?=
HCC1806 NX:1PG5pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTZwOEG5N|Eh|ryP MXzTRW5ITVJ?
BCPAP MnfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{myNmlEPTB;Nz6yNVc3PCEQvF2= NVrMfYZHW0GQR1XS
LB2241-RCC NWnkeZZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTdwM{[5NFch|ryP NInKcVVUSU6JRWK=
COLO-741 NULTZZRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlT4TWM2OD16LkCxOlc6KM7:TR?= NYfJeFNtW0GQR1XS
HSC-3 Mke0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXn6VY9uUUN3ME24MlA4ODZ6IN88US=> Mnf1V2FPT0WU
SW982 MoHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETacHhKSzVyPUiuOFE2OTZizszN M2rDSHNCVkeHUh?=
GCT MlPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRThwN{WzNVQh|ryP NIDHNYRUSU6JRWK=
KY821 M1PiZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3iUZVKSzVyPUmuNFUyPzhizszN MW\TRW5ITVJ?
JVM-3 M4nOdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jCdmlEPTB;OT61Olk6QSEQvF2= Mn7sV2FPT0WU
RS4-11 MmDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfm[Is6UUN3ME25MlYxPDhizszN NYjEXIFwW0GQR1XS
VA-ES-BJ Mk\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILld4NKSzVyPUGwMlAyPDlizszN NV3pOFBiW0GQR1XS
A431 M2PXNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjxV2pHUUN3ME2xNE41OjF{IN88US=> M1H4eXNCVkeHUh?=
LXF-289 M1P1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;3Vm1KSzVyPUGwMlQ2QCEQvF2= M37UR3NCVkeHUh?=
SK-MEL-24 NH7MR|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXYVoNKSzVyPUGwMlgzPzRizszN M1TqenNCVkeHUh?=
NOS-1 NILOS4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\YR2lEPTB;MUCuPFQ4OiEQvF2= Mn7HV2FPT0WU
KNS-62 M3PGZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTFzLkK0NFQh|ryP M4P1enNCVkeHUh?=
SK-HEP-1 NF;5UFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfVem9KSzVyPUGxMlM2OjdizszN Mlz2V2FPT0WU
A3-KAW MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTFzLkexO|gh|ryP NV3o[Y55W0GQR1XS
SK-LU-1 Mn76S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXnR|VKSzVyPUGyMlI3PTVizszN NXjETYJqW0GQR1XS
TYK-nu MkDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTF{LkO5N|Ih|ryP Mk\YV2FPT0WU
NMC-G1 MoDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\2OWV[UUN3ME2xNk43ODZ{IN88US=> NUfPNoxQW0GQR1XS
BB65-RCC NX\CXGRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITjU4lKSzVyPUGyMlcyPjlizszN Mkj6V2FPT0WU
QIMR-WIL MmXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLLe283UUN3ME2xNk45QDN|IN88US=> MXfTRW5ITVJ?
D-566MG NXHOb5RxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3j0bGlEPTB;MUOuPVU4PiEQvF2= NF\zRo5USU6JRWK=
KYSE-140 Ml\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTQTWM2OD1zND6wO|U{KM7:TR?= NXixW|JOW0GQR1XS
SCC-4 MoHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTF2LkOzOVkh|ryP NUTTdZdZW0GQR1XS
U251 M{iyNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXzTWM2OD1zND64OFkzKM7:TR?= MlfkV2FPT0WU
D-542MG M3r0VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XPcGlEPTB;MUSuPVIzOiEQvF2= M17y[nNCVkeHUh?=
LAMA-84 NGf3UJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXyZoFFUUN3ME2xOE46QTN{IN88US=> MYXTRW5ITVJ?
NCI-H720 MlXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEKzcIJKSzVyPUG1MlI3QDRizszN NVWxZ2FHW0GQR1XS
DEL M3TuNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDsdnNFUUN3ME2xOU41Ojl|IN88US=> NY\kb5RmW0GQR1XS
SBC-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPDVXp6UUN3ME2xOU41OzB3IN88US=> M3HpUnNCVkeHUh?=
ECC10 M3TCTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;HTWM2OD1zNT60OFU5KM7:TR?= MWnTRW5ITVJ?
Daoy Mn\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{T4V2lEPTB;MUWuO|YyPiEQvF2= MWXTRW5ITVJ?
SCH MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTF3Lke4N|Uh|ryP NWXTdohsW0GQR1XS
MZ2-MEL MmCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoL5TWM2OD1zNj6wOlQ3KM7:TR?= MnjzV2FPT0WU
CAL-12T NV64W|Z4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmOzTWM2OD1zNj60PFYzKM7:TR?= M2\5THNCVkeHUh?=
KE-37 NUTMe3dnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;PemVwUUN3ME2xOk45OTB5IN88US=> NX\G[JdWW0GQR1XS
LS-411N M2\JW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTF5LkGxPEDPxE1? MofNV2FPT0WU
NCI-H2228 MlTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPuUFJKUUN3ME2xO{4{ODdzIN88US=> NVXKR3dlW0GQR1XS
SK-MEL-2 NGf4OI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\NTWM2OD1zNz60PVY2KM7:TR?= NIjUbGFUSU6JRWK=
HN M2DObmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPlcHJ4UUN3ME2xO{44OjR6IN88US=> Ml3IV2FPT0WU
NCI-H1648 NEHEUYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DF[WlEPTB;MUeuPFE5KM7:TR?= NWnCb4tJW0GQR1XS
IA-LM MmX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TaWGlEPTB;MUiuN|E4OiEQvF2= MlTCV2FPT0WU
EW-13 MkW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37ub2lEPTB;MUiuOVcxQCEQvF2= MVfTRW5ITVJ?
YKG-1 MmTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETuTXRKSzVyPUG5MlU4OTFizszN NUPR[WE6W0GQR1XS
KNS-81-FD MoD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTQTWM2OD1zOT61PFU5KM7:TR?= MXHTRW5ITVJ?
23132-87 NXnt[ZluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV60ZVNSUUN3ME2xPU44PjR{IN88US=> MVrTRW5ITVJ?
NUGC-3 NHHPbGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfsUZlKSzVyPUG5Mlk5QDdizszN NInaW2lUSU6JRWK=
5637 M3v3UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJyLkC0O|gh|ryP NFfDfZFUSU6JRWK=
NCI-H1755 NV;vXVE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTJyLkS3OlQh|ryP NVnRT4V[W0GQR1XS
RH-18 MkLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nnOGlEPTB;MkCuOVc1QCEQvF2= NV7GWmtpW0GQR1XS
RXF393 NVu4UpFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHKS5BTUUN3ME2yNE43PzV4IN88US=> MV3TRW5ITVJ?
LU-134-A NWr6UGNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTJyLkewOVYh|ryP MVvTRW5ITVJ?
TE-12 MmHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoWyTWM2OD1{MD63NlAyKM7:TR?= NXnFcXZwW0GQR1XS
MOLT-4 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvNTWM2OD1{MT6xPVE2KM7:TR?= NFHkT5ZUSU6JRWK=
IGR-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DmdmlEPTB;MkGuN|c6PiEQvF2= NXfxTmVEW0GQR1XS
HOP-92 M3TNV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTJzLkS5PFch|ryP NWHvcFVNW0GQR1XS
SK-MES-1 MmLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LXfWlEPTB;MkGuO|M5OSEQvF2= Mn;DV2FPT0WU
LU-65 MlXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTJzLki2NlQh|ryP NHKwb45USU6JRWK=
MS-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LlUmlEPTB;MkKuNVIxOyEQvF2= Mlz1V2FPT0WU
LoVo NETCXZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk[0TWM2OD1{Mj6yOFQh|ryP NV23e4l1W0GQR1XS
A704 NHPmXXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXe4W3lnUUN3ME2yNk42OTV3IN88US=> M1PCcHNCVkeHUh?=
HT-1376 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjxW|FKSzVyPUKyMlYxPTlizszN M1\u[HNCVkeHUh?=
IST-MEL1 Mn;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLnS2V5UUN3ME2yNk43PzVzIN88US=> MXzTRW5ITVJ?
Ramos-2G6-4C10 Mn6wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXMTWM2OD1{Mj63N|Y3KM7:TR?= MlnLV2FPT0WU
T47D Mm\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LBRmlEPTB;MkKuO|k4QSEQvF2= NX20ZZVbW0GQR1XS
HT-1197 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3ITWM2OD1{Mz6wPFE4KM7:TR?= MnTPV2FPT0WU
LB2518-MEL NYH0UoZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVm1RlhLUUN3ME2yN{43PDF{IN88US=> NFzVWWxUSU6JRWK=
J-RT3-T3-5 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDvR25KSzVyPUK0Mlc2QTVizszN MVrTRW5ITVJ?
SK-NEP-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTOTWM2OD1{ND64O|Q1KM7:TR?= NFPxdXpUSU6JRWK=
NCI-H526 MmjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3FfIxKSzVyPUK1MlAxOjNizszN MmPBV2FPT0WU
IST-SL1 NVK4eFF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTJ3LkK3OVEh|ryP M1zMZ3NCVkeHUh?=
HH MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfVXWZCUUN3ME2yOU4{OTl{IN88US=> MkLxV2FPT0WU
NCI-H82 NUTWUYQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoK0TWM2OD1{NT65N|gh|ryP NYPoWol{W0GQR1XS
SNU-449 M2r2emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\UV2lEPTB;MkeuNlAyQCEQvF2= MlfjV2FPT0WU
COR-L23 NUW4VnhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moj5TWM2OD1{Nz6yPFE{KM7:TR?= M3;aTHNCVkeHUh?=
LOXIMVI NHm5b4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTJ5LkO2PEDPxE1? M3TUPXNCVkeHUh?=
GR-ST NWjLbW5oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nNbmlEPTB;MkeuOlcxPiEQvF2= MmnaV2FPT0WU
NCI-SNU-1 NXL4bHRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTJ5Lkm0OEDPxE1? M4XmNnNCVkeHUh?=
ALL-PO M2TRSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrDbm1wUUN3ME2yPE4yPjB2IN88US=> MlTPV2FPT0WU
ML-2 NHnWUGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PQcGlEPTB;MkiuNlgyPCEQvF2= Mo\rV2FPT0WU
HOP-62 NXn3NI5GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLjTWM2OD1{OD63NVMh|ryP M2O1TnNCVkeHUh?=
EGI-1 NX;qT5ZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTJ6Lki4OFUh|ryP NF7rNHRUSU6JRWK=
TCCSUP MmXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmr2TWM2OD1{OD65NlczKM7:TR?= M3vnenNCVkeHUh?=
LB996-RCC NWrnOJlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXrTWM2OD1{OT61OlgzKM7:TR?= MVvTRW5ITVJ?
LCLC-97TM1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHQZY9MUUN3ME2zNk4yQTZ2IN88US=> NIrPcmpUSU6JRWK=
NCI-H1304 NEXyZppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLiTWM2OD1|Mj6zN|AyKM7:TR?= Mn;lV2FPT0WU
KP-N-YS Mk\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoraTWM2OD1|Mj61PVc{KM7:TR?= NV;RdpRwW0GQR1XS
NCI-H1770 M1XvTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPveZBKSzVyPUOzMlE3PDhizszN M3PSbHNCVkeHUh?=
EM-2 NYnoepFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfTOI5KSzVyPUOzMlY2ODRizszN M4[5bHNCVkeHUh?=
ChaGo-K-1 MoDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXmTWM2OD1|Mz63NlM3KM7:TR?= M{TwVnNCVkeHUh?=
ACHN MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XlfmlEPTB;M{OuPFM5PSEQvF2= MWTTRW5ITVJ?
MN-60 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nJTWlEPTB;M{OuPFU1PCEQvF2= MoPqV2FPT0WU
EW-18 NIDiSJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvuRXV7UUN3ME2zN{45QTdzIN88US=> MnPYV2FPT0WU
KGN MlvuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjwdWtiUUN3ME2zOU44Ojl{IN88US=> NICwVYlUSU6JRWK=
U031 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTN3LkixN|Ih|ryP MW\TRW5ITVJ?
HMV-II M2rIZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTN4LkC3O|Qh|ryP MYfTRW5ITVJ?
L-363 NVjJR5loT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTN5Lk[0OVUh|ryP MVHTRW5ITVJ?
NCI-H1155 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWThWpZsUUN3ME2zPE4xODF3IN88US=> MljUV2FPT0WU
NCI-H1793 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;4ZnJKSzVyPUO4MlExOjZizszN NXXGXnNiW0GQR1XS
P30-OHK M1riZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTN6LkGzN|Ih|ryP NIrnOJVUSU6JRWK=
AN3-CA NYjmXWFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn:0TWM2OD1|OD6xOlE2KM7:TR?= NGL1SIxUSU6JRWK=
UACC-257 Mn:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTN6Lke5JO69VQ>? NVHneGRWW0GQR1XS
MCF7 NITwdpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TmUWlEPTB;M{muPFYzQSEQvF2= Ml;zV2FPT0WU
KP-N-YN MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTRyLkSyPFUh|ryP M1rIWXNCVkeHUh?=
T98G MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXKwU5E{UUN3ME20NE41QTV5IN88US=> MVTTRW5ITVJ?
HGC-27 NGLrc41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYn6R2JJUUN3ME20N{4zPzRizszN M1HxV3NCVkeHUh?=
NCI-H1092 NWLtPZNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTR|LkK4PVUh|ryP M2DvOXNCVkeHUh?=
KARPAS-299 MofDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjlPGFKSzVyPUSzMlMxPzFizszN M3\2UXNCVkeHUh?=
LB1047-RCC NWrHV5JET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\3TGlEPTB;NESuPVk2QSEQvF2= MmHCV2FPT0WU
786-0 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWSwUWFzUUN3ME20OU43PSEQvF2= NIm0VndUSU6JRWK=
HCC2157 NXfUXYdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHzO3dRUUN3ME20Ok4xOzV7IN88US=> NVSxcWc4W0GQR1XS
NY Mn[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFn1WFBKSzVyPUS2MlE4PzhizszN MYPTRW5ITVJ?
EFM-19 NIjLRoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHzO5NwUUN3ME20Ok44PTN|IN88US=> Ml21V2FPT0WU
EW-16 NEPtS|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTR4Lke4NFYh|ryP MWrTRW5ITVJ?
UM-UC-3 NIHDTZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjZXppKSzVyPUS2MlgxPTlizszN NFLKephUSU6JRWK=
HT-29 NILyc|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1WxXWlEPTB;NEeuPFc6OiEQvF2= NIHDV2tUSU6JRWK=
LN-405 NHjHe5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PzSGlEPTB;NEiuNFgzPyEQvF2= NHywZWdUSU6JRWK=
NCI-H727 NUTQcHFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHTcnBKSzVyPUS4Mlc4OjZizszN MlPUV2FPT0WU
D-502MG MoDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nSOWlEPTB;NEiuPVY4PiEQvF2= MnLxV2FPT0WU
GMS-10 M{XBfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1WxN2lEPTB;NEmuNlk4PCEQvF2= NXzNNpkyW0GQR1XS
MEL-JUSO MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fpTmlEPTB;NEmuN|Q4KM7:TR?= M{\mfHNCVkeHUh?=

... 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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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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