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 NGXiOlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTBwMEe0OVch|ryP NFj2OZFUSU6JRWK=
EoL-1-cell NFXFcFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXKdVhKSzVyPUCuNVQyPjZizszN M3z5WHNCVkeHUh?=
C32 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXWbXpKSzVyPUCuNVUyOzFizszN M{XNOnNCVkeHUh?=
M14 MoPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3z1WGlEPTB;MD6yNVc2PyEQvF2= Mn\JV2FPT0WU
CP50-MEL-B M3TBSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrNcFR6UUN3ME2wMlI6Pzh2IN88US=> Ml:yV2FPT0WU
A101D NYj2[ZRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwM{K1PFkh|ryP M4LQfHNCVkeHUh?=
G-361 M1;M[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTBwM{S2N|ch|ryP M2LKb3NCVkeHUh?=
HT-144 M1vQc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPxbXVKSzVyPUCuN|Y{OjlizszN M1y3eHNCVkeHUh?=
ACN MmS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DsRmlEPTB;MD6zPFQ4PyEQvF2= NWXPWlh5W0GQR1XS
COLO-829 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIGyXJlKSzVyPUCuN|g6PjhizszN MWTTRW5ITVJ?
MEL-HO MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NET3U5JKSzVyPUCuOFEyPzlizszN MVnTRW5ITVJ?
SH-4 M4TxOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MluyTWM2OD1yLkSxOFIzKM7:TR?= NV3U[VZ6W0GQR1XS
SK-MEL-3 M{fofGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2n4OWlEPTB;MD61NVU3QCEQvF2= Ml\CV2FPT0WU
A375 NWjQZXJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fQUWlEPTB;MD62O|M2QSEQvF2= NUjHZpd7W0GQR1XS
MMAC-SF M{fPRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Ll[WlEPTB;MD62PFYyPCEQvF2= MVrTRW5ITVJ?
BHT-101 MkfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3ZdWhKSzVyPUCuO|A4ODJizszN M1z3SnNCVkeHUh?=
K5 M4r2S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoT6TWM2OD1yLke2NVQ5KM7:TR?= NILHZo5USU6JRWK=
BV-173 NIHVcGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LCVWlEPTB;MD63PVY1PCEQvF2= M{[xZnNCVkeHUh?=
RVH-421 NWT5[XRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[2TWM2OD1yLki2O|k3KM7:TR?= NFXYclBUSU6JRWK=
HCC2218 M2HJfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHYdoFOUUN3ME2wMlg4QDR2IN88US=> MWHTRW5ITVJ?
WM-115 NYT2[mp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELJ[HRKSzVyPUCuPFg3QTJizszN NFvUe|BUSU6JRWK=
SK-MEL-28 NYfqVZhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknTTWM2OD1zLkC0OVY6KM7:TR?= NFLk[VlUSU6JRWK=
COLO-679 NGWzXGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTFwMUC0OlQh|ryP M2r1Z3NCVkeHUh?=
MZ7-mel MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;nWmlEPTB;MT6xOFk3OyEQvF2= NH3tUXNUSU6JRWK=
SK-MEL-30 MmiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1P1PWlEPTB;MT6zN|M5PiEQvF2= Mmj3V2FPT0WU
NCI-H209 NV2zeVZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnh[Y9WUUN3ME2xMlYxQDZizszN M3zxWnNCVkeHUh?=
HTC-C3 M1fncWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HoZmlEPTB;MT62OlI6PCEQvF2= MYHTRW5ITVJ?
KARPAS-45 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TDVGlEPTB;Mj6wOFk4QCEQvF2= NF70VHBUSU6JRWK=
NCI-SNU-5 NEK2[2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTJwMUG5Olkh|ryP Mn\DV2FPT0WU
KP-4 M4\tVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPwTGZvUUN3ME2yMlMxPzh5IN88US=> MlrBV2FPT0WU
PA-1 NFf1bZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LHNWlEPTB;Mj63NlY4OyEQvF2= NYjsfJNPW0GQR1XS
HuO-3N1 NWfke5FmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIL4VWtKSzVyPUKuPFc6PDZizszN NGjoZolUSU6JRWK=
NCI-H358 NIn0VZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XOb2lEPTB;Mj65NlI{OiEQvF2= NYrwSnRSW0GQR1XS
CTB-1 NHuxe2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTNwNECxO|Yh|ryP NEHibFJUSU6JRWK=
697 NFHqcXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTNwNUWyOlYh|ryP NGjofmlUSU6JRWK=
CP66-MEL M3PKWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LGT2lEPTB;ND6xOVkzPyEQvF2= NU[y[Jp[W0GQR1XS
NB13 NV7EcZVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPFO4lKSzVyPUSuOFkyPzlizszN M3PYd3NCVkeHUh?=
DBTRG-05MG Mn:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXsPGM3UUN3ME20MlU{OzJ3IN88US=> MlLnV2FPT0WU
A2058 NGOzNmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXL5Uot2UUN3ME20MlczOTZ2IN88US=> NYHtVldsW0GQR1XS
KG-1 NF7nUVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\uTWM2OD12LkezPVA5KM7:TR?= MlT6V2FPT0WU
8305C MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvN[o9KSzVyPUWuNVg4OyEQvF2= NYXCcoNQW0GQR1XS
RPMI-7951 MoT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnBTWM2OD13LkiwNlg{KM7:TR?= MU\TRW5ITVJ?
CHL-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHwdJN4UUN3ME21Mlk4PjB|IN88US=> MX;TRW5ITVJ?
TI-73 MonTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTZwMEC5NFIh|ryP M3rPd3NCVkeHUh?=
HT-1080 MkLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTZwMUC5OFYh|ryP MVzTRW5ITVJ?
ES5 MlXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XUc2lEPTB;Nj6xOFkzPCEQvF2= NYTuVG9QW0GQR1XS
8-MG-BA M{L6U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjqOlRKSzVyPU[uNVgyOjlizszN Mnj3V2FPT0WU
NB7 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4m5WGlEPTB;Nj6yNVM4OyEQvF2= MVPTRW5ITVJ?
H4 NGixXo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLDeYVKSzVyPU[uNlI1QTNizszN MmHoV2FPT0WU
CAL-72 NVvGOHlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTZwNEW0NlMh|ryP NGrU[YlUSU6JRWK=
HCC1806 NITGUoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDKVVVKSzVyPU[uPFE6OzFizszN NFLGfHZUSU6JRWK=
BCPAP MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTdwMkG3OlQh|ryP MoLVV2FPT0WU
LB2241-RCC NFXv[JNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnW3TWM2OD15LkO2PVA4KM7:TR?= M2jUcXNCVkeHUh?=
COLO-741 M1TGWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PxZWlEPTB;OD6wNVY4QSEQvF2= NEXRWoJUSU6JRWK=
HSC-3 MoH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfWS2NKSzVyPUiuNFcxPjhizszN NYLPSFZ[W0GQR1XS
SW982 Mm\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPBTWM2OD16LkSxOVE3KM7:TR?= MYLTRW5ITVJ?
GCT NWS1ZXU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPMTWM2OD16Lke1N|E1KM7:TR?= NYfY[GV6W0GQR1XS
KY821 M{HS[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXVV|FKSzVyPUmuNFUyPzhizszN MlrDV2FPT0WU
JVM-3 MlWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3:yeGlEPTB;OT61Olk6QSEQvF2= NWO1SGdWW0GQR1XS
RS4-11 M32wTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILZWFlKSzVyPUmuOlA1QCEQvF2= M2XRSnNCVkeHUh?=
VA-ES-BJ M{CzTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFyLkCxOFkh|ryP M3fwSXNCVkeHUh?=
A431 NXzifYxOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7zTWM2OD1zMD60NlEzKM7:TR?= M1\LTXNCVkeHUh?=
LXF-289 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4CwT2lEPTB;MUCuOFU5KM7:TR?= MVPTRW5ITVJ?
SK-MEL-24 MoHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFG3SW1KSzVyPUGwMlgzPzRizszN NHnoeYJUSU6JRWK=
NOS-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHCbYxKSzVyPUGwMlg1PzJizszN NIfKOmxUSU6JRWK=
KNS-62 NWjYVJpCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HDNGlEPTB;MUGuNlQxPCEQvF2= Mof4V2FPT0WU
SK-HEP-1 NWHYV2FXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjKTWM2OD1zMT6zOVI4KM7:TR?= NUe3UnlEW0GQR1XS
A3-KAW NHKx[4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTFzLkexO|gh|ryP NFzoN5dUSU6JRWK=
SK-LU-1 Mn6xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHLd2NKSzVyPUGyMlI3PTVizszN M4rGO3NCVkeHUh?=
TYK-nu NYP1bmNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXBTWM2OD1zMj6zPVMzKM7:TR?= M4TGW3NCVkeHUh?=
NMC-G1 M1LsNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTZfHJKSzVyPUGyMlYxPjJizszN NFXDNXlUSU6JRWK=
BB65-RCC M3jJNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTF{LkexOlkh|ryP MXzTRW5ITVJ?
QIMR-WIL MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvtPI5KSzVyPUGyMlg5OzNizszN NU\YU4FJW0GQR1XS
D-566MG MoPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Tp[GlEPTB;MUOuPVU4PiEQvF2= NWnxRYdLW0GQR1XS
KYSE-140 M1;1OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2GzV2lEPTB;MUSuNFc2OyEQvF2= M1jMPHNCVkeHUh?=
SCC-4 M3P4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HZeGlEPTB;MUSuN|M2QSEQvF2= MlnJV2FPT0WU
U251 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mom4TWM2OD1zND64OFkzKM7:TR?= NFL2[2JUSU6JRWK=
D-542MG NXPwd21MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjrNoNKSzVyPUG0MlkzOjJizszN MYTTRW5ITVJ?
LAMA-84 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorDTWM2OD1zND65PVMzKM7:TR?= MXrTRW5ITVJ?
NCI-H720 MlLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTF3LkK2PFQh|ryP MnLLV2FPT0WU
DEL M{fPXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUK1Zm95UUN3ME2xOU41Ojl|IN88US=> NXu1UIJHW0GQR1XS
SBC-1 M3uzd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTF3LkSzNFUh|ryP NG\XeVZUSU6JRWK=
ECC10 NUDEW5N4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlqzTWM2OD1zNT60OFU5KM7:TR?= MnjkV2FPT0WU
Daoy NX3oTFBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDRbo5KSzVyPUG1Mlc3OTZizszN M3G0VnNCVkeHUh?=
SCH M4PNdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfCeIREUUN3ME2xOU44QDN3IN88US=> M{\nUHNCVkeHUh?=
MZ2-MEL MmDoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTF4LkC2OFYh|ryP NIXIV2VUSU6JRWK=
CAL-12T NFTWZZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTF4LkS4OlIh|ryP NEHXcHRUSU6JRWK=
KE-37 NYfuWoJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\NNWlEPTB;MU[uPFExPyEQvF2= M2[4Z3NCVkeHUh?=
LS-411N NHf3dlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXFTWM2OD1zNz6xNVgh|ryP NH\yOFlUSU6JRWK=
NCI-H2228 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PHcWlEPTB;MUeuN|A4OSEQvF2= Mmr3V2FPT0WU
SK-MEL-2 MnvSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml2zTWM2OD1zNz60PVY2KM7:TR?= NFvpPGlUSU6JRWK=
HN MoW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zTc2lEPTB;MUeuO|I1QCEQvF2= MYfTRW5ITVJ?
NCI-H1648 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTF5LkixPEDPxE1? NGrhc3pUSU6JRWK=
IA-LM NYnvWWNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTF6LkOxO|Ih|ryP NVfu[IdYW0GQR1XS
EW-13 MlfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PjUWlEPTB;MUiuOVcxQCEQvF2= NVOx[ZJtW0GQR1XS
YKG-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnMcmlQUUN3ME2xPU42PzFzIN88US=> MlzaV2FPT0WU
KNS-81-FD MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHZemZKSzVyPUG5MlU5PThizszN NWj6R2N[W0GQR1XS
23132-87 NW\BXINwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnC[JNKSzVyPUG5Mlc3PDJizszN NY\lemdZW0GQR1XS
NUGC-3 NXHjU2lmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTF7Lkm4PFch|ryP NInoOVRUSU6JRWK=
5637 NFHxdJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTJyLkC0O|gh|ryP MoDrV2FPT0WU
NCI-H1755 M1qwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInZNY5KSzVyPUKwMlQ4PjRizszN NF7qVGRUSU6JRWK=
RH-18 NWXjcGo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnCOoJ7UUN3ME2yNE42PzR6IN88US=> MkGzV2FPT0WU
RXF393 M3rmNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTJyLk[3OVYh|ryP Ml[1V2FPT0WU
LU-134-A MkfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\jN|c3UUN3ME2yNE44ODV4IN88US=> NEnD[XpUSU6JRWK=
TE-12 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn:wTWM2OD1{MD63NlAyKM7:TR?= MX3TRW5ITVJ?
MOLT-4 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTJzLkG5NVUh|ryP NVzRXZlGW0GQR1XS
IGR-1 MlfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLMTWM2OD1{MT6zO|k3KM7:TR?= NYfORpJ6W0GQR1XS
HOP-92 NYHlOY5UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fESmlEPTB;MkGuOFk5PyEQvF2= NEXHRnZUSU6JRWK=
SK-MES-1 MnvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7icZZLUUN3ME2yNU44OzhzIN88US=> NWnuWlBEW0GQR1XS
LU-65 M4XROGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\5WJVKSzVyPUKxMlg3OjRizszN MnfTV2FPT0WU
MS-1 NX\vS|VjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX62ZpZyUUN3ME2yNk4yOjB|IN88US=> MkSxV2FPT0WU
LoVo NUnpb4pRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjoVYtTUUN3ME2yNk4zPDRizszN NIHXcHVUSU6JRWK=
A704 NIjtV5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfFZVZKSzVyPUKyMlUyPTVizszN M3\XXnNCVkeHUh?=
HT-1376 MmP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTBTWM2OD1{Mj62NFU6KM7:TR?= Mlm1V2FPT0WU
IST-MEL1 NYjEUncxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTJ{Lk[3OVEh|ryP MmTaV2FPT0WU
Ramos-2G6-4C10 Mkn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWG5N|RzUUN3ME2yNk44OzZ4IN88US=> NVvTNWNHW0GQR1XS
T47D M{nSN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fQTGlEPTB;MkKuO|k4QSEQvF2= M1vxfXNCVkeHUh?=
HT-1197 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXL[lBKSzVyPUKzMlA5OTdizszN MXfTRW5ITVJ?
LB2518-MEL MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nGUGlEPTB;MkOuOlQyOiEQvF2= MV\TRW5ITVJ?
J-RT3-T3-5 Ml\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrvb5RIUUN3ME2yOE44PTl3IN88US=> NVzUZnE{W0GQR1XS
SK-NEP-1 NWjaO2VNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\YTWM2OD1{ND64O|Q1KM7:TR?= NYHwTZNxW0GQR1XS
NCI-H526 NHrYR4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWWyNHRUUUN3ME2yOU4xODJ|IN88US=> Mk[yV2FPT0WU
IST-SL1 MlPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\oWG9pUUN3ME2yOU4zPzVzIN88US=> Mo\wV2FPT0WU
HH M3GwSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJ3LkOxPVIh|ryP M3zESnNCVkeHUh?=
NCI-H82 NWXVNWtYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTpTWM2OD1{NT65N|gh|ryP NIrhSYVUSU6JRWK=
SNU-449 NF;pbFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4izW2lEPTB;MkeuNlAyQCEQvF2= MUnTRW5ITVJ?
COR-L23 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LNU2lEPTB;MkeuNlgyOyEQvF2= MV7TRW5ITVJ?
LOXIMVI NIfRRWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnmPIdKSzVyPUK3MlM3QCEQvF2= MYXTRW5ITVJ?
GR-ST MlrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{CwRmlEPTB;MkeuOlcxPiEQvF2= MYTTRW5ITVJ?
NCI-SNU-1 NIPmVo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfDXpRKSzVyPUK3Mlk1PCEQvF2= NUDseYRiW0GQR1XS
ALL-PO M1\F[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTJ6LkG2NFQh|ryP NHS2fJdUSU6JRWK=
ML-2 MnLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\uVWx4UUN3ME2yPE4zQDF2IN88US=> MXvTRW5ITVJ?
HOP-62 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVqwUnFHUUN3ME2yPE44OTNizszN M2fUXHNCVkeHUh?=
EGI-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzaTWM2OD1{OD64PFQ2KM7:TR?= MV3TRW5ITVJ?
TCCSUP NFfqPIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3UTWM2OD1{OD65NlczKM7:TR?= MkSwV2FPT0WU
LB996-RCC NX\PXpEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILKcFBKSzVyPUK5MlU3QDJizszN NH\HdFNUSU6JRWK=
LCLC-97TM1 NIDXVZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnHZnZ[UUN3ME2zNk4yQTZ2IN88US=> NI[yNHFUSU6JRWK=
NCI-H1304 MmfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3KzbmlEPTB;M{KuN|MxOSEQvF2= NX3iNnhHW0GQR1XS
KP-N-YS M4DyRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjkdoVKSzVyPUOyMlU6PzNizszN NF7He4xUSU6JRWK=
NCI-H1770 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4m3VWlEPTB;M{OuNVY1QCEQvF2= NX\R[ppHW0GQR1XS
EM-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLkV3RJUUN3ME2zN{43PTB2IN88US=> M17NPXNCVkeHUh?=
ChaGo-K-1 NEXRS2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTN|LkeyN|Yh|ryP NWTke21WW0GQR1XS
ACHN NI\CUZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnWZ4pKSzVyPUOzMlg{QDVizszN M{T4VnNCVkeHUh?=
MN-60 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYe1T4EzUUN3ME2zN{45PTR2IN88US=> M2TMPHNCVkeHUh?=
EW-18 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTN|Lki5O|Eh|ryP Mo\FV2FPT0WU
KGN M{LBSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEO0XGdKSzVyPUO1MlczQTJizszN M4\KSnNCVkeHUh?=
U031 NWO1d41IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn31TWM2OD1|NT64NVMzKM7:TR?= MlnLV2FPT0WU
HMV-II NVnHd454T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVu1fIk2UUN3ME2zOk4xPzd2IN88US=> MlO1V2FPT0WU
L-363 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7MeW9KSzVyPUO3MlY1PTVizszN M37XV3NCVkeHUh?=
NCI-H1155 MnnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDHTWM2OD1|OD6wNFE2KM7:TR?= NEXIbo1USU6JRWK=
NCI-H1793 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTN6LkGwNlYh|ryP NFXFZYNUSU6JRWK=
P30-OHK MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVX2emRMUUN3ME2zPE4yOzN{IN88US=> Mn3RV2FPT0WU
AN3-CA NW\PWXA{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTN6LkG2NVUh|ryP NGKzWolUSU6JRWK=
UACC-257 NH7yd3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NImyXIVKSzVyPUO4Mlc6KM7:TR?= NU\WZ45OW0GQR1XS
MCF7 M3O0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{f6bWlEPTB;M{muPFYzQSEQvF2= MWPTRW5ITVJ?
KP-N-YN NFjYN|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTLTWM2OD12MD60Nlg2KM7:TR?= MmrsV2FPT0WU
T98G MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTRyLkS5OVch|ryP M2\DeHNCVkeHUh?=
HGC-27 NHXHdJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXOelZKSzVyPUSzMlI4PCEQvF2= MkTBV2FPT0WU
NCI-H1092 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HIfmlEPTB;NEOuNlg6PSEQvF2= NIjMWFZUSU6JRWK=
KARPAS-299 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTTTWM2OD12Mz6zNFcyKM7:TR?= MX;TRW5ITVJ?
LB1047-RCC MmLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHydHpxUUN3ME20OE46QTV7IN88US=> MX\TRW5ITVJ?
786-0 NUj1[WNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPvUWxKSzVyPUS1MlY2KM7:TR?= M4nLPXNCVkeHUh?=
HCC2157 M3\PdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DHbGlEPTB;NE[uNFM2QSEQvF2= NF3McJlUSU6JRWK=
NY M{Tj[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXDTWM2OD12Nj6xO|c5KM7:TR?= MlW0V2FPT0WU
EFM-19 M33hfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTR4Lke1N|Mh|ryP M{HYSnNCVkeHUh?=
EW-16 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7wTWM2OD12Nj63PFA3KM7:TR?= M323dnNCVkeHUh?=
UM-UC-3 Mn3YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfqTWM2OD12Nj64NFU6KM7:TR?= MoW0V2FPT0WU
HT-29 NXuxN2ppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3we4hKSzVyPUS3Mlg4QTJizszN M4izVnNCVkeHUh?=
LN-405 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXrTWM2OD12OD6wPFI4KM7:TR?= M{HrUXNCVkeHUh?=
NCI-H727 M160Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTR6Lke3NlYh|ryP M1r3Z3NCVkeHUh?=
D-502MG NGnh[GJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrQUW9KSzVyPUS4Mlk3PzZizszN MUnTRW5ITVJ?
GMS-10 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTR7LkK5O|Qh|ryP MUTTRW5ITVJ?
MEL-JUSO MnnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\KTWM2OD12OT6zOFch|ryP Ml;LV2FPT0WU

... 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)

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)

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    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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