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 NX7uOmd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnmTWM2OD1yLkC3OFU4KM7:TR?= M1P2VnNCVkeHUh?=
EoL-1-cell M3XRemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTWWGtzUUN3ME2wMlE1OTZ4IN88US=> Ml\4V2FPT0WU
C32 Mk[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3RVXZKUUN3ME2wMlE2OTNzIN88US=> MYrTRW5ITVJ?
M14 NIn5VWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfWOoxKSzVyPUCuNlE4PTdizszN M3PQXnNCVkeHUh?=
CP50-MEL-B MnHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjTbmo4UUN3ME2wMlI6Pzh2IN88US=> NH:wS3BUSU6JRWK=
A101D Mk\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTBwM{K1PFkh|ryP MkPoV2FPT0WU
G-361 M4faZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PheGlEPTB;MD6zOFY{PyEQvF2= NFy1XWRUSU6JRWK=
HT-144 NU[2W257T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7IRnVKSzVyPUCuN|Y{OjlizszN NYrpSI1NW0GQR1XS
ACN M3\5b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\XNlZxUUN3ME2wMlM5PDd5IN88US=> Mo\0V2FPT0WU
COLO-829 NGn2ZlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXyO4FlUUN3ME2wMlM5QTZ6IN88US=> MknZV2FPT0WU
MEL-HO MkPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrjTWM2OD1yLkSxNVc6KM7:TR?= MmD5V2FPT0WU
SH-4 M3:ycWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfGTWM2OD1yLkSxOFIzKM7:TR?= Mnj5V2FPT0WU
SK-MEL-3 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4f2RmlEPTB;MD61NVU3QCEQvF2= NW\ucW1GW0GQR1XS
A375 NF\0W2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTHTWM2OD1yLk[3N|U6KM7:TR?= MlnlV2FPT0WU
MMAC-SF M1excWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwNki2NVQh|ryP M4\NdXNCVkeHUh?=
BHT-101 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHVdpFJUUN3ME2wMlcxPzB{IN88US=> NHL1O2tUSU6JRWK=
K5 MnK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzYTWM2OD1yLke2NVQ5KM7:TR?= NHGzZVBUSU6JRWK=
BV-173 NF7sTXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTBwN{m2OFQh|ryP NFnhS|hUSU6JRWK=
RVH-421 NVqyPFQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVS3blBYUUN3ME2wMlg3Pzl4IN88US=> NVz5VXBxW0GQR1XS
HCC2218 NFuwZlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwOEe4OFQh|ryP NV;M[nFzW0GQR1XS
WM-115 MljLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4[4eWlEPTB;MD64PFY6OiEQvF2= NETmd|VUSU6JRWK=
SK-MEL-28 NYjndWJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjaRZNKSzVyPUGuNFQ2PjlizszN M4DLOnNCVkeHUh?=
COLO-679 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33t[mlEPTB;MT6xNFQ3PCEQvF2= M1GzcXNCVkeHUh?=
MZ7-mel M4KzTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\mTWM2OD1zLkG0PVY{KM7:TR?= Mlj3V2FPT0WU
SK-MEL-30 NH2w[2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljITWM2OD1zLkOzN|g3KM7:TR?= NYLpeWg{W0GQR1XS
NCI-H209 NEDDRlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfTfHRKSzVyPUGuOlA5PiEQvF2= M1vZfnNCVkeHUh?=
HTC-C3 M{XEUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\IR|ZKSzVyPUGuOlYzQTRizszN M{D1[nNCVkeHUh?=
KARPAS-45 NYf2SpEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnBTJRKSzVyPUKuNFQ6PzhizszN MV3TRW5ITVJ?
NCI-SNU-5 MlexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PB[WlEPTB;Mj6xNVk3QSEQvF2= NF\oNZNUSU6JRWK=
KP-4 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknwTWM2OD1{LkOwO|g4KM7:TR?= Mk\CV2FPT0WU
PA-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXJfXZKSzVyPUKuO|I3PzNizszN MmXpV2FPT0WU
HuO-3N1 M4\y[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Dx[GlEPTB;Mj64O|k1PiEQvF2= NH61V|dUSU6JRWK=
NCI-H358 NYjjXZcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HmT2lEPTB;Mj65NlI{OiEQvF2= NFexZ29USU6JRWK=
CTB-1 NXnlbIRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Hz[2lEPTB;Mz60NFE4PiEQvF2= M1:yOXNCVkeHUh?=
697 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3BZm5XUUN3ME2zMlU2OjZ4IN88US=> M4LqeXNCVkeHUh?=
CP66-MEL NEm1SYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGH6SVBKSzVyPUSuNVU6OjdizszN NVXTfm5GW0GQR1XS
NB13 MkjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTRwNEmxO|kh|ryP MVTTRW5ITVJ?
DBTRG-05MG NX3BXJpqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfQNHZDUUN3ME20MlU{OzJ3IN88US=> M2HBOHNCVkeHUh?=
A2058 MlPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXziTHVQUUN3ME20MlczOTZ2IN88US=> NF7lVYlUSU6JRWK=
KG-1 M2fQV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTRwN{O5NFgh|ryP MXLTRW5ITVJ?
8305C MlnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGf3enhKSzVyPUWuNVg4OyEQvF2= NX\TcWpTW0GQR1XS
RPMI-7951 NHi5N3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jYcGlEPTB;NT64NFI5OyEQvF2= NUH4b3M2W0GQR1XS
CHL-1 MlvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF6zeVRKSzVyPUWuPVc3ODNizszN M3fD[HNCVkeHUh?=
TI-73 NXK4XIdUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XXbGlEPTB;Nj6wNFkxOiEQvF2= M2L0cnNCVkeHUh?=
HT-1080 NW\seJJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzoRWU5UUN3ME22MlExQTR4IN88US=> MmfPV2FPT0WU
ES5 M13iU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEiyUFdKSzVyPU[uNVQ6OjRizszN M4rIcnNCVkeHUh?=
8-MG-BA M2DpWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\4W2lEPTB;Nj6xPFEzQSEQvF2= NXnJbmRYW0GQR1XS
NB7 MmHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTZwMkGzO|Mh|ryP MVvTRW5ITVJ?
H4 NEP1eWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXFbmZKSzVyPU[uNlI1QTNizszN NXjycHQ3W0GQR1XS
CAL-72 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;Y[ZZKSzVyPU[uOFU1OjNizszN M{G0e3NCVkeHUh?=
HCC1806 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTZwOEG5N|Eh|ryP MUTTRW5ITVJ?
BCPAP MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfYXohKSzVyPUeuNlE4PjRizszN Ml3TV2FPT0WU
LB2241-RCC MnnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTBU|VKSzVyPUeuN|Y6ODdizszN NX\wXYkzW0GQR1XS
COLO-741 NG\xU2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfpXoRSUUN3ME24MlAyPjd7IN88US=> NF3EZmJUSU6JRWK=
HSC-3 M2TpTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjLOXlKSzVyPUiuNFcxPjhizszN MX7TRW5ITVJ?
SW982 NULNdm9RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWG2Ulk2UUN3ME24MlQyPTF4IN88US=> MkjsV2FPT0WU
GCT M1HqTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\tTWM2OD16Lke1N|E1KM7:TR?= NIfkRmNUSU6JRWK=
KY821 MmHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\zbXBKSzVyPUmuNFUyPzhizszN NFvFbJBUSU6JRWK=
JVM-3 NIG0VXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTlwNU[5PVkh|ryP NYnyNI1zW0GQR1XS
RS4-11 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlK3TWM2OD17Lk[wOFgh|ryP NH3LU5VUSU6JRWK=
VA-ES-BJ NGrycWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPFTWM2OD1zMD6wNVQ6KM7:TR?= MXPTRW5ITVJ?
A431 M{DL[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLTNlBKSzVyPUGwMlQzOTJizszN NHXEeYZUSU6JRWK=
LXF-289 NXfRSFY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3X0VGlEPTB;MUCuOFU5KM7:TR?= MmXGV2FPT0WU
SK-MEL-24 NI[4VItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTFyLkiyO|Qh|ryP NGHnfJNUSU6JRWK=
NOS-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3EfY54UUN3ME2xNE45PDd{IN88US=> MUfTRW5ITVJ?
KNS-62 NFrUW5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnrTWM2OD1zMT6yOFA1KM7:TR?= M1\C[HNCVkeHUh?=
SK-HEP-1 M{DMT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTFzLkO1Nlch|ryP NFjjcnVUSU6JRWK=
A3-KAW NHvkPIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTPfJNKSzVyPUGxMlcyPzhizszN MlTXV2FPT0WU
SK-LU-1 MonLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHLdppKSzVyPUGyMlI3PTVizszN Ml76V2FPT0WU
TYK-nu MmjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTF{LkO5N|Ih|ryP MW\TRW5ITVJ?
NMC-G1 NFrHPHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\1TWM2OD1zMj62NFYzKM7:TR?= Ml3WV2FPT0WU
BB65-RCC NGfuepFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvjTWM2OD1zMj63NVY6KM7:TR?= Mnn0V2FPT0WU
QIMR-WIL MlzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLic4VpUUN3ME2xNk45QDN|IN88US=> NHPFOI1USU6JRWK=
D-566MG NUDDNIFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjm[HNtUUN3ME2xN{46PTd4IN88US=> M{C1T3NCVkeHUh?=
KYSE-140 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEj0SIxKSzVyPUG0MlA4PTNizszN NXTqeYhUW0GQR1XS
SCC-4 NHrxXJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jtd2lEPTB;MUSuN|M2QSEQvF2= NHHQ[XRUSU6JRWK=
U251 MmnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHPTYVUUUN3ME2xOE45PDl{IN88US=> M4DpWHNCVkeHUh?=
D-542MG NUPQTm55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTF2LkmyNlIh|ryP NWTKZVE2W0GQR1XS
LAMA-84 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPQbFVPUUN3ME2xOE46QTN{IN88US=> M4K1dnNCVkeHUh?=
NCI-H720 M2POdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\qW3ZCUUN3ME2xOU4zPjh2IN88US=> M3K5UXNCVkeHUh?=
DEL Ml\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfXZ3c6UUN3ME2xOU41Ojl|IN88US=> MVjTRW5ITVJ?
SBC-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTF3LkSzNFUh|ryP MV7TRW5ITVJ?
ECC10 NX6yOJZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7KNYdKSzVyPUG1MlQ1PThizszN Ml7mV2FPT0WU
Daoy NXLIfWw2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTF3Lke2NVYh|ryP Mkj6V2FPT0WU
SCH NFzaVFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fKV2lEPTB;MUWuO|g{PSEQvF2= MkHBV2FPT0WU
MZ2-MEL NF:5NoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrmTWM2OD1zNj6wOlQ3KM7:TR?= MV\TRW5ITVJ?
CAL-12T NVG4ZngxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;HdlVZUUN3ME2xOk41QDZ{IN88US=> Mm\vV2FPT0WU
KE-37 M37q[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfhVIZKSzVyPUG2MlgyODdizszN Ml\wV2FPT0WU
LS-411N NF:xN2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPuTWM2OD1zNz6xNVgh|ryP M4TTenNCVkeHUh?=
NCI-H2228 M33Nb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\RVGlEPTB;MUeuN|A4OSEQvF2= NUfh[4lGW0GQR1XS
SK-MEL-2 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13tZWlEPTB;MUeuOFk3PSEQvF2= MYDTRW5ITVJ?
HN NIHyTFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfZUplKSzVyPUG3MlczPDhizszN MoTVV2FPT0WU
NCI-H1648 NGKw[HhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTF5LkixPEDPxE1? MVrTRW5ITVJ?
IA-LM NG\HXG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzLO41KSzVyPUG4MlMyPzJizszN Mn;IV2FPT0WU
EW-13 NYnCeoFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfDWWNKSzVyPUG4MlU4ODhizszN Ml\UV2FPT0WU
YKG-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTF7LkW3NVEh|ryP Mn;rV2FPT0WU
KNS-81-FD M2[5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLuTWM2OD1zOT61PFU5KM7:TR?= NWDFR3Q5W0GQR1XS
23132-87 MkOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTF7Lke2OFIh|ryP MVjTRW5ITVJ?
NUGC-3 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfyR29wUUN3ME2xPU46QDh5IN88US=> MoXTV2FPT0WU
5637 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLVOJJKSzVyPUKwMlA1PzhizszN M4f5W3NCVkeHUh?=
NCI-H1755 NHLoZotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrRbIhKSzVyPUKwMlQ4PjRizszN NIrGfFdUSU6JRWK=
RH-18 NHzPeYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\Ec|RKSzVyPUKwMlU4PDhizszN M1\J[3NCVkeHUh?=
RXF393 MoPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnsZnlDUUN3ME2yNE43PzV4IN88US=> M2PjUHNCVkeHUh?=
LU-134-A NH\tTmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonvTWM2OD1{MD63NFU3KM7:TR?= NXfkVINFW0GQR1XS
TE-12 NIrnVFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moi3TWM2OD1{MD63NlAyKM7:TR?= MnzaV2FPT0WU
MOLT-4 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTJzLkG5NVUh|ryP NXfuN|JxW0GQR1XS
IGR-1 NXXVcol7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvHTWM2OD1{MT6zO|k3KM7:TR?= NVjTWpdiW0GQR1XS
HOP-92 NX\nS2JVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rBfGlEPTB;MkGuOFk5PyEQvF2= MVvTRW5ITVJ?
SK-MES-1 M1LqOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGC4NIJKSzVyPUKxMlc{QDFizszN M{PsNnNCVkeHUh?=
LU-65 NF73ZnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlO1TWM2OD1{MT64OlI1KM7:TR?= MYfTRW5ITVJ?
MS-1 M1T1Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[wfnJKSzVyPUKyMlEzODNizszN MUPTRW5ITVJ?
LoVo MoXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHmc2ZKSzVyPUKyMlI1PCEQvF2= MVnTRW5ITVJ?
A704 NInKPXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33rOWlEPTB;MkKuOVE2PSEQvF2= MljWV2FPT0WU
HT-1376 MljGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF73NHlKSzVyPUKyMlYxPTlizszN NFPseGRUSU6JRWK=
IST-MEL1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlr6TWM2OD1{Mj62O|UyKM7:TR?= NI\ZdZhUSU6JRWK=
Ramos-2G6-4C10 NUiyd3ZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LrO2lEPTB;MkKuO|M3PiEQvF2= MVHTRW5ITVJ?
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IST-SL1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;hPGlEPTB;MkWuNlc2OSEQvF2= MX3TRW5ITVJ?
HH NWjr[FgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTJ3LkOxPVIh|ryP MmH1V2FPT0WU
NCI-H82 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLMTWM2OD1{NT65N|gh|ryP NIfTZWxUSU6JRWK=
SNU-449 NFnmcXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4K0d2lEPTB;MkeuNlAyQCEQvF2= NX3jSZVbW0GQR1XS
COR-L23 M4\FU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjUOJBZUUN3ME2yO{4zQDF|IN88US=> NUT3R|A2W0GQR1XS
LOXIMVI MmXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\pd5JKSzVyPUK3MlM3QCEQvF2= NU[1TII6W0GQR1XS
GR-ST NVP3N2tuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmS4TWM2OD1{Nz62O|A3KM7:TR?= Mlj6V2FPT0WU
NCI-SNU-1 M{nBOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGf4PYRKSzVyPUK3Mlk1PCEQvF2= NUW4cJJrW0GQR1XS
ALL-PO M4fPemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTybFVsUUN3ME2yPE4yPjB2IN88US=> NXXCTHZWW0GQR1XS
ML-2 NF3vN|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlS2TWM2OD1{OD6yPFE1KM7:TR?= MYXTRW5ITVJ?
HOP-62 M37JVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTJ6LkexN{DPxE1? MVrTRW5ITVJ?
EGI-1 Mlj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTtfGZMUUN3ME2yPE45QDR3IN88US=> NYjySYZnW0GQR1XS
TCCSUP Mmq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfZbm5sUUN3ME2yPE46Ojd{IN88US=> MWHTRW5ITVJ?
LB996-RCC M4LBcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13tRWlEPTB;MkmuOVY5OiEQvF2= MVXTRW5ITVJ?
LCLC-97TM1 M1\0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTN{LkG5OlQh|ryP NInXUnlUSU6JRWK=
NCI-H1304 M2Xwdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\FVmlEPTB;M{KuN|MxOSEQvF2= M4fze3NCVkeHUh?=
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NCI-H1770 NGDDcWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4G3b2lEPTB;M{OuNVY1QCEQvF2= MVnTRW5ITVJ?
EM-2 MmTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTyVGVkUUN3ME2zN{43PTB2IN88US=> M3iwNHNCVkeHUh?=
ChaGo-K-1 NVXOeWhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnlW|BLUUN3ME2zN{44OjN4IN88US=> NFfuOHFUSU6JRWK=
ACHN M{PqU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTN|LkizPFUh|ryP MVXTRW5ITVJ?
MN-60 NUH3TYJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;STWM2OD1|Mz64OVQ1KM7:TR?= NGnISFNUSU6JRWK=
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KGN NW[4Z481T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTyTWM2OD1|NT63NlkzKM7:TR?= NYTMdFVNW0GQR1XS
U031 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\Gc2lEPTB;M{WuPFE{OiEQvF2= M4HyS3NCVkeHUh?=
HMV-II NGXEXFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDrUHpGUUN3ME2zOk4xPzd2IN88US=> NHywXnpUSU6JRWK=
L-363 NUHENFQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\6cXBZUUN3ME2zO{43PDV3IN88US=> M3K0b3NCVkeHUh?=
NCI-H1155 NFKxNGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XGPGlEPTB;M{iuNFAyPSEQvF2= NXHheGtnW0GQR1XS
NCI-H1793 NWruS21wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTN6LkGwNlYh|ryP MWHTRW5ITVJ?
P30-OHK NIn5NnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTN6LkGzN|Ih|ryP MnTSV2FPT0WU
AN3-CA NUDiOnVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzPTWM2OD1|OD6xOlE2KM7:TR?= MVrTRW5ITVJ?
UACC-257 NH3KVFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\aT5U6UUN3ME2zPE44QSEQvF2= NGPxPIpUSU6JRWK=
MCF7 NH64SWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjvNXVKSzVyPUO5Mlg3OjlizszN NVLWXppMW0GQR1XS
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NCI-H1092 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTR|LkK4PVUh|ryP MkPUV2FPT0WU
KARPAS-299 NFPleodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\nRXdKSzVyPUSzMlMxPzFizszN M2DxTXNCVkeHUh?=
LB1047-RCC M2T5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGKwXnZKSzVyPUS0Mlk6PTlizszN MkL4V2FPT0WU
786-0 M4\2S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHyTWM2OD12NT62OUDPxE1? MWPTRW5ITVJ?
HCC2157 NYPqN2dHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHEcZpKSzVyPUS2MlA{PTlizszN M4XqWXNCVkeHUh?=
NY NX3aNHpiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPtc2pNUUN3ME20Ok4yPzd6IN88US=> MXnTRW5ITVJ?
EFM-19 NUG2XGZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DB[WlEPTB;NE[uO|U{OyEQvF2= NEfuW4JUSU6JRWK=
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UM-UC-3 NXHreYJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjvTWM2OD12Nj64NFU6KM7:TR?= MnrkV2FPT0WU
HT-29 M4\5b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4SyUmlEPTB;NEeuPFc6OiEQvF2= NU\CdXN4W0GQR1XS
LN-405 MmrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\IWY5ZUUN3ME20PE4xQDJ5IN88US=> NWnvUlNxW0GQR1XS
NCI-H727 Mkj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjTdFFPUUN3ME20PE44PzJ4IN88US=> NEfKWXNUSU6JRWK=
D-502MG Moi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPTSHhKSzVyPUS4Mlk3PzZizszN MnnMV2FPT0WU
GMS-10 NH\jZVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jPW2lEPTB;NEmuNlk4PCEQvF2= NIjue2NUSU6JRWK=
MEL-JUSO NILjU2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vYV2lEPTB;NEmuN|Q4KM7:TR?= MnvEV2FPT0WU

... 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 Na+0.5% Tween 80 30mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 N-(3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide

文献中の引用 (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)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

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他の質問がある場合は、お気軽くお問合せください。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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