PLX-4720 化学構造
分子量: 413.83

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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 NIDwcHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlX6TWM2OD1yLkC3OFU4KM7:TR?= M2nGW3NCVkeHUh?=
EoL-1-cell Mk\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTBwMUSxOlYh|ryP NGTZdIdUSU6JRWK=
C32 MnKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3ziW2lEPTB;MD6xOVE{OSEQvF2= MkDGV2FPT0WU
M14 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwMkG3OVch|ryP Mn;PV2FPT0WU
CP50-MEL-B MnzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4P1R2lEPTB;MD6yPVc5PCEQvF2= MnWxV2FPT0WU
A101D NVTJcHM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LpXGlEPTB;MD6zNlU5QSEQvF2= MoXqV2FPT0WU
G-361 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PKUmlEPTB;MD6zOFY{PyEQvF2= NXqxXmJSW0GQR1XS
HT-144 M4rLRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTBwM{[zNlkh|ryP MVjTRW5ITVJ?
ACN MonXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTBwM{i0O|ch|ryP MYTTRW5ITVJ?
COLO-829 NFLib4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTBwM{i5Olgh|ryP M2r5WXNCVkeHUh?=
MEL-HO MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fpOmlEPTB;MD60NVE4QSEQvF2= MlzLV2FPT0WU
SH-4 NFrrZXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHX6WVVKSzVyPUCuOFE1OjJizszN NWXT[ohkW0GQR1XS
SK-MEL-3 NXvDN4RCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXU[XZSUUN3ME2wMlUyPTZ6IN88US=> NYqwWIRGW0GQR1XS
A375 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTBwNkezOVkh|ryP MVjTRW5ITVJ?
MMAC-SF NV24eZZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2e5dGlEPTB;MD62PFYyPCEQvF2= M3GyU3NCVkeHUh?=
BHT-101 M3HYTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIS5SGZKSzVyPUCuO|A4ODJizszN M2jtb3NCVkeHUh?=
K5 NV33VXF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXBe|dKSzVyPUCuO|YyPDhizszN NU\IbYQxW0GQR1XS
BV-173 MoDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTMcpVKSzVyPUCuO|k3PDRizszN MXPTRW5ITVJ?
RVH-421 MmHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\BcmlEPTB;MD64Olc6PiEQvF2= NV\2cXJ4W0GQR1XS
HCC2218 NVrOcnBIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3nTWM2OD1yLki3PFQ1KM7:TR?= Mm\BV2FPT0WU
WM-115 MlrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjNcVE2UUN3ME2wMlg5Pjl{IN88US=> NF\LTIhUSU6JRWK=
SK-MEL-28 NX;BU|Z7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTFwMES1Olkh|ryP NXzWRoVjW0GQR1XS
COLO-679 MljkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWe0Z3V2UUN3ME2xMlExPDZ2IN88US=> NWLWXG14W0GQR1XS
MZ7-mel NV3scIV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPIO3lKSzVyPUGuNVQ6PjNizszN NFfUTWpUSU6JRWK=
SK-MEL-30 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrvTWM2OD1zLkOzN|g3KM7:TR?= NXLiOIZ3W0GQR1XS
NCI-H209 Mmi4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTFwNkC4OkDPxE1? NFvrNIpUSU6JRWK=
HTC-C3 NXrCVnVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTFwNk[yPVQh|ryP NUPLR|k5W0GQR1XS
KARPAS-45 NX7CV25FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPBepRKSzVyPUKuNFQ6PzhizszN MV\TRW5ITVJ?
NCI-SNU-5 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDVdmlKSzVyPUKuNVE6PjlizszN NXzjOm91W0GQR1XS
KP-4 MofkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnJfoxWUUN3ME2yMlMxPzh5IN88US=> M{\NS3NCVkeHUh?=
PA-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7rOGQ4UUN3ME2yMlczPjd|IN88US=> M1iyTnNCVkeHUh?=
HuO-3N1 MkHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXncnNiUUN3ME2yMlg4QTR4IN88US=> MVfTRW5ITVJ?
NCI-H358 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWm5[FlMUUN3ME2yMlkzOjN{IN88US=> NHzxWlNUSU6JRWK=
CTB-1 NXy4UIt3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfZWZRKSzVyPUOuOFAyPzZizszN Mn\VV2FPT0WU
697 Mn;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfKTWM2OD1|LkW1NlY3KM7:TR?= Mlv2V2FPT0WU
CP66-MEL NETSWIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTRwMUW5Nlch|ryP NU\aZ2NGW0GQR1XS
NB13 NVi0Z4JLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjSRm9KSzVyPUSuOFkyPzlizszN NXT5Oph5W0GQR1XS
DBTRG-05MG MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;D[JFKSzVyPUSuOVM{OjVizszN MnzhV2FPT0WU
A2058 NV\nNWszT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3MV|dKSzVyPUSuO|IyPjRizszN MkHSV2FPT0WU
KG-1 NHHPdFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTRwN{O5NFgh|ryP MXXTRW5ITVJ?
8305C M3vpcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jVXmlEPTB;NT6xPFc{KM7:TR?= NFrw[21USU6JRWK=
RPMI-7951 NILn[ItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLOTWM2OD13LkiwNlg{KM7:TR?= NGrhU5FUSU6JRWK=
CHL-1 NVnOboxvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWr6UHI5UUN3ME21Mlk4PjB|IN88US=> MYrTRW5ITVJ?
TI-73 NWrQUlM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofuTWM2OD14LkCwPVAzKM7:TR?= MVTTRW5ITVJ?
HT-1080 Mk\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfucWNQUUN3ME22MlExQTR4IN88US=> MWTTRW5ITVJ?
ES5 NEPKZXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjKbYxKSzVyPU[uNVQ6OjRizszN M3WxOHNCVkeHUh?=
8-MG-BA M1zq[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFToNFNKSzVyPU[uNVgyOjlizszN NX7r[|J4W0GQR1XS
NB7 M3S0PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLLTWM2OD14LkKxN|c{KM7:TR?= MV7TRW5ITVJ?
H4 MlnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHKwV4ZKSzVyPU[uNlI1QTNizszN M17kbHNCVkeHUh?=
CAL-72 M3fIdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXizSXplUUN3ME22MlQ2PDJ|IN88US=> M{XGRnNCVkeHUh?=
HCC1806 MnnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDJTWM2OD14LkixPVMyKM7:TR?= NFjBNZdUSU6JRWK=
BCPAP NUTkO|V[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGmxdpVKSzVyPUeuNlE4PjRizszN NFfHXZBUSU6JRWK=
LB2241-RCC NXXGTY9iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jNR2lEPTB;Nz6zOlkxPyEQvF2= NXm0d2NSW0GQR1XS
COLO-741 NF[xOlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEm2OmRKSzVyPUiuNFE3PzlizszN NUiz[5NMW0GQR1XS
HSC-3 MlrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nNXWlEPTB;OD6wO|A3QCEQvF2= Mn3oV2FPT0WU
SW982 M3H2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvKTWM2OD16LkSxOVE3KM7:TR?= NFjTN5VUSU6JRWK=
GCT M2qyb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3KzdmlEPTB;OD63OVMyPCEQvF2= MknLV2FPT0WU
KY821 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoSwTWM2OD17LkC1NVc5KM7:TR?= NIHOfohUSU6JRWK=
JVM-3 MkLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\CVllKSzVyPUmuOVY6QTlizszN MlzBV2FPT0WU
RS4-11 NV;Ie3c3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjJOmlYUUN3ME25MlYxPDhizszN M4DER3NCVkeHUh?=
VA-ES-BJ NYP5[m0xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTFyLkCxOFkh|ryP M4LwU3NCVkeHUh?=
A431 MlHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTFyLkSyNVIh|ryP NH;v[mhUSU6JRWK=
LXF-289 NU\Pfnp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjYU5lKSzVyPUGwMlQ2QCEQvF2= NYKyNY0yW0GQR1XS
SK-MEL-24 MnLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXOVId{UUN3ME2xNE45Ojd2IN88US=> NITSWXRUSU6JRWK=
NOS-1 NVvIfWpFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDqTWM2OD1zMD64OFczKM7:TR?= NVTuV5U2W0GQR1XS
KNS-62 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTFzLkK0NFQh|ryP MnrhV2FPT0WU
SK-HEP-1 Mn\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljKTWM2OD1zMT6zOVI4KM7:TR?= NWW4PIxVW0GQR1XS
A3-KAW NHHMeVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTFzLkexO|gh|ryP M{\Md3NCVkeHUh?=
SK-LU-1 NEXnbFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\JN3FKSzVyPUGyMlI3PTVizszN M4TycnNCVkeHUh?=
TYK-nu NWHs[Jo2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTF{LkO5N|Ih|ryP NVjZdoZMW0GQR1XS
NMC-G1 NXXDUlFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTF{Lk[wOlIh|ryP MWnTRW5ITVJ?
BB65-RCC M1TGVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{n1ZWlEPTB;MUKuO|E3QSEQvF2= M2KzdHNCVkeHUh?=
QIMR-WIL Mom1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDsOHNiUUN3ME2xNk45QDN|IN88US=> MnW5V2FPT0WU
D-566MG NH\GRXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFz3eodKSzVyPUGzMlk2PzZizszN MXrTRW5ITVJ?
KYSE-140 NIPYbpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2m0b2lEPTB;MUSuNFc2OyEQvF2= M1jxSHNCVkeHUh?=
SCC-4 M3PUNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojBTWM2OD1zND6zN|U6KM7:TR?= NF\abWtUSU6JRWK=
U251 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rkb2lEPTB;MUSuPFQ6OiEQvF2= NHXsW5ZUSU6JRWK=
D-542MG MkH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHzWpR1UUN3ME2xOE46OjJ{IN88US=> MlT2V2FPT0WU
LAMA-84 NW\oeIJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2mzNGlEPTB;MUSuPVk{OiEQvF2= MUHTRW5ITVJ?
NCI-H720 M4XyVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTF3LkK2PFQh|ryP MUPTRW5ITVJ?
DEL M3nkTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLTSopxUUN3ME2xOU41Ojl|IN88US=> MYjTRW5ITVJ?
SBC-1 MkLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XP[mlEPTB;MUWuOFMxPSEQvF2= M2\yNHNCVkeHUh?=
ECC10 NHvyWmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjKU|hiUUN3ME2xOU41PDV6IN88US=> MoLvV2FPT0WU
Daoy NGTj[pdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDhTWM2OD1zNT63OlE3KM7:TR?= NWq1PFdFW0GQR1XS
SCH MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTF3Lke4N|Uh|ryP MlHUV2FPT0WU
MZ2-MEL MnHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTGTWM2OD1zNj6wOlQ3KM7:TR?= NUnWUHMyW0GQR1XS
CAL-12T NVXY[2Y2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moj6TWM2OD1zNj60PFYzKM7:TR?= MWjTRW5ITVJ?
KE-37 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnyxTWM2OD1zNj64NVA4KM7:TR?= MluzV2FPT0WU
LS-411N NFfUOoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XaUmlEPTB;MUeuNVE5KM7:TR?= NHuyXFlUSU6JRWK=
NCI-H2228 NH[2c2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjocHBKSzVyPUG3MlMxPzFizszN NYDw[ZQyW0GQR1XS
SK-MEL-2 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\xTWM2OD1zNz60PVY2KM7:TR?= NGDqbINUSU6JRWK=
HN NGT0T5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3iwVGlEPTB;MUeuO|I1QCEQvF2= MmC3V2FPT0WU
NCI-H1648 M3fuNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jXb2lEPTB;MUeuPFE5KM7:TR?= MmKwV2FPT0WU
IA-LM NGjIVJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnRRo1KSzVyPUG4MlMyPzJizszN NV\2W2JWW0GQR1XS
EW-13 M1m2fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTF6LkW3NFgh|ryP NIHjOmdUSU6JRWK=
YKG-1 M2Llb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvsSnRWUUN3ME2xPU42PzFzIN88US=> MYjTRW5ITVJ?
KNS-81-FD M1jH[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml35TWM2OD1zOT61PFU5KM7:TR?= MmnJV2FPT0WU
23132-87 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHzXHlKSzVyPUG5Mlc3PDJizszN M1q5PXNCVkeHUh?=
NUGC-3 NX3jdWh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTF7Lkm4PFch|ryP M4HlcHNCVkeHUh?=
5637 NXqzcG9ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfkPFZKSzVyPUKwMlA1PzhizszN NWWx[I9lW0GQR1XS
NCI-H1755 M2HmXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fMWGlEPTB;MkCuOFc3PCEQvF2= M1LWU3NCVkeHUh?=
RH-18 MnPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTJyLkW3OFgh|ryP NHTZb4ZUSU6JRWK=
RXF393 M4q3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXpRlhFUUN3ME2yNE43PzV4IN88US=> NVnMWVN2W0GQR1XS
LU-134-A MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTyblB5UUN3ME2yNE44ODV4IN88US=> NXvvOYJJW0GQR1XS
TE-12 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4G4eWlEPTB;MkCuO|IxOSEQvF2= NEfGTlRUSU6JRWK=
MOLT-4 M{\XdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTJzLkG5NVUh|ryP MUDTRW5ITVJ?
IGR-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELIWXZKSzVyPUKxMlM4QTZizszN NIHp[JBUSU6JRWK=
HOP-92 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2L2PGlEPTB;MkGuOFk5PyEQvF2= NUnV[mJnW0GQR1XS
SK-MES-1 M2nGR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfQTWM2OD1{MT63N|gyKM7:TR?= MXnTRW5ITVJ?
LU-65 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTJzLki2NlQh|ryP NXXUOoJ{W0GQR1XS
MS-1 MonRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;DSm9tUUN3ME2yNk4yOjB|IN88US=> NUjic5NOW0GQR1XS
LoVo M1TBdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fKXGlEPTB;MkKuNlQ1KM7:TR?= M{OzU3NCVkeHUh?=
A704 NH6xOodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4f1WmlEPTB;MkKuOVE2PSEQvF2= M{DONHNCVkeHUh?=
HT-1376 M3Pmb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjPRVIzUUN3ME2yNk43ODV7IN88US=> NFfDN|RUSU6JRWK=
IST-MEL1 NWL2VWlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHYTWM2OD1{Mj62O|UyKM7:TR?= MX3TRW5ITVJ?
Ramos-2G6-4C10 MnXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknOTWM2OD1{Mj63N|Y3KM7:TR?= MWjTRW5ITVJ?
T47D M{nyRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13peGlEPTB;MkKuO|k4QSEQvF2= NGnETmlUSU6JRWK=
HT-1197 NUDVSmlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTJ|LkC4NVch|ryP Mlz4V2FPT0WU
LB2518-MEL NF2yWlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnP6TWM2OD1{Mz62OFEzKM7:TR?= M2\xd3NCVkeHUh?=
J-RT3-T3-5 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTJ2Lke1PVUh|ryP MlrnV2FPT0WU
SK-NEP-1 NX7BTVRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\EZmlEPTB;MkSuPFc1PCEQvF2= M4e2VXNCVkeHUh?=
NCI-H526 NEfyW5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DKfWlEPTB;MkWuNFAzOyEQvF2= MoSxV2FPT0WU
IST-SL1 NVjkd4ZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;XU3UzUUN3ME2yOU4zPzVzIN88US=> NUnaNXVoW0GQR1XS
HH NV:5TnBsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7GRYtOUUN3ME2yOU4{OTl{IN88US=> NGXa[oZUSU6JRWK=
NCI-H82 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPBcGt{UUN3ME2yOU46OzhizszN NFHxdVBUSU6JRWK=
SNU-449 M2rwPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;2XGlEPTB;MkeuNlAyQCEQvF2= MYHTRW5ITVJ?
COR-L23 Ml7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIf6c|RKSzVyPUK3MlI5OTNizszN M1jlZnNCVkeHUh?=
LOXIMVI MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\wOXZXUUN3ME2yO{4{PjhizszN Ml\lV2FPT0WU
GR-ST NFXqfmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rxZWlEPTB;MkeuOlcxPiEQvF2= M1mwVHNCVkeHUh?=
NCI-SNU-1 NXXk[5JZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2joN2lEPTB;MkeuPVQ1KM7:TR?= NFL0VlBUSU6JRWK=
ALL-PO Mn\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfxTWM2OD1{OD6xOlA1KM7:TR?= MoPGV2FPT0WU
ML-2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjSfohqUUN3ME2yPE4zQDF2IN88US=> NXXlbnZzW0GQR1XS
HOP-62 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTJ6LkexN{DPxE1? NVixSJREW0GQR1XS
EGI-1 NVvSdZV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUC3OY1ZUUN3ME2yPE45QDR3IN88US=> MV\TRW5ITVJ?
TCCSUP M4XueWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfaTWM2OD1{OD65NlczKM7:TR?= NWLJdWFDW0GQR1XS
LB996-RCC M1\FSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTJ7LkW2PFIh|ryP MlrRV2FPT0WU
LCLC-97TM1 NHfRR4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXkRolKSzVyPUOyMlE6PjRizszN MnfpV2FPT0WU
NCI-H1304 NH6zfmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGflbVlKSzVyPUOyMlM{ODFizszN M1z5W3NCVkeHUh?=
KP-N-YS MnHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XHTmlEPTB;M{KuOVk4OyEQvF2= M{GzRnNCVkeHUh?=
NCI-H1770 M1fmXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vVS2lEPTB;M{OuNVY1QCEQvF2= M4G3WnNCVkeHUh?=
EM-2 NFXkWIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUG5WFlGUUN3ME2zN{43PTB2IN88US=> NG\RW|BUSU6JRWK=
ChaGo-K-1 M{Hpb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nv[2lEPTB;M{OuO|I{PiEQvF2= NIfsUFhUSU6JRWK=
ACHN NXnUdm5OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTN|LkizPFUh|ryP Ml:wV2FPT0WU
MN-60 NVvvOYxHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;YeWlEPTB;M{OuPFU1PCEQvF2= NEW3TplUSU6JRWK=
EW-18 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvOTWM2OD1|Mz64PVcyKM7:TR?= NH;3NoZUSU6JRWK=
KGN NGfNd|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\LTWM2OD1|NT63NlkzKM7:TR?= MoHmV2FPT0WU
U031 NXvZTFNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjUW3duUUN3ME2zOU45OTN{IN88US=> NUn6cXBWW0GQR1XS
HMV-II NIDJRnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTN4LkC3O|Qh|ryP MoS3V2FPT0WU
L-363 MmDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWryZok5UUN3ME2zO{43PDV3IN88US=> NYfTVpdtW0GQR1XS
NCI-H1155 NVvnRY4yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXmXZJKSzVyPUO4MlAxOTVizszN M1rveXNCVkeHUh?=
NCI-H1793 NW\U[3VtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfTd|R5UUN3ME2zPE4yODJ4IN88US=> MljOV2FPT0WU
P30-OHK MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTN6LkGzN|Ih|ryP MkLkV2FPT0WU
AN3-CA NH3GRmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4i0dmlEPTB;M{iuNVYyPSEQvF2= NWDLNGlqW0GQR1XS
UACC-257 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk[4TWM2OD1|OD63PUDPxE1? MUPTRW5ITVJ?
MCF7 NGL4[Y5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvlVIRNUUN3ME2zPU45PjJ7IN88US=> NWHTV4xDW0GQR1XS
KP-N-YN MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3MXGZKSzVyPUSwMlQzQDVizszN NF;rO4tUSU6JRWK=
T98G NG[4Z3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTRyLkS5OVch|ryP MVHTRW5ITVJ?
HGC-27 Mm\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzJTWM2OD12Mz6yO|Qh|ryP NIPGbm5USU6JRWK=
NCI-H1092 NFLabZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTR|LkK4PVUh|ryP NILSVI9USU6JRWK=
KARPAS-299 M2n5RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTR|LkOwO|Eh|ryP Mk\iV2FPT0WU
LB1047-RCC MkCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLrfJhDUUN3ME20OE46QTV7IN88US=> NWXFV|NPW0GQR1XS
786-0 MlL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnKfY1MUUN3ME20OU43PSEQvF2= NVvXV4xSW0GQR1XS
HCC2157 NVS0TJNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTR4LkCzOVkh|ryP NFfiTWNUSU6JRWK=
NY MlTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTR4LkG3O|gh|ryP MYHTRW5ITVJ?
EFM-19 MofCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTR4Lke1N|Mh|ryP M373O3NCVkeHUh?=
EW-16 MkizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXv0b3pPUUN3ME20Ok44QDB4IN88US=> MonwV2FPT0WU
UM-UC-3 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvsTWpKSzVyPUS2MlgxPTlizszN MojzV2FPT0WU
HT-29 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFi5U2FKSzVyPUS3Mlg4QTJizszN MVPTRW5ITVJ?
LN-405 M2q5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTKem9KSzVyPUS4MlA5OjdizszN NVzGRoFEW0GQR1XS
NCI-H727 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfzZoVKSzVyPUS4Mlc4OjZizszN M2rITnNCVkeHUh?=
D-502MG NE[3[WlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTR6Lkm2O|Yh|ryP NFfUSWxUSU6JRWK=
GMS-10 NHrVdmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rGSGlEPTB;NEmuNlk4PCEQvF2= M3zhb3NCVkeHUh?=
MEL-JUSO NGrGR4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\v[WN6UUN3ME20PU4{PDdizszN NHHh[YlUSU6JRWK=

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 83 mg/mL (200.56 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+50% PEG 300+5% Tween 80+ddH2O 5mg/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 (45)

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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