PLX-4720

Catalog No.S1152

For research use only.

PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.

PLX-4720 Chemical Structure

CAS No. 918505-84-7

Selleck's PLX-4720 has been cited by 167 publications

Purity & Quality Control

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Biological Activity

Description PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.
Targets
C-Raf-1 (Y340D/Y341D) [1]
(Cell-free assay)
B-Raf (V600E) [1]
(Cell-free assay)
BRK [1]
(Cell-free assay)
B-Raf [1]
(Cell-free assay)
6.7 nM 13 nM 130 nM 160 nM
In vitro

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DU-4475 M2fNPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoCwTWM2OD1yLkC3OFU4KM7:TR?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
EoL-1-cell NIPGXWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofFTWM2OD1yLkG0NVY3KM7:TR?= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
C32 NF3kXXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;PTWM2OD1yLkG1NVMyKM7:TR?= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
M14 NGjKWFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvlOVZ3UUN3ME2wMlIyPzV5IN88US=> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
CP50-MEL-B MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwMkm3PFQh|ryP MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
A101D M{WyXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTBwM{K1PFkh|ryP M2nXPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
G-361 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfLT45KSzVyPUCuN|Q3OzdizszN MoO1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
HT-144 M1jkdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTBwM{[zNlkh|ryP NYfSTGF{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
ACN NYnrPYVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTBwM{i0O|ch|ryP MmWzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
COLO-829 MoTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HiTmlEPTB;MD6zPFk3QCEQvF2= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
MEL-HO MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LoZmlEPTB;MD60NVE4QSEQvF2= MkP4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
SH-4 MnzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV25TY9OUUN3ME2wMlQyPDJ{IN88US=> M3LT[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
SK-MEL-3 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3K0bmlEPTB;MD61NVU3QCEQvF2= NXyxU2ZWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
A375 NF3FeldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTBwNkezOVkh|ryP MkPLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
MMAC-SF MnvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLaTWM2OD1yLk[4OlE1KM7:TR?= NHTEUo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
BHT-101 NV;3PWFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTBwN{C3NFIh|ryP MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
K5 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjVTHQ1UUN3ME2wMlc3OTR6IN88US=> NX73NGhORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
BV-173 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjFTWM2OD1yLke5OlQ1KM7:TR?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
RVH-421 M2Dpfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jRcWlEPTB;MD64Olc6PiEQvF2= NV;CbmdjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
HCC2218 Mnz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTBwOEe4OFQh|ryP NG\lTZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
WM-115 MmDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXThR|BIUUN3ME2wMlg5Pjl{IN88US=> NXWyWXBCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
SK-MEL-28 Mkm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPh[ZlnUUN3ME2xMlA1PTZ7IN88US=> MoHoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
COLO-679 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUf1Z2Z6UUN3ME2xMlExPDZ2IN88US=> M{m5elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
MZ7-mel M{jGb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Hae2lEPTB;MT6xOFk3OyEQvF2= M1\qUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
SK-MEL-30 M3GzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTFwM{OzPFYh|ryP MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
NCI-H209 Ml31S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrncpBxUUN3ME2xMlYxQDZizszN NV7oSFZyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
HTC-C3 NX\xTnJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHtfphKSzVyPUGuOlYzQTRizszN NGLy[Hk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
KARPAS-45 Mo\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mny4TWM2OD1{LkC0PVc5KM7:TR?= NEnNXpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
NCI-SNU-5 M4\EPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLpSJhKSzVyPUKuNVE6PjlizszN NVPUVmFjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
KP-4 NUDSSYpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjCU2pKSzVyPUKuN|A4QDdizszN MlnWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
PA-1 NV3sSnJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHWT4pKSzVyPUKuO|I3PzNizszN MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
HuO-3N1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HYbWlEPTB;Mj64O|k1PiEQvF2= MkfNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
NCI-H358 M4DzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTJwOUKyN|Ih|ryP M3zVSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
CTB-1 MmPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPWTWM2OD1|LkSwNVc3KM7:TR?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
697 MmPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDrTWM2OD1|LkW1NlY3KM7:TR?= MnjVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
CP66-MEL MoPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTRwMUW5Nlch|ryP MlTvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
NB13 NW\JbIJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3WTWM2OD12LkS5NVc6KM7:TR?= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
DBTRG-05MG NFnaWVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjqTWM2OD12LkWzN|I2KM7:TR?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
A2058 NH:xW|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvDeHNXUUN3ME20MlczOTZ2IN88US=> NHLqRmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
KG-1 NX7NXm1kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFz2elRKSzVyPUSuO|M6ODhizszN NXvuPZAyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
8305C MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrlcJlKSzVyPUWuNVg4OyEQvF2= Mo\UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
RPMI-7951 MlLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXYTWM2OD13LkiwNlg{KM7:TR?= NWTPSWpTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
CHL-1 MmD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTVwOUe2NFMh|ryP MmPrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
TI-73 NVvScFBvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTZwMEC5NFIh|ryP M1PBdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
HT-1080 NFjzUJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTZwMUC5OFYh|ryP M1LmPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
ES5 NIjYPWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVWyfYY3UUN3ME22MlE1QTJ2IN88US=> NHnqWWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
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NB1643 MnTQdWhVWyCjc4PhfS=> NUTmUY9neUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> M1fUd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 M{PVVpFJXFNiYYPzZZk> Mn\LdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= M1HtUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 NF;yV2tyUFSVIHHzd4F6 MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= M4nxNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC Mkm4dWhVWyCjc4PhfS=> MoTmdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Assay
Methods Test Index PMID
Western blot p-MEK / MEK / p-ERK / ERK / p-FAK(S910) ; p-EGFR 1173 / EGFR / p-Akt / Akt ; p27 / Cyclin D1 / pRb ; pAkt(Ser473) / pAkt(Thr308) 23076151 26023796 21828154
Immunofluorescence LAMP1 ; ZKSCAN3 / TFEB 30979895
Growth inhibition assay Cell viability 27848137
ELISA mIFN-γ 23204132
In vivo 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]

Protocol (from reference)

Kinase Assay:[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.

Cell Research:[1]
  • Cell lines: COLO205, A375, WM2664, COLO829, HT716, SW620, H460, Calu-6, HCT116, SK-MEL2, SK-MEL3, Lovo, H1299, 1205Lu, and C8161 cells
  • Concentrations: Dissolved in DMSO, final concentrations ~1 mM
  • Incubation Time: 24, 48, and 72 hours
  • Method: 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.
Animal Research:[1]
  • Animal Models: Female athymic mice (NCr nu/nu) implanted s.c. with COLO205 cells, and SCID mice with 1205Lu or C8161 cells
  • Dosages: 5, 20, or 100 mg/kg
  • Administration: Oral gavage once or twice daily

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+50% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 413.83
Formula

C17H14ClF2N3O3S

CAS No. 918505-84-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=C2C=C(C=N3)Cl)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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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.

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