PLX-4720

For research use only.

Catalog No.S1152

159 publications

PLX-4720 Chemical Structure

CAS No. 918505-84-7

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.

Selleck's PLX-4720 has been cited by 159 publications

Purity & Quality Control

Choose Selective Raf Inhibitors

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 NF:yNVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\KVWRjUUN3ME2wMlA4PDV5IN88US=> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
EoL-1-cell MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1r5NGlEPTB;MD6xOFE3PiEQvF2= NED5SlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
C32 MnTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTBwMUWxN|Eh|ryP NILiXXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
M14 M1\6fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTBwMkG3OVch|ryP MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
CP50-MEL-B NVfKdnhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwMkm3PFQh|ryP NG\kN2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
A101D MnLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTBwM{K1PFkh|ryP Mk\QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
G-361 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLyWHV2UUN3ME2wMlM1PjN5IN88US=> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
HT-144 NYrOWmVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTBwM{[zNlkh|ryP MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
ACN NHHvSXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\QWlI1UUN3ME2wMlM5PDd5IN88US=> NGDFXG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
COLO-829 M3zHV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rIZWlEPTB;MD6zPFk3QCEQvF2= NUWxZVVjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
MEL-HO MkO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDk[Yp{UUN3ME2wMlQyOTd7IN88US=> NFzlOpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
SH-4 NIHBTGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoGyTWM2OD1yLkSxOFIzKM7:TR?= MmfCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
SK-MEL-3 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[wS2pKSzVyPUCuOVE2PjhizszN MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
A375 MnPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;uUmxsUUN3ME2wMlY4OzV7IN88US=> NHG4c4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
MMAC-SF NYPiR45mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTBwNki2NVQh|ryP MlPnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
BHT-101 M3;6Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHneIRDUUN3ME2wMlcxPzB{IN88US=> NIW0cVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
K5 MnrES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2G4OmlEPTB;MD63OlE1QCEQvF2= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
BV-173 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTqOoFKSzVyPUCuO|k3PDRizszN M2HXS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
RVH-421 NGj5NZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXL1eXFMUUN3ME2wMlg3Pzl4IN88US=> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
HCC2218 NYixUlByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLle3RKSzVyPUCuPFc5PDRizszN NVPIU49PRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
WM-115 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;VTWM2OD1yLki4OlkzKM7:TR?= MmjwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
SK-MEL-28 NH7oT4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzPe|NKSzVyPUGuNFQ2PjlizszN MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
COLO-679 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTFwMUC0OlQh|ryP M4nxcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
MZ7-mel MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTFwMUS5OlMh|ryP Ml7EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
SK-MEL-30 NETFRYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPGTWM2OD1zLkOzN|g3KM7:TR?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
NCI-H209 MnGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUX4SlBrUUN3ME2xMlYxQDZizszN MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
HTC-C3 NV\uSIpCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jPfGlEPTB;MT62OlI6PCEQvF2= NHHjdpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
KARPAS-45 M4jEcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\XfmVKSzVyPUKuNFQ6PzhizszN Ml:3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
NCI-SNU-5 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPtSW5KSzVyPUKuNVE6PjlizszN MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
KP-4 NWnDR4F1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;ZXmlEPTB;Mj6zNFc5PyEQvF2= MnPiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
PA-1 M{C2dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTJwN{K2O|Mh|ryP NIDtW|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
HuO-3N1 NIfnb5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjsTWM2OD1{Lki3PVQ3KM7:TR?= NX;YOlhiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
NCI-H358 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXofVNGUUN3ME2yMlkzOjN{IN88US=> NYLGR|NTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
CTB-1 MlvoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nNOmlEPTB;Mz60NFE4PiEQvF2= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
697 M3jNTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorlTWM2OD1|LkW1NlY3KM7:TR?= NFLGdWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
CP66-MEL NWH3[3ZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTRwMUW5Nlch|ryP NHy1fY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
NB13 Mnr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDsXJRKSzVyPUSuOFkyPzlizszN Mme2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
DBTRG-05MG MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTRwNUOzNlUh|ryP MlHDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
A2058 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4WycGlEPTB;ND63NlE3PCEQvF2= NI\LbJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
KG-1 M1\4bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LBZ2lEPTB;ND63N|kxQCEQvF2= Mkn6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
8305C M4PJV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;NTWM2OD13LkG4O|Mh|ryP NVT1TnFtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
RPMI-7951 NGHESpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDMUmt7UUN3ME21MlgxOjh|IN88US=> Ml7ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
CHL-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvSUWZDUUN3ME21Mlk4PjB|IN88US=> MoDwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
TI-73 M4KwfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk[wTWM2OD14LkCwPVAzKM7:TR?= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
HT-1080 NF3ndG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPWWmNCUUN3ME22MlExQTR4IN88US=> NXS2W4t5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
ES5 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PCcmlEPTB;Nj6xOFkzPCEQvF2= MkSzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
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CAL-72 M{PJd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHS[WhKSzVyPU[uOFU1OjNizszN MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
HCC1806 NGm5dHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTZwOEG5N|Eh|ryP MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
BCPAP MoTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTdwMkG3OlQh|ryP Mon1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
LB2241-RCC M2TWXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTdwM{[5NFch|ryP MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
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HSC-3 MonTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRThwMEewOlgh|ryP MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
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GCT M3jOU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDjN2dKSzVyPUiuO|U{OTRizszN M3jQZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
KY821 MlLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\jTWM2OD17LkC1NVc5KM7:TR?= NFPwXYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
JVM-3 MmTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXlTWM2OD17LkW2PVk6KM7:TR?= NFTJeFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
RS4-11 NXn2elNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTUOndKSzVyPUmuOlA1QCEQvF2= M3v2SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
VA-ES-BJ NHvmZ3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\ye2lEPTB;MUCuNFE1QSEQvF2= M4[5O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
A431 M1ThWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PTcGlEPTB;MUCuOFIyOiEQvF2= M4HPXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
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SK-MEL-24 M{TyS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTFyLkiyO|Qh|ryP MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
NOS-1 M4TLXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTFyLki0O|Ih|ryP MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
KNS-62 M1zUXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe2R2hKSzVyPUGxMlI1ODRizszN M2j3PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
SK-HEP-1 NWnj[JRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWO1W3lMUUN3ME2xNU4{PTJ5IN88US=> MoTNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
A3-KAW NXH0b2UyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvCTWM2OD1zMT63NVc5KM7:TR?= MorUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
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TYK-nu MlftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTF{LkO5N|Ih|ryP MojxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
NMC-G1 MkL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXG[Y1KSzVyPUGyMlYxPjJizszN NWXnU5RnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
BB65-RCC NWT3[nAxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLPNFBKSzVyPUGyMlcyPjlizszN M4ixblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
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D-566MG NVTk[JRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTF|Lkm1O|Yh|ryP M4DYO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
KYSE-140 MkW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPyTWM2OD1zND6wO|U{KM7:TR?= NVzmSnNDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
SCC-4 MlnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGm3NXNKSzVyPUG0MlM{PTlizszN MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
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LAMA-84 NFi4TI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDpe4QyUUN3ME2xOE46QTN{IN88US=> NGXXR2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjNyMEKwM{c,W0GQR1XSQE9iRg>?
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ECC10 NFO2NWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDITIxKSzVyPUG1MlQ1PThizszN MmTaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI{ODB{MD:nQnNCVkeHUkyvZV4>
Daoy NFHjcpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PvVmlEPTB;MUWuO|YyPiEQvF2= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
SCH M4j2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HRTmlEPTB;MUWuO|g{PSEQvF2= M2n4bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOzByMkCvK|5USU6JRWK8M4E,
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CAL-12T NEHFbXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXX6N4FjUUN3ME2xOk41QDZ{IN88US=> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlMxODJyLze+V2FPT0WUPD;hQi=>
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NCI-H2228 NYLjOXZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rNUmlEPTB;MUeuN|A4OSEQvF2= NYW2eGZkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ|MECyNE8oRlODTlfFVlww[T5?
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NB1643 NXvIe4NNeUiWUzDhd5NigQ>? MWrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| NYjuTml[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 NWn4ZZdweUiWUzDhd5NigQ>? MUjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| NEjGZWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 MmLwdWhVWyCjc4PhfS=> NUjlTZF{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> NIewd|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC NHfRTW1yUFSVIHHzd4F6 NUG0dnhUeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> M{HaU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pAkt(Ser473) / pAkt(Thr308); 

PubMed: 21828154     


Immunoblot analysis revealed that both AZD6244 and PLX4720 induced an early (within 2–6 hours of exposure) increase in the levels of phosphorylated Akt (at residues Ser473 and Thr308) in both BRAF-mutant OCM3 and Gα-mutant OMM1.3 cells. Eventually, and with prolonged drug exposure, the phosphorylation of Akt returned to baseline in Gα-mutant OMM1.3 cells and decreased even below baseline levels in BRAF-mutant OCM3 cells.

p27 / Cyclin D1 / pRb; 

PubMed: 21828154     


Immunoblot analysis revealed that PLX4720 (3 μM) decreased levels of phosphorylated ERK, decreased levels of cyclin D1, increased levels of p27, and decreased levels of phosphorylated Rb in BRAF-mutant (OCM3) cells. On the contrary, in Gα-mutant (OMM1.3) UM cells, PLX4720 induced a paradoxical increase in phosphorylated ERK and Rb levels and an early increase in cyclin D1 levels but did not stimulate p27 levels.

p-EGFR 1173 / EGFR / p-Akt / Akt; 

PubMed: 26023796     


Three BRAF(V600E) glioma cell lines, NMC-G1, AM38 and DBTRG-05MG were subjected to a 24 hour time course treatment with 5 μM PLX4720 in the presence or absence of 1 μM HKI-272. These cells were serum starved for 16 hours before being stimulated with 10% FBS and harvested for immunoblotting analysis. Cells treated with PLX4720 alone showed an initial suppression of MEK and ERK phosphorylation followed by a profound rebound of MAPK pathway activation as early as one hour post-PLX4720 treatment. Elevated levels of EGFR phosphorylation were also observed in the PLX4720 treated cells. The extent of Akt phosphorylation increased upon PLX4720 treatment, although the extent varies between cell lines. In contrast, no reactivation of EGFR, MEK, ERK or Akt was observed in cells pre-treated with HKI-272.

p-MEK / MEK / p-ERK / ERK / p-FAK(S910); 

PubMed: 23076151     


WM793 and WM793-Res NRAS cells were seeded overnight in the absence of PLX4720 and then treated with 1 μm PLX4720 for times ranging from 0 to 24 h. Samples were analyzed by Western blotting for phospho-MEK, total MEK, phospho-ERK1/2, total ERK1/2, phospho-S910 FAK, and total FAK.

21828154 26023796 23076151
Immunofluorescence
ZKSCAN3 / TFEB ; 

PubMed: 30979895     


Representative confocal images of subcellular translocation of endogenous TFEB (green) and ZKSCAN3 (red) in A375 cells treated with PLX4720 (1 μM, 12 h). n = 3 independent experiments. 

LAMP1; 

PubMed: 30979895     


Representative images of LysoTracker Red (red) and LAMP1 (green) immunostaining of PLX4720 (1 μM, 12 h-treated) A375 cells with depletion of the indicated genes. Note the reduced lysosome staining in PLX4720-treated cells upon TFEB depletion. 

30979895
Growth inhibition assay
Cell viability; 

PubMed: 27848137     


AM-38 and DBTRG-05MG cells were treated for 5 days. Media was changed once every 3 days. Cell viability was measured using WST-1 assay. Error bars indicate the variation between triplicate measurements. PLX4720 and PD0325901 alone or in combination reduced cell viability significantly. However, combined therapy led to the most significant cell viability reduction compared to either monotherapy in both AM-38 and DBTRG-05MG cell lines.

27848137
ELISA
mIFN-γ; 

PubMed: 23204132     


(C, D and E) IFN-γ secretion by pmel-1 T cells co-cultured with transduced melanoma cells (after cell sorting) that had been pre-treated with the indicated concentrations of PLX4720, as determined by ELISA. (*P<0.05, ** P<0.01) Data are representative of 3 independent experiments.

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

Kinase Assay:[1]
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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]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL (200.56 mM)
Water Insoluble
Ethanol Insoluble
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

* 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.

Chemical Information

Molecular Weight 413.83
Formula

C17H14ClF2N3O3S

CAS No. 918505-84-7
Storage powder
in solvent
Synonyms N/A
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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID