Vemurafenib (PLX4032)

Catalog No.S1267 Synonyms: RG7204, RO5185426

For research use only.

Vemurafenib (PLX4032, RG7204, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.

Vemurafenib (PLX4032) Chemical Structure

CAS No. 918504-65-1

Selleck's Vemurafenib (PLX4032) has been cited by 532 publications

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Biological Activity

Description Vemurafenib (PLX4032, RG7204, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.
Features A novel and potent inhibitor of the B-RAFV600E oncoprotein.
Targets
SRMS [1]
(Cell-free assay)
ACK1 [1]
(Cell-free assay)
B-Raf (V600E) [1]
(Cell-free assay)
C-Raf [1]
(Cell-free assay)
MAP4K5 (KHS1) [1]
(Cell-free assay)
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18 nM 19 nM 31 nM 48 nM 51 nM
In vitro

PLX4032 inhibits B-RAFV600E, C-RAF, as well as wildtype B-RAF, with IC50 of 31 nM, 48 nM and 100 nM, respectively. PLX4032 also inhibits several non-RAF kinases, including ACK1, KHS1, and SRMS, with IC50 of 18 nM to 51 nM. [1] In melanoma cell lines, the inhibitory effect by PLX4032 depends on B-RAF mutational status, because PLX4032 potently inhibits those harboring B-RAF V600 mutants, including V600E, V600D, V600K, and V600R, but not wildtype or other mutants. The IC50 values of PLX4032 on these cells, including MALME-3M, Colo829, Colo38, A375, SK-MEL28, and A2058, ranges from 20 nM to 1 μM. In these cells, PLX4032 (0.1 μM to 30 μM) also inhibits the phosphorylation of both MEK1/2 and ERK1/2. [2] PLX4032 is highly effective in the treatment of melanoma, for its ability of inhibiting B-RAFV600E. However, PLX4032 displays limited effect in colon cancer patients that also carrying B-RAFV600E oncoprotein. The reason for this is that, in colon cancer cells, B-RAFV600E inhibition by PLX4032 results in a rapid feedback EGFR activation, which compensates for the PLX4032-inhibited cell proliferation. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKMEL19 M{HR[WZ2dmO2aX;uJGF{e2G7 NUfaVFl7PiEQvF2= NVTGeINvPDhiaB?= M175fWROW09? NXmxcVJMXHKrZ3fldpMhTVJic4Ty[ZN{ M1qwNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{[yNlQxLz5{M{O2NlI1ODxxYU6=
VMM12 M3nBW2Z2dmO2aX;uJGF{e2G7 NIfGfGY{KM7:TR?= M2nCWFQ5KGh? Mk\uSG1UVw>? M1;YUmlv[3KnYYPld{Bkd2yuYXflckB{gW62aHXzbZMh[W6mIHTlZ5Jm[XOnczDJUE06KGW6cILld5Nqd25? MoXRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7OEm1NFYoRjJ3OUi5OVA3RC:jPh?=
C4 NHXTd4JHfW6ldHnvckBCe3OjeR?= NW\JVXA3OyEQvF2= MY[0PEBp MUXEUXNQ MoTWTY5kemWjc3XzJINwdGyjZ3XuJJN6dnSqZYPpd{BidmRiZHXjdoVie2W|IFnMMVgh\XiycnXzd4lwdg>? NInybZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm4PVUxPid-MkW5PFk2ODZ:L3G+
Calu-6 MWXGeY5kfGmxbjDBd5NigQ>? M4DEc|HjiIoQvF2= MlLnNUBp M3fFXGROW09? M1n5dGFkfGm4YYTld{BOTUtxRWLLJIlvKGOnbHzzJJdqfGhid3ns[E11gXCnIFLSRWY> NEfZUI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEG3PVcxPSd-MkCxO|k4ODV:L3G+
PC MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfqdY86PiCq MX7FR|UxRiBzMECwJI5O MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh6MEe5Nkc,OTl6OEC3PVI9N2F-
TPC-1 (RET/PTC1) MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHUPJRbQTZiaB?= NXLaSnBVTUN3MPMJqVExODBibl2= MmnOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6OEC3PVIoRjF7OEiwO|kzRC:jPh?=
CAL62 (KRAS G12R) > 1000 > 1000 NF7YTWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLiPVYhcA>? MUjFR|UxRiBzMECwJI5O MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh6MEe5Nkc,OTl6OEC3PVI9N2F-
HTH7 (NRAS Q61R) M1LOSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPhPVYhcA>? NWL3cXJNTUN3MPMJqUAyODByIH7N Mn3GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6OEC3PVIoRjF7OEiwO|kzRC:jPh?=
C643 (HRAS G13R)≥ 500 NIHzOo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7sdZdxQTZiaB?= MVLFR|UxKOLLpTC1NFAhdk1? NGr2[FI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi4NFc6Oid-MUm4PFA4QTJ:L3G+
BCPAP (BRAF WT/V600E) MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3K0d|k3KGh? M13BRWVEPTB;N{igcm0> M33FRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEiwO|kzLz5zOUi4NFc6OjxxYU6=
BHT101 (BRAF WT/V600E) M3jxfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUS5OkBp M1rXfmVEPTB;OUegcm0> NGfW[2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi4NFc6Oid-MUm4PFA4QTJ:L3G+
SW1736 (BRAF WT/V600E) NUnJUXhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\BWZg5QTZiaB?= M3LkUWVEPTB;Mkmgcm0> NHzXWGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi4NFc6Oid-MUm4PFA4QTJ:L3G+
8505C (BRAF V600E/V600E) MoXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrPPVYhcA>? MmDlSWM2OD13NzDuUS=> NF\xZYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi4NFc6Oid-MUm4PFA4QTJ:L3G+
ARO MVHGeY5kfGmxbjDBd5NigQ>? MVyxNEDPxE1? MoDjO|IhcA>? NULpVZBHTE2VTx?= NWPKR5FGUW6mdXPld{B1cGVicnXlfJBz\XO|aX;uJI9nKHSqZTDOTXMheHWvcB?= NIrrVI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOES1PFA2Oyd-MUi0OVgxPTN:L3G+
A375 MXPBdI9xfG:|aYOgRZN{[Xl? MXKxNEDPxE1? M3vOc2ROW09? NHXiT|JRem:vb4Tld{BieG:ydH;0bYMh\GWjdHi= M3n4WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEW4NFU{Lz5zOES1PFA2OzxxYU6=
TPCI MmfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnP[mcyODBizszN NWDXXFNRQTZiaB?= NYXJW2pYTE2VTx?= MknwTWM2OD1zMD63O{DPxE1? NGDPTJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOES1PFA2Oyd-MUi0OVgxPTN:L3G+
ARO NX7ISGRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[3PGpvOTByIN88US=> MlHkPVYhcA>? NH\3OYxFVVOR M3\VOmlEPTB;MkC1JI5O NXrYT5V7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi0OVgxPTNpPkG4OFU5ODV|PD;hQi=>
NPA MnHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfxfHAyODBizszN NG\aPWM6PiCq MVPEUXNQ NVvvZpRpUUN3ME2yOkBvVQ>? NED3Wpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOES1PFA2Oyd-MUi0OVgxPTN:L3G+
A375 Mm\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHpNVAxKM7:TR?= NV;jR29[QTZiaB?= NVKyR3dXTE2VTx?= NFnSNpRKSzVyPUS3JI5O M{mxb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEW4NFU{Lz5zOES1PFA2OzxxYU6=
UKF-NB-3 (ABCB1) MVfGeY5kfGmxbjDBd5NigQ>? NIGxcYgyNjJ3INM1US=> MVWyJIg> MoO0SG1UVw>? NV7HNZpjTW6qYX7j[ZMh[WOldX31cIF1cW:wIH;mJJRp\SCobIXvdoV{[2WwdDDBRmNDOSC|dXLzeJJifGVicnjv[IFucW6nIEGyNy=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd|NUe2Okc,OjR5M{W3OlY9N2F-
UKF-NB-3 MYfGeY5kfGmxbjDBd5NigQ>? NWHVTIxoOS5{NTFCuW0> MnHTNkBp NU\jdlFJTE2VTx?= MVPTbYdvcW[rY3HueIx6KGGoZnXjeJMhd25iYXPjeY12dGG2aX;uJI9nKHSqZTDmcJVwemW|Y3XueEBCSkOEMTDzeYJ{fHKjdHWgdohw\GGvaX7lJFEzOw>? M3HsbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{O1O|Y3Lz5{NEezOVc3PjxxYU6=
A375 (BRAFV600E) NGXtPGRHfW6ldHnvckBCe3OjeR?= MXq4JIg> NWLaS4xPTE2VTx?= NH3QelRKdmO{ZXHz[ZMhcW62cnHj[YxtfWyjcjDSU3Mh[W6mIF7PJIxmfmWucx?= NUnacXo6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOlM3PDRpPkK1N|Y{PjR2PD;hQi=>
A375P MXjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MXHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF|N{XQJINmdGy|LDDJR|UxKD1iMD6yOVQh|ryPLh?= M4DNZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NE[wNFMxLz5{MkS2NFA{ODxxYU6=
A375 MkX5RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NWrEZZpVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIV5eHKnc4PpcochSi2UYX[gWlYxOEVibYX0ZY51KGGwZDD3bYxlKHS7cHWgVoF{NCCLQ{WwJF0hOC5|MTFOwG0v NVj5[o5yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFg6OTFpPkKyPFA5QTFzPD;hQi=>
A375P NUHhXoh6SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M{W4PVQ5KGi{cx?= M3;xVmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OXAh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNlUh|ryPLh?= NGfSW3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGyPFQyOCd-MkSxNlg1OTB:L3G+
A375 Mo[zR5l1d3SxeHnjbZR6KGG|c3H5 M4rX[FczKGi{cx?= NH7pUFZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjF6IN88UU4> M3niOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkG1PFE5Lz5{NEKxOVgyQDxxYU6=
SK-MEL-28 NV\nS4k{S3m2b4TvfIlkcXS7IHHzd4F6 MWPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiZYjwdoV{e2mwZzDCMZJi\iCYNkCwSUBufXSjboSsJGlEPTBiPTCwMlEh|ryPLh?= Mn;SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{G0OlYoRjJ2NEexOFY3RC:jPh?=
M229 M4jEN2N6fG:2b4jpZ4l1gSCjc4PhfS=> M1Hq[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG0zOjliY3XscJMh\XiycnXzd4lv\yCELYLh[kBXPjByRTDteZRidnRuIFnDOVAhRSByLkGg{txONg>? M2nPdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEexOFY3Lz5{NES3NVQ3PjxxYU6=
M263 NVf0e3o5S3m2b4TvfIlkcXS7IHHzd4F6 MWrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNNlY{KGOnbHzzJIV5eHKnc4PpcochSi2{YX[gWlYxOEVibYX0ZY51NCCLQ{WwJF0hOC5zIN88UU4> NInxfIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES3NVQ3Pid-MkS0O|E1PjZ:L3G+
M321 NGLXeHFEgXSxdH;4bYNqfHliYYPzZZk> NWqwV5JDS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVTN{MTDj[YxteyCneIDy[ZN{cW6pIFKtdoFnKFZ4MEDFJI12fGGwdDygTWM2OCB;IECuNUDPxE1w MlzLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{G0OlYoRjJ2NEexOFY3RC:jPh?=
M238 NGTBfIxEgXSxdH;4bYNqfHliYYPzZZk> MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNNlM5KGOnbHzzJIV5eHKnc4PpcochSi2{YX[gWlYxOEVibYX0ZY51NCCLQ{WwJF0hOC5zIN88UU4> MkHzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{G0OlYoRjJ2NEexOFY3RC:jPh?=
M262 NE\1bmFEgXSxdH;4bYNqfHliYYPzZZk> NH;jTmdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOOjZ{IHPlcIx{KGW6cILld5NqdmdiQj3yZYYhXjZyMFWgcZV1[W62LDDJR|UxKD1iMD6xJO69VS5? Mn;VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{G0OlYoRjJ2NEexOFY3RC:jPh?=
M249 M{fVNWN6fG:2b4jpZ4l1gSCjc4PhfS=> MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNNlQ6KGOnbHzzJIV5eHKnc4PpcochSi2{YX[gWlYxOEVibYX0ZY51NCCLQ{WwJF0hOC5zIN88UU4> NXm4So4zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0O|E1PjZpPkK0OFcyPDZ4PD;hQi=>
M14 M3\TUmN6fG:2b4jpZ4l1gSCjc4PhfS=> Mlu5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUVE1KGOnbHzzJIV5eHKnc4PpcochVlKDUzDHNVJEKG23dHHueEwhUUN3MDC9JFAvOTVizszNMi=> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR5MUS2Okc,OjR2N{G0OlY9N2F-
SK-MEL-28 NWf0XHBsSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MYe2PEBpenN? NWD2WnhYSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiaHHyZo9zcW6pIFLSRWYhXjZyMFWgcZV1[W62IHHmeIVzKDZ6IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkS4JO69VS5? MlOwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OEiwO|MoRjJ2NUi4NFc{RC:jPh?=
insect cell MVLGeY5kfGmxbjDhd5NigQ>? M2jYR|YxKG2rboO= NHzrco1KdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJIh2dWGwIFKtVoFnKFZ4MEDFJI12fGGwdDDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiaX7z[YN1KGOnbHzzJIF{e2W|c3XkJIF{KFupYX3tZU0{O1CfaX7jc5Jxd3KjdHnvckBqdnSxIF3FT{Bi\nSncjC2NEBucW6|IHL5JJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFnDOVAhRSByLkCzNUDPxE1w NVHnUG1URGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA{OTVpPkK0PVAxOzF3PD;hQi=>
MALME-3M NVr1XGF7TnWwY4Tpc44h[XO|YYm= M4\ldVEhcHJ? MXvJcohq[mm2aX;uJI9nKEJvUnHmJHY3ODCHIH31eIFvfC2vZXTpZZRm\CCHcnugdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF3BUG1GNTOPIHPlcIx{KGGodHXyJFEhcHJiYomg[ox2d3Knc3PlcoNmKGGwYXz5d4l{NCCLQ{WwJF0hOC5yNkGg{txONg>? MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEOxOUc,OjR7MECzNVU9N2F-
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OHS-50 MmCxdWhVWyCjc4PhfS=> MX7xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| M1rleFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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SJ-GBM2 M4nZeJFJXFNiYYPzZZk> MULxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= NYLacJp5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC NWfBWWlkeUiWUzDhd5NigQ>? NVvTNHNzeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> M{nXXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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TC32 MlzUdWhVWyCjc4PhfS=> M13kVZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM> MlLqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Assay
Methods Test Index PMID
Western blot p-ERK / p-CRAF ; p-MEK(S217/221) / pAKT(T308) / p-AKT(S473) / p-P70 S6K(T389) / p-S6(Ser235-236) / P-4EB-P1 ; Bax / Bcl2 / Bcl-xl / BIM / Mcl1 22448344 22194965 28382170
Growth inhibition assay Cell viability 29179510
Immunofluorescence uPAR / α5-β1 ; p-Akt(Thr308) 30611716 27293997
In vivo In B-RAFV600E-mutant mice xenograft models, PLX4032 (6 mg/kg–20 mg/kg) inhibits tumor growth. [1] In mice xenograft models of LOX, Colo829, and A375 cells, PLX4032 (12.5 mg/kg–100 mg/kg) inhibits tumor growth and prolongs mice survival. [2]

Protocol (from reference)

Kinase Assay:

[1]

  • RAF kinase activity measurements:

    The kinase activities of wild-type RAF and mutants are determined by measuring phosphorylation of biotinylated-BAD protein. For each enzyme (0.01 ng), 20 μL reactions are carried out in 20 mM Hepes (pH 7.0), 10 mM MgCl2, 1 mM DTT, 0.01% (v/v) Tween-20, 50 nM biotin-BAD protein, and 1 mM ATP at room temperature. Reactions are stopped at 5 min with 5 μL of a solution containing 20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, 0.3% (w/v) bovine serum albumin (BSA). The stop solution also includes phospho-BAD (Ser112) antibody, streptavidin-coated donor beads, and protein A acceptor beads. The antibody and beads are pre-incubated in stop solution in the dark at room temperature for 30 min. The final dilution of antibody is 1/2000 and the final concentration of each bead is 10 μg/mL. The assay plates are incubated at room temperature for one hour and then are read on a PerkinElmer AlphaQuest reader. Mutant activities are the average of two different batches of purified protein assayed in duplicate in three different experiments.

Cell Research:

[2]

  • Cell lines: MALME-3M, Colo829, Colo38, A375, SK-MEL28, and A2058 cells
  • Concentrations: 0–10 μM , dissolved in DMSO
  • Incubation Time: 5 days
  • Method:

    Cellular proliferation is evaluated by MTT assay. Briefly, cells are plated in 96-well microtiter plates at a density of 1000 to 5000 cells per well in a volume of 180 μL. PLX4032 is prepared at 10 times the final assay concentration in media containing 1% DMSO. Twenty-four hours after cell plating, 20 μL of the appropriate dilution of PLX4032 are added to plates in duplicate. The plates are assayed for proliferation 6 days after the cells are plated. Percent inhibition is calculated and the IC50 is determined from the regression of a plot of the logarithm of the concentration versus percent inhibition.

  • (Only for Reference)
Animal Research:

[2]

  • Animal Models: Mice (athymic nude) xenograft models of LOX, Colo829, and A375 cells
  • Dosages: 12.5 mg/kg–100 mg/kg
  • Administration: Oral gavage twice daily
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 97 mg/mL
(197.99 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+61% ddH2O
For best results, use promptly after mixing.

1.25mg/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 489.92
Formula

C23H18ClF2N3O3S

CAS No. 918504-65-1
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)C4=CC=C(C=C4)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

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05068752 Recruiting Drug: Vemurafenib|Drug: Sorafenib Pancreas Cancer HonorHealth Research Institute|Bayer|Genentech Inc. October 28 2021 Phase 2
NCT03410875 Active not recruiting Drug: Vemurafenib|Drug: Obinutuzumab Hairy Cell Leukemia|Leukemia|Leukemia Hairy Cell Memorial Sloan Kettering Cancer Center|Dana-Farber Cancer Institute|Yale University February 9 2018 Phase 2
NCT03013491 Active not recruiting Drug: CX-072|Drug: ipilimumab|Drug: vemurafenib Solid Tumor|Lymphoma CytomX Therapeutics January 2017 Phase 1|Phase 2
NCT02441465 Completed Drug: Vemurafenib|Drug: 14C-Labeled Vemurafenib Malignant Melanoma Cancer Hoffmann-La Roche August 13 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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:
How about the half-life of Vemurafenib(S1267)?

Answer:
It was reported that the half-life of the compound is 57 hours.

Question 2:
The vemurafenib power, when prepared in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O solutions, form a pellet down the tube?

Answer:
When prepare this kind of vehicle, please dissolve the drug in DMSO clearly first. If it dissolves not readily, please sonicate and warm in the water bath at about 45 degree. Then add PEG and Tween. After they mixed homogeneously, then dilute with water.

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