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Vemurafenib (PLX4032)

Name: Vemurafenib (PLX4032)
Brand: Selleck Chemicals
SKU: S1267
Rating: 5 (554 reviews)

Catalog No.S1267 Synonyms: RG7204, RO5185426

For research use only.

Vemurafenib (PLX4032, RG7204, RO5185426) is a novel and potent inhibitor of B-Raf^V600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-Raf^V600E 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 554 publications

Purity & Quality Control

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Raf Signaling Pathway Map

Biological Activity

Description

Features

A novel and potent inhibitor of the B-RAF^V600E 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)	Click to View More Targets
18 nM	19 nM	31 nM	48 nM	51 nM	Click to View More Targets

In vitro

PLX4032 inhibits B-RAF^V600E, 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-RAF^V600E. However, PLX4032 displays limited effect in colon cancer patients that also carrying B-RAF^V600E oncoprotein. The reason for this is that, in colon cancer cells, B-RAF^V600E 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	NGTYdIFHfW6ldHnvckBCe3OjeR?=	MmfaOkDPxE1?	MV[0PEBp	MX7EUXNQ	NX7K[5RoXHKrZ3fldpMhTVJic4Ty[ZN{	MmHOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|NkKyOFAoRjJ\|M{[yNlQxRC:jPh?=
VMM12	M2TIdWZ2dmO2aX;uJGF{e2G7	MmnYN{DPxE1?	MYe0PEBp	MX\EUXNQ	MmrjTY5kemWjc3XzJINwdGyjZ3XuJJN6dnSqZYPpd{BidmRiZHXjdoVie2W\|IFnMMVkh\XiycnXzd4lwdg>?	NF7UcII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm4PVUxPid-MkW5PFk2ODZ:L3G+
C4	MnTiSpVv[3Srb36gRZN{[Xl?	MYWzJO69VQ>?	M2ewUVQ5KGh?	M3jxcWROW09?	NX34TJJSUW6lcnXhd4V{KGOxbHzh[4VvKHO7boTo[ZNqeyCjbnSg[IVkemWjc3XzJGlNNThiZYjwdoV{e2mxbh?=	NWnmZng6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5PFk2ODZpPkK1PVg6PTB4PD;hQi=>
Calu-6	M1vubGZ2dmO2aX;uJGF{e2G7	MlLsNgKBkc7:TR?=	MUOxJIg>	MVXEUXNQ	MYrBZ5RqfmG2ZYOgUWVMN0WUSzDpckBk\WyuczD3bZRpKHerbHSteJlx\SCEUlHG	NXfy[2RERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO\|k4ODVpPkKwNVc6PzB3PD;hQi=>
PC	NVi3eJVxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MkTiPVYhcA>?		NGDrVolGSzVyPjCxNFAxKG6P	MoHJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6OEC3PVIoRjF7OEiwO\|kzRC:jPh?=
TPC-1 (RET/PTC1)	M3y3NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NUHrdIhGQTZiaB?=		NYWzbWg{TUN3MPMJqVExODBibl2=	NYPKb2NtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4PFA4QTJpPkG5PFgxPzl{PD;hQi=>
CAL62 (KRAS G12R) > 1000 > 1000	NY\0NVV5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NF\NXXo6PiCq		M125RWVEPTB-IEGwNFAhdk1?	MoW0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6OEC3PVIoRjF7OEiwO\|kzRC:jPh?=
HTH7 (NRAS Q61R)	M{DMeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MWO5OkBp		MYLFR\|Ux6onnIEGwNFAhdk1?	MkT0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6OEC3PVIoRjF7OEiwO\|kzRC:jPh?=
C643 (HRAS G13R)≥ 500	NWLRN5RUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M1fIZ\|k3KGh?		NF\mSpRGSzVyIPMJqUA2ODBibl2=	NVWxUJJLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4PFA4QTJpPkG5PFgxPzl{PD;hQi=>
BCPAP (BRAF WT/V600E)	Mon2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NGPvbYs6PiCq		MY\FR\|UxRTd6IH7N	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh6MEe5Nkc,OTl6OEC3PVI9N2F-
BHT101 (BRAF WT/V600E)	MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M1jZVlk3KGh?		NH7iR\|NGSzVyPUm3JI5O	M1;HOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEiwO\|kzLz5zOUi4NFc6OjxxYU6=
SW1736 (BRAF WT/V600E)	NUCzRlAxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M2nz[\|k3KGh?		MnvDSWM2OD1{OTDuUS=>	M{\5O\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEiwO\|kzLz5zOUi4NFc6OjxxYU6=
8505C (BRAF V600E/V600E)	MnvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NIn5SIY6PiCq		NULRepROTUN3ME21O{BvVQ>?	MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh6MEe5Nkc,OTl6OEC3PVI9N2F-
ARO	NXLabJBlTnWwY4Tpc44hSXO\|YYm=	NIDKcmEyOCEQvF2=	NVrwb4lIPzJiaB?=	M1vLRWROW09?	NXLXU4I5UW6mdXPld{B1cGVicnXlfJBz\XO\|aX;uJI9nKHSqZTDOTXMheHWvcB?=	MnTkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh2NUiwOVMoRjF6NEW4NFU{RC:jPh?=
A375	NHPxd5ZCeG:ydH;zbZMhSXO\|YYm=	NFLKb5kyOCEQvF2=		MXXEUXNQ	M2K3O3Bzd22xdHXzJIFxd3C2b4TpZ{Bl\WG2aB?=	M3n1SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEW4NFU{Lz5zOES1PFA2OzxxYU6=
TPCI	MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NIiwNXIyODBizszN	NXnsSlN1QTZiaB?=	MXXEUXNQ	NIjufG1KSzVyPUGwMlc4KM7:TR?=	MmDZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh2NUiwOVMoRjF6NEW4NFU{RC:jPh?=
ARO	NI\mTYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MkCxNVAxKM7:TR?=	M13HVFk3KGh?	NF7TSnJFVVOR	M3vSVGlEPTB;MkC1JI5O	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDR3OEC1N{c,OTh2NUiwOVM9N2F-
NPA	M1nrSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWSxNFAh\|ryP	MlL1PVYhcA>?	M3OzeWROW09?	NIW1foxKSzVyPUK2JI5O	M4L0XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEW4NFU{Lz5zOES1PFA2OzxxYU6=
A375	NIW2U4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NGrORlQyODBizszN	M37VU\|k3KGh?	MmTqSG1UVw>?	MofiTWM2OD12NzDuUS=>	NUHVZ4NJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi0OVgxPTNpPkG4OFU5ODV\|PD;hQi=>
UKF-NB-3 (ABCB1)	MlKySpVv[3Srb36gRZN{[Xl?	NVHScllPOS5{NTFCuW0>	MYqyJIg>	Mn[xSG1UVw>?	M4C3e2VvcGGwY3XzJIFk[3WvdXzheIlwdiCxZjD0bIUh\my3b4Lld4NmdnRiQVLDRlEhe3Wkc4TyZZRmKHKqb3ThcYlv\SBzMkO=	NIPtcGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEezOVc3Pid-MkS3N\|U4PjZ:L3G+
UKF-NB-3	MX3GeY5kfGmxbjDBd5NigQ>?	NILtbYgyNjJ3INM1US=>	M4XS[VIhcA>?	MlXTSG1UVw>?	Mm\sV4lodmmoaXPhcpRtgSCjZn\lZ5R{KG:wIHHjZ5VufWyjdHnvckBw\iC2aHWg[ox2d3Knc3PlcpQhSUKFQkGgd5Vje3S{YYTlJJJpd2SjbXnu[UAyOjN?	NV\LTFZVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3N\|U4PjZpPkK0O\|M2PzZ4PD;hQi=>
A375 (BRAFV600E)	NXjxO2lVTnWwY4Tpc44hSXO\|YYm=		NUHlbId4QCCq	M2nLN2ROW09?	NUTqcpRTUW6lcnXhd4V{KGmwdILhZ4VtdHWuYYKgVm9UKGGwZDDOU{Bt\X[nbIO=	NXS4bWV7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOlM3PDRpPkK1N\|Y{PjR2PD;hQi=>
A375P	MX3BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?				NIHFdIRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO\|VRKGOnbHzzMEBKSzVyIE2gNE4zPTRizszNMi=>	M2X2SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NE[wNFMxLz5{MkS2NFA{ODxxYU6=
A375	NIPBRWVCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=				NHv3flNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO\|Uh[2WubIOg[ZhxemW\|c3nu[{BDNVKjZjDWOlAxTSCvdYThcpQh[W6mIIfpcIQhfHmyZTDSZZMtKEmFNUCgQUAxNjNzIN88UU4>	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyOEmxNUc,OjJ6MEi5NVE9N2F-
A375P	M2W0TWFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MWS0PEBpenN?		NHTOe4pCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO\|VRKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCwMlI2KM7:TT6=	MnLhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzMki0NVAoRjJ2MUK4OFExRC:jPh?=
A375	NHSyR3pEgXSxdH;4bYNqfHliYYPzZZk>		NXrQbJhQPzJiaILz		MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBN\|c2KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCwMlE5KM7:TT6=	MnezQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{MUW4NVgoRjJ2MkG1PFE5RC:jPh?=
SK-MEL-28	NYfJe2JUS3m2b4TvfIlkcXS7IHHzd4F6				NUPXPYVkS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTVXMMVI5KGOnbHzzJIV5eHKnc4PpcochSi2{YX[gWlYxOEVibYX0ZY51NCCLQ{WwJF0hOC5zIN88UU4>	M336RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEexOFY3Lz5{NES3NVQ3PjxxYU6=
M229	MljQR5l1d3SxeHnjbZR6KGG\|c3H5				MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNNlI6KGOnbHzzJIV5eHKnc4PpcochSi2{YX[gWlYxOEVibYX0ZY51NCCLQ{WwJF0hOC5zIN88UU4>	NV3KfZplRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0O\|E1PjZpPkK0OFcyPDZ4PD;hQi=>
M263	M2rtWGN6fG:2b4jpZ4l1gSCjc4PhfS=>				MojSR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUVI3OyClZXzsd{BmgHC{ZYPzbY5oKEJvcnHmJHY3ODCHIH31eIFvfCxiSVO1NEA:KDBwMTFOwG0v	M1[3UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEexOFY3Lz5{NES3NVQ3PjxxYU6=
M321	MV3DfZRwfG:6aXPpeJkh[XO\|YYm=				MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNN\|IyKGOnbHzzJIV5eHKnc4PpcochSi2{YX[gWlYxOEVibYX0ZY51NCCLQ{WwJF0hOC5zIN88UU4>	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR5MUS2Okc,OjR2N{G0OlY9N2F-
M238	M3LMb2N6fG:2b4jpZ4l1gSCjc4PhfS=>				NUPJdXdvS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVTJ\|ODDj[YxteyCneIDy[ZN{cW6pIFKtdoFnKFZ4MEDFJI12fGGwdDygTWM2OCB;IECuNUDPxE1w	Mn:zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{G0OlYoRjJ2NEexOFY3RC:jPh?=
M262	NX3Db2htS3m2b4TvfIlkcXS7IHHzd4F6				MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNNlYzKGOnbHzzJIV5eHKnc4PpcochSi2{YX[gWlYxOEVibYX0ZY51NCCLQ{WwJF0hOC5zIN88UU4>	MknNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{G0OlYoRjJ2NEexOFY3RC:jPh?=
M249	M2LSdWN6fG:2b4jpZ4l1gSCjc4PhfS=>				NXzyNIlCS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVTJ2OTDj[YxteyCneIDy[ZN{cW6pIFKtdoFnKFZ4MEDFJI12fGGwdDygTWM2OCB;IECuNUDPxE1w	NVLJV5F3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0O\|E1PjZpPkK0OFcyPDZ4PD;hQi=>
M14	M2PjPGN6fG:2b4jpZ4l1gSCjc4PhfS=>				MlXHR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUVE1KGOnbHzzJIV5eHKnc4PpcochVlKDUzDHNVJEKG23dHHueEwhUUN3MDC9JFAvOTVizszNMi=>	M3vhc\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEexOFY3Lz5{NES3NVQ3PjxxYU6=
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Sf9	MnvjSpVv[3Srb36gZZN{[Xl?		M3LpfFMxKG2rboO=		NF;oZpJKdmirYnn0bY9vKG:oIF6teIVzdWmwYXygS3NVNXSjZ3fl[EBz\WOxbXLpcoFvfCCqdX3hckBnfWyuLXzlcod1cCCcQVug[ZhxemW\|c3XkJIlvKGKjY4Xsc5ZqenW\|IHnu[oVkfGWmIGPmPUBqdnOnY4SgZ4VtdHNidYPpcochVUKSIHHzJJN2[nO2cnH0[UBi\nSncjCzNEBucW6\|IHL5JGFFWC2JbH:gZZN{[XluIFnDOVAhRSByLkCzNVQh\|ryPLh?=	NGnFfXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEW4OlIyOSd-Mki1PFYzOTF:L3G+
UACC-903	MnXSR5l1d3SxeHnjbZR6KGG\|c3H5	NFz1OGczPSC3TR?=	MoTOOFghcHK\|		Mm[1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWWFESy17MEOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYYSgNlUhfU1iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSC{ZXzheIl3\SC2bzDjc451em:uLDDJR\|UxKD1iMz62JO69VS5?	M13HZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUOzNFM2Lz5{OUGzN\|A{PTxxYU6=
CHL-1	NH3pcXhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NVv5cm4xPzJiaILz		NVS0XnlESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDTGwuOSClZXzsd{Bp[XKkb4Lpcochf2muZDD0fZBmKEKUQV[gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEGzMlch\|ryPLh?=	NW[5NZViRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxN\|MxOzVpPkK5NVM{ODN3PD;hQi=>
A375	NGDrVIFHfW6ldHnvckBie3OjeR?=		MlLoPVYhcHK\|		MknaTY5pcWKrdHnvckBw\iCEUlHGJHY3ODCHIH31eIFvfCCrbjDoeY1idiCDM{e1JINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJBzd2yrZnXyZZRqd25iaX7jeYJifGWmIH\vdkA6PiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC5zMkeg{txONg>?	NXfpRZhNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PzdpPkK5OFA4QTd5PD;hQi=>
A375	NXTZfZlTTnWwY4Tpc44h[XO\|YYm=				NE\QVHJKdmirYnn0bY9vKG:oIFLSRWYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIFGzO\|Uh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKGmwIFXST{BxcG:\|cHjvdplt[XSrb36gZpkhSWyyaHHTZ5Jm\W5iYYPzZZktKEmFNUCgQUAxNjB\|MjFOwG0v	Mlj6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NkG4NlcoRjJ7NE[xPFI4RC:jPh?=
SK-MEL-32	M1nTV2N6fG:2b4jpZ4l1gSCjc4PhfS=>				NYPTbnBLS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTVXMMVMzKGOnbHzzMEBKSzVyIE2gNE4{OSEQvF2u	M3zQWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NE[xPFI4Lz5{OUS2NVgzPzxxYU6=
WM266.4	NEHiNmNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		M3HiN\|Q5KGi{cx?=		NIXNSIhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGfNNlY3NjRiY3XscJMh[W[2ZYKgOFghcHK\|IHL5JG1VXCCjc4PhfUwhT0l3MDC9JFAvOjFizszNMi=>	NXvLTWRlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFA1PjNpPkK5PVQxPDZ\|PD;hQi=>
A375	NXvzVFJPSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NUXEOnpIPDhiaILz		MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF\|N{WgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiR1m1NEA:KDBwOUWg{txONg>?	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl2MES2N{c,Ojl7NEC0OlM9N2F-
HT-29	MU\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MVq0PEBpenN?		NIjUTHlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO\|YYmsJGdKPTBiPTCxMlg5KM7:TT6=	M1n2PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUSwOFY{Lz5{OUm0NFQ3OzxxYU6=
WM1361	NUTEblhiSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		Mo[4OFghcHK\|		NXzxWoNXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDXUVE{PjFiY3XscJMh[W[2ZYKgOFghcHK\|IHL5JG1VXCCjc4PhfUwhT0l3MDC9JFIxNjhizszNMi=>	MmPXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NEC0OlMoRjJ7OUSwOFY{RC:jPh?=
HCT116	M1:1UmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MVe0PEBpenN?		MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDHTVUxKD1iMkWuNkDPxE1w	NWHtOGhHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFA1PjNpPkK5PVQxPDZ\|PD;hQi=>
A673	NE\WSppyUFSVIHHzd4F6				MoS4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN?	NEXVT2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
DAOY	MoDodWhVWyCjc4PhfS=>				NUHWRmtieUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFTBU3kh[2WubIO=	NF3PWo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
RD	NUnUZYRUeUiWUzDhd5NigQ>?				MXHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM>	NXK4NmVqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH	MVvxTHRUKGG\|c3H5				M2T3[ZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
MG 63 (6-TG R)	MVnxTHRUKGG\|c3H5				MVrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN?	NG\0[FE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
NB1643	MoDYdWhVWyCjc4PhfS=>				MVrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy\|	MnvqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
OHS-50	M1PTZpFJXFNiYYPzZZk>				MmG1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?=	M2[0fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673	M4fZfZFJXFNiYYPzZZk>				NUfZNVBneUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl?	Mk\oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
U-2 OS	MkHBdWhVWyCjc4PhfS=>				MUPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDVMVIhV1NiY3XscJM>	NYe1U5h[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41	Mkj2dWhVWyCjc4PhfS=>				M{i3WJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpPDFiY3XscJM>	MnzxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2	M4eySJFJXFNiYYPzZZk>				NIfqXnlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=>	NV;vR4V7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC	MV7xTHRUKGG\|c3H5				MWfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	NHPCeXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
LAN-5	NYrTWWpDeUiWUzDhd5NigQ>?				M{j4UJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?=	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-MC	MWDxTHRUKGG\|c3H5				Mn[zdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2PQzDj[Yxtew>?	NXuzXW1{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32	NGfQ[VRyUFSVIHHzd4F6				M2rBd5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM>	NFrUSmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+

Click to View More Cell Line Experimental Data

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-RAF^V600E-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.
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

References

+ Expand

Solubility (25°C)

In vitro


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. Click to purchase: PEG300 Tween 80	1.25mg/mL

Chemical Information

Molecular Weight	489.92
Formula	C₂₃H₁₈ClF₂N₃O₃S
CAS No.	918504-65-1
Storage	3 years	-20°C	powder
Storage	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

Download Vemurafenib (PLX4032) SDF

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:μL Number of animals:

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% DMSO + % + % Tween 80 + % ddH₂O

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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
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Dilution Calculator Molecular Weight Calculator

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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