Vemurafenib (PLX4032)

For research use only. Not for use in humans.

目录号：S1267 别名： RG7204, RO5185426 中文名称：维罗非尼

Vemurafenib (PLX4032) Chemical Structure

CAS No. 918504-65-1

Vemurafenib (PLX4032, RG7204, RO5185426)是一种新型有效的B-Raf^V600E抑制剂，IC50为31 nM。Vemurafenib对B-Raf^V600E的选择性比对野生型B-Raf的选择性高10倍，在细胞实验中，选择性可高100倍以上。Vemurafenib (PLX4032, RG7204) 可诱导自噬。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 746.23	现货
10mg	RMB 567.23	现货
50mg	RMB 2213.19	现货
200mg	RMB 6308.84	现货
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客户使用Selleck生产的Vemurafenib (PLX4032)发表文献516篇：

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产品安全说明书

Raf抑制剂选择性比较

生物活性

产品描述

特性

PLX4032是新型有效的B-RAF^V600E 肿瘤蛋白抑制剂。

靶点

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)	点击更多
18 nM	19 nM	31 nM	48 nM	51 nM	点击更多

体外研究

PLX4032抑制B-RAF^V600E, C-RAF, 和野生型B-RAF, IC50分别为31 nM, 48 nM, 和100 nM。PLX4032 也抑制一些非-RAF激酶,包括ACK1, KHS1,和SRMS, IC50 为18 nM 到51 nM。^[1] PLX4032作用于黑色素瘤细胞系，抑制效果依赖于B-RAF突变状态，因为PLX4032有效抑制含B-RAF^V600突变的细胞, 包括V600E, V600D, V600K, 和V600R, 但是对野生型或其他突变没有作用效果。PLX4032作用于MALME-3M, Colo829, Colo38, A375, SK-MEL28, 和A2058细胞时，IC50为20 nM 到 1 μM。0.1 μM 到30 μM PLX4032 也抑制MEK1/2 和ERK1/2磷酸化作用。^[2] PLX4032高效作用于黑色素瘤的治疗，因为PLX4032有效抑制B-RAF^V600E。PLX4032作用于结肠癌细胞，抑制B-RAF ^V600E导致 EGFR激活的快速回应，可用于补偿PLX4032抑制的细胞增殖。^[3]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
SKMEL19	Ml;CSpVv[3Srb36gRZN{[Xl?	MnnwOkDPxE1?	NGLjWoY1QCCq	M3;We2ROW09?	M4rKPHRzcWepZYLzJGVTKHO2cnXzdy=>	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN4MkK0NEc,OjN\|NkKyOFA9N2F-
VMM12	MUPGeY5kfGmxbjDBd5NigQ>?	NIjadVE{KM7:TR?=	MWG0PEBp	NVe4XY1STE2VTx?=	Mof1TY5kemWjc3XzJINwdGyjZ3XuJJN6dnSqZYPpd{BidmRiZHXjdoVie2W\|IFnMMVkh\XiycnXzd4lwdg>?	NIfuOZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm4PVUxPid-MkW5PFk2ODZ:L3G+
C4	NHznSIFHfW6ldHnvckBCe3OjeR?=	Ml3XN{DPxE1?	M2n0VFQ5KGh?	NHXWbHZFVVOR	Ml7WTY5kemWjc3XzJINwdGyjZ3XuJJN6dnSqZYPpd{BidmRiZHXjdoVie2W\|IFnMMVgh\XiycnXzd4lwdg>?	MorqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7OEm1NFYoRjJ3OUi5OVA3RC:jPh?=
Calu-6	MXnGeY5kfGmxbjDBd5NigQ>?	MkTBNgKBkc7:TR?=	NUDhXYMyOSCq	M2DrU2ROW09?	NFHEdlZC[3SrdnH0[ZMhVUWNL1XST{BqdiClZXzsd{B4cXSqIIfpcIQufHmyZTDCVmFH	NVHFXI94RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO\|k4ODVpPkKwNVc6PzB3PD;hQi=>
PC	NYnrPFVnT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MnLtPVYhcA>?		MkXJSWM2OD5iMUCwNEBvVQ>?	MnH0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6OEC3PVIoRjF7OEiwO\|kzRC:jPh?=
TPC-1 (RET/PTC1)	M2HsT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MUC5OkBp		MWXFR\|Ux6onnMUCwNEBvVQ>?	M2S1c\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEiwO\|kzLz5zOUi4NFc6OjxxYU6=
CAL62 (KRAS G12R) > 1000 > 1000	M1XuZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MV[5OkBp		NGD1SGRGSzVyPjCxNFAxKG6P	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh6MEe5Nkc,OTl6OEC3PVI9N2F-
HTH7 (NRAS Q61R)	NGfXcm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NW[5fVB1QTZiaB?=		MoHESWM2OOLLpTCxNFAxKG6P	M2rXS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEiwO\|kzLz5zOUi4NFc6OjxxYU6=
C643 (HRAS G13R)≥ 500	Mme2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NIX1TI86PiCq		MojwSWM2OCEkibWgOVAxKG6P	NVvP[21{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4PFA4QTJpPkG5PFgxPzl{PD;hQi=>
BCPAP (BRAF WT/V600E)	NVmxPYNxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NX7qZVJjQTZiaB?=		MX\FR\|UxRTd6IH7N	NUXnN3UyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4PFA4QTJpPkG5PFgxPzl{PD;hQi=>
BHT101 (BRAF WT/V600E)	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M3X5dFk3KGh?		NF:zXGFGSzVyPUm3JI5O	NULjc2tXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4PFA4QTJpPkG5PFgxPzl{PD;hQi=>
SW1736 (BRAF WT/V600E)	NIXQOWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M1nJUVk3KGh?		MmXVSWM2OD1{OTDuUS=>	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh6MEe5Nkc,OTl6OEC3PVI9N2F-
8505C (BRAF V600E/V600E)	MmnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NUTDO2NxQTZiaB?=		M3\WXGVEPTB;NUegcm0>	NEj0epo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi4NFc6Oid-MUm4PFA4QTJ:L3G+
ARO	NGHCdIdHfW6ldHnvckBCe3OjeR?=	NXvlVHJlOTBizszN	NHXDOIw4OiCq	Mn\5SG1UVw>?	Mn;1TY5lfWOnczD0bIUhemWneIDy[ZN{cW:wIH;mJJRp\SCQSWOgdJVueA>?	NF;TOII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOES1PFA2Oyd-MUi0OVgxPTN:L3G+
A375	M{\nXGFxd3C2b4Ppd{BCe3OjeR?=	M1nRNVExKM7:TR?=		MnL1SG1UVw>?	NYTxfW5JWHKxbX;0[ZMh[XCxcITveIlkKGSnYYTo	NFHINXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOES1PFA2Oyd-MUi0OVgxPTN:L3G+
TPCI	NEL2RWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYqxNFAh\|ryP	M3vlUFk3KGh?	MVHEUXNQ	MWPJR\|UxRTFyLke3JO69VQ>?	NHTq[HQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOES1PFA2Oyd-MUi0OVgxPTN:L3G+
ARO	M4Twemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWmxNFAh\|ryP	MYq5OkBp	M2fic2ROW09?	M1f3V2lEPTB;MkC1JI5O	M4jtR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEW4NFU{Lz5zOES1PFA2OzxxYU6=
NPA	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnHsNVAxKM7:TR?=	MX:5OkBp	NEjFcYZFVVOR	MW\JR\|UxRTJ4IH7N	M3fxbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEW4NFU{Lz5zOES1PFA2OzxxYU6=
A375	MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnHyNVAxKM7:TR?=	NFrXNZc6PiCq	NWS0[WNmTE2VTx?=	NHHNWW1KSzVyPUS3JI5O	NF;Y[mI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOES1PFA2Oyd-MUi0OVgxPTN:L3G+
UKF-NB-3 (ABCB1)	NV;RNW9oTnWwY4Tpc44hSXO\|YYm=	NGDrR2YyNjJ3INM1US=>	NYnDUVVkOiCq	NYjLb\|QyTE2VTx?=	M{nVS2VvcGGwY3XzJIFk[3WvdXzheIlwdiCxZjD0bIUh\my3b4Lld4NmdnRiQVLDRlEhe3Wkc4TyZZRmKHKqb3ThcYlv\SBzMkO=	NX7qOGpPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3N\|U4PjZpPkK0O\|M2PzZ4PD;hQi=>
UKF-NB-3	NVS4bndMTnWwY4Tpc44hSXO\|YYm=	MX[xMlI2KML3TR?=	MlnaNkBp	MVnEUXNQ	NGHBVXVUcWewaX\pZ4FvfGy7IHHm[oVkfHNib36gZYNkfW23bHH0bY9vKG:oIITo[UBndHWxcnXzZ4VvfCCDQlPCNUB{fWK\|dILheIUhemixZHHtbY5mKDF{Mx?=	NXnMVod[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3N\|U4PjZpPkK0O\|M2PzZ4PD;hQi=>
A375 (BRAFV600E)	MoKySpVv[3Srb36gRZN{[Xl?		MkLPPEBp	MVnEUXNQ	MXfJcoNz\WG\|ZYOgbY51emGlZXzseYxieiCUT2OgZY5lKE6RIHzleoVtew>?	NXXsVWtJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOlM3PDRpPkK1N\|Y{PjR2PD;hQi=>
A375P	MmXQRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?				M4HGSGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OXAh[2WubIOsJGlEPTBiPTCwMlI2PCEQvF2u	M362PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NE[wNFMxLz5{MkS2NFA{ODxxYU6=
A375	NWLXUGdpSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=				MoPRRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCDM{e1JINmdGy\|IHX4dJJme3OrbnegRk1T[WZiVk[wNGUhdXW2YX70JIFv\CC5aXzkJJR6eGViUnHzMEBKSzVyIE2gNE4{OSEQvF2u	NF3Q[m09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiwPFkyOSd-MkK4NFg6OTF:L3G+
A375P	MonKRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NVzJZ4NYPDhiaILz		M1THZ2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OXAh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNlUh\|ryPLh?=	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF{OESxNEc,OjRzMki0NVA9N2F-
A375	M3zEXWN6fG:2b4jpZ4l1gSCjc4PhfS=>		NF\0[VI4OiCqcoO=		NYnZVIN{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTN5NTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC5zODFOwG0v	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJzNUixPEc,OjR{MUW4NVg9N2F-
SK-MEL-28	MmHhR5l1d3SxeHnjbZR6KGG\|c3H5				MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiZYjwdoV{e2mwZzDCMZJi\iCYNkCwSUBufXSjboSsJGlEPTBiPTCwMlEh\|ryPLh?=	MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR5MUS2Okc,OjR2N{G0OlY9N2F-
M229	M3jwdmN6fG:2b4jpZ4l1gSCjc4PhfS=>				NFntboFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOOjJ7IHPlcIx{KGW6cILld5NqdmdiQj3yZYYhXjZyMFWgcZV1[W62LDDJR\|UxKD1iMD6xJO69VS5?	NV;VfGw2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0O\|E1PjZpPkK0OFcyPDZ4PD;hQi=>
M263	NF2x[phEgXSxdH;4bYNqfHliYYPzZZk>				MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNNlY{KGOnbHzzJIV5eHKnc4PpcochSi2{YX[gWlYxOEVibYX0ZY51NCCLQ{WwJF0hOC5zIN88UU4>	M1TuelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEexOFY3Lz5{NES3NVQ3PjxxYU6=
M321	NFjFZ\|NEgXSxdH;4bYNqfHliYYPzZZk>				MoXwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUVMzOSClZXzsd{BmgHC{ZYPzbY5oKEJvcnHmJHY3ODCHIH31eIFvfCxiSVO1NEA:KDBwMTFOwG0v	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR5MUS2Okc,OjR2N{G0OlY9N2F-
M238	Ml3hR5l1d3SxeHnjbZR6KGG\|c3H5				NXz3Z4wzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVTJ\|ODDj[YxteyCneIDy[ZN{cW6pIFKtdoFnKFZ4MEDFJI12fGGwdDygTWM2OCB;IECuNUDPxE1w	M4jtRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEexOFY3Lz5{NES3NVQ3PjxxYU6=
M262	NUXLPXk{S3m2b4TvfIlkcXS7IHHzd4F6				M3XNTmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG0zPjJiY3XscJMh\XiycnXzd4lv\yCELYLh[kBXPjByRTDteZRidnRuIFnDOVAhRSByLkGg{txONg>?	M4HLdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEexOFY3Lz5{NES3NVQ3PjxxYU6=
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CHL-1	Ml\4RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NYq3dXpQPDhiaILz		MVHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOKTD2xJINmdGy\|IHjhdoJwemmwZzD3bYxlKHS7cHWgRnJCTiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOjBizszNMi=>	M2PlcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NEW4NVM1Lz5{OES1PFE{PDxxYU6=
HCT116	MVjGeY5kfGmxbjDhd5NigQ>?				MUTTeIlufWyjdHnvckBw\iCEUlHGMWNTSUZiZHnt[ZJqgmG2aX;uJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCkeTDseYNq\mW{YYPlJINwdXCuZX3lcpRifGmxbjDhd5NigSxiRVO1NEA:KDBwNkCxJO69VS5?	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV3N{S1PEc,Ojh3NUe0OVg9N2F-
Calu6	MUTGeY5kfGmxbjDhd5NigQ>?	MUizJJVO	MmD1NkBpenN?		MYHBZ5RqfmG2aX;uJI9nKEOUQV[gbY4hcHWvYX6gR4FtfTZiY3XscJMh[XO\|ZYPz[YQh[XNiaX7jdoVie2ViaX6gUWVMKHCqb4PwbI9zgWyjdHnvckBifCB\|IIXNJIFnfGW{IEKgbJJ{KGK7IF\SSXQh[XO\|YYm=	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV3N{S1PEc,Ojh3NUe0OVg9N2F-
Sf9	NVr1RXd{TnWwY4Tpc44h[XO\|YYm=		MojBNUBpeg>?		MX\Jcohq[mm2aX;uJI9nKGi3bXHuJHpCUyBqNTD0c{A{ODlicnXzbYR2\XNrIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVZkmgbY5{\WO2IHPlcIx{KHW\|aX7nJHpCU3SrZHWgZZMhe3Wkc4TyZZRmKGGodHXyJFEhcHJiYomgcYF{eyC\|cHXjeJJwdWW2comsJGlEPTBiPTCwMlAzOyEQvF2u	NIDLN4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEW4OlIyOSd-Mki1PFYzOTF:L3G+
Sf9	MYXGeY5kfGmxbjDhd5NigQ>?		MXyzNEBucW6\|		NXHOUHFoUW6qaXLpeIlwdiCxZjDOMZRmem2rbnHsJGdUXC22YXfn[YQhemWlb33ibY5idnRiaIXtZY4h\nWubD3s[Y5ofGhiWlHLJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6\|ZXP0JINmdGy\|IIXzbY5oKE2EUDDhd{B{fWK\|dILheIUh[W[2ZYKgN\|AhdWmwczDifUBCTFBvR3zvJIF{e2G7LDDJR\|UxKD1iMD6wN\|E1KM7:TT6=	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV6NkKxNUc,Ojh3OE[yNVE9N2F-
UACC-903	MmTJR5l1d3SxeHnjbZR6KGG\|c3H5	MWSyOUB2VQ>?	NECxcZk1QCCqcoO=		M3vWTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHVCS0NvOUCzJINmdGy\|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHH0JFI2KHWPIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XlicnXsZZRqfmVidH:gZ49vfHKxbDygTWM2OCB;IEOuOkDPxE1w	NGi5Z2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGzN\|A{PSd-MkmxN\|MxOzV:L3G+
CHL-1	NHPVNGhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NXvXUGZ5PzJiaILz		MmSxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCFSFytNUBk\WyuczDoZZJjd3Krbnege4lt\CC2eYDlJGJTSUZiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDF\|Lkeg{txONg>?	Mn\vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzM{OwN\|UoRjJ7MUOzNFM2RC:jPh?=
A375	NHHMWW9HfW6ldHnvckBie3OjeR?=		MlTCPVYhcHK\|		NHi5Zm1KdmirYnn0bY9vKG:oIFLSRWYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIFGzO\|Uh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwheHKxbHnm[ZJifGmxbjDpcoN2[mG2ZXSg[o9zKDl4IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkGyO{DPxE1w	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3O{c,Ojl2MEe5O\|c9N2F-
A375	M2q2[2Z2dmO2aX;uJIF{e2G7				NUTGXogzUW6qaXLpeIlwdiCxZjDCVmFHKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDBN\|c2KGOnbHzzJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjDFVmsheGixc4Doc5J6dGG2aX;uJIJ6KEGucHjhV4Nz\WWwIHHzd4F6NCCLQ{WwJF0hOC5yM{Kg{txONg>?	NVvsU4x2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OlE5OjdpPkK5OFYyQDJ5PD;hQi=>
SK-MEL-32	NEPIdoVEgXSxdH;4bYNqfHliYYPzZZk>				Ml3oR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2suVUWOLUOyJINmdGy\|LDDJR\|UxKD1iMD6zNUDPxE1w	NU\WSIZlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OlE5OjdpPkK5OFYyQDJ5PD;hQi=>
WM266.4	Mn36RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NHnqbZk1QCCqcoO=		MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFePMk[2MlQh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygS2k2OCB;IECuNlEh\|ryPLh?=	MnzYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NEC0OlMoRjJ7OUSwOFY{RC:jPh?=
A375	MW\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NXLqeZplPDhiaILz		MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF\|N{WgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiR1m1NEA:KDBwOUWg{txONg>?	NXnxdGFWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFA1PjNpPkK5PVQxPDZ\|PD;hQi=>
HT-29	NVPZOWFISW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NEKxXFI1QCCqcoO=		M2HlVmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygS2k2OCB;IEGuPFgh\|ryPLh?=	Mo\QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NEC0OlMoRjJ7OUSwOFY{RC:jPh?=
WM1361	M4fV[mFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NFzwZVk1QCCqcoO=		MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFePMUO2NUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDHTVUxKD1iMkCuPEDPxE1w	NEXaeos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm0NFQ3Oyd-Mkm5OFA1PjN:L3G+
HCT116	NXPRdZh3SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M3jZb\|Q5KGi{cx?=		MlL5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKQ2SxNVYh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygS2k2OCB;IEK1MlIh\|ryPLh?=	NGDjOY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm0NFQ3Oyd-Mkm5OFA1PjN:L3G+
A673	NV3XS\|BjeUiWUzDhd5NigQ>?				M2PFcZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy\|	Ml3wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
DAOY	MnPLdWhVWyCjc4PhfS=>				NVz1WHNJeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFTBU3kh[2WubIO=	MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
RD	MkLOdWhVWyCjc4PhfS=>				NYTORodyeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGLEJINmdGy\|	M2XPelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH	MkX2dWhVWyCjc4PhfS=>				MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?=	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
MG 63 (6-TG R)	NGX3bYVyUFSVIHHzd4F6				M4LWW5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?=	NVrPXo1nRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643	MUPxTHRUKGG\|c3H5				M{O3V5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO=	NVvDS3dlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50	MXfxTHRUKGG\|c3H5				MWnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy\|	MoPkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
A673	NXXRbppQeUiWUzDhd5NigQ>?				MVvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDBOlc{KGOnbHzzLS=>	M1PnR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS	MX3xTHRUKGG\|c3H5				NUfXT\|ZFeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXS1{IF;TJINmdGy\|	M4HZ[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41	NFPpfYpyUFSVIHHzd4F6				NGXS[4VyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDRzIHPlcIx{	M3H4OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2	NF22cGJyUFSVIHHzd4F6				MljGdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO=	M1e3O\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC	NXi3T4l6eUiWUzDhd5NigQ>?				NHnwOlFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=>	M4XRcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5	M170fZFJXFNiYYPzZZk>				MWPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN?	NHqwZXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
SK-N-MC	NI\jO3NyUFSVIHHzd4F6				M3jES5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN?	NUPvN25sRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32	MXTxTHRUKGG\|c3H5				MmTidWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWGM{OiClZXzsdy=>	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-ERK / p-CRAF; PubMed: 22448344 Cancer Discov BRAF mutant cell lines from (A) were treated with 3µM vemurafenib for the indicated times, and lysates were probed with the indicated antibodies. p-MEK(S217/221) / pAKT(T308) / p-AKT(S473) / p-P70 S6K(T389) / p-S6(Ser235-236) / P-4EB-P1; PubMed: 22194965 PLoS One Western blot analysis of phosphorylated and the total amount of key proteins in the MAPK and PI3K/AKT pathways after 24 hours of exposure to the solvent (DMSO), or various concentrations of the BRAF inhibitor vemurafenib. The vemurafenib-sensitive M238 and M229 cell lines and the vemurafenib in vitro acquired resistant sublines M238-AR2 and M229-AR9 were cultured at different concentrations of vemurafenib. p70 and p-p70 S6K in this figure are referred to S6K1 and phosphorylated form of S6K1, respectively. Bax / Bcl2 / Bcl-xl / BIM / Mcl1; PubMed: 28382170 Theranostics Change of Bcl-2 family proteins following Vemurafenib treatment for 24 h.	22448344 22194965 28382170
Growth inhibition assay	Cell viability; PubMed: 29179510 Oncotarget At different time point of the experiment (expressed in days), sensitivity to vemurafenib was evaluated in the different A375 cell lines. Cells were treated with 10-fold dilution series (1 nM to 10 uM) of Vemurafenib and cell viability was assessed after 72 h by Crystal violet staining. Cell viability results are expressed in fold vs. the untreated cells.	29179510
Immunofluorescence	uPAR / α5-β1; PubMed: 30611716 EBioMedicine Representative images of confocal microscopy of companion M6R treated cultures stained with specific anti-uPAR (red), α5β1 (green) and DAPI (blue). Experiments have been performed three times in triplicate with analogous results. The co-localization score is quantified by image J andreported within each picture as Manders' coefficient (MC). The shown pictures are representative of 20 different pictures for each experimental condition. Scale bar = 20 μm. p-Akt(Thr308); PubMed: 27293997 Am J Cancer Res Vemurafenib reduced phosphorylated Akt in HUVEC. Cells were treated with vemurafenib for 4 h and processed for immunofluorescence staining with antibodies against p-AktThr308. Cell nuclei were stained with DAPI. Scale bar represents 50 μm.	30611716 27293997

体内研究

PLX4032按6 mg/kg-20 mg/kg 剂量作用于B-RAF^V600E-突变鼠移植瘤模型，抑制肿瘤生长。^[1] PLX4032按12.5 mg/kg-100 mg/kg剂量作用于携带LOX, Colo829, 和A375移植瘤小鼠，抑制肿瘤生长，延长小鼠寿命。^[2]

激酶实验： ^[1]	- 合并 RAF激酶活性测定: 通过测量生物素化的BAD蛋白磷酸化而测定野生型RAF和突变型的激酶活性。在20 mM Hepes (pH 7.0), 10 mM MgCl₂, 1 mM DTT, 0.01% (v/v) Tween-20, 50 nM 生物素-BAD 蛋白，和 1 mM ATP 的混合物中室温下进行反应。加入5 μL 含20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, 0.3% (w/v) 牛血清蛋白 (BSA)的溶液，5分钟后，反应终止。终止溶液也包含p-BAD (Ser112) 抗体,链霉亲和素包被的供体小珠，蛋白A 受体小珠。抗体和小珠在终止溶液中黑暗环境下室温预温育30分钟。最终抗体被稀释2000倍，每个小珠的终浓度为10 μg/mL。重复做三次单独纯化蛋白实验，去不同两批的平均值作为突变活性。
细胞实验： ^[2]	- 合并 Cell lines: MALME-3M, Colo829, Colo38, A375, SK-MEL28, 和 A2058 细胞 Concentrations: 0–10 μM , 溶于 DMSO Incubation Time: 5 天 Method: 通过MTT 实验测评细胞增殖。细胞按每孔1000到5000个接种在96孔板上，体积为180 μL。PLX4032按最终实验浓度的10倍储备在含1% DMSO的培养基中。细胞接种24小时后, 加入20 μL适当稀释的PLX4032。接种6天后，进行增殖实验。计算抑制百分数，根据抑制百分数与浓度的对数的回归分析测定IC50值。 (Only for Reference)
动物实验： ^[2]	- 合并 Animal Models: 携带LOX, Colo829, 和A375移植瘤细胞的无胸腺裸鼠 Dosages: 12.5 mg/kg–100 mg/kg Administration: 口服饲喂，每天两次 (Only for Reference)

参考文献

- 合并

溶解度 (25°C)

体外	DMSO	97 mg/mL (197.99 mM)
	Water	Insoluble
	Ethanol	Insoluble
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 4% DMSO+30% PEG 300+5% Tween 80+61% ddH2O	1.25mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Vemurafenib (PLX4032) SDF

分子量	489.92
化学式	C₂₃H₁₈ClF₂N₃O₃S
CAS号	918504-65-1
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	RG7204, RO5185426

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-09-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03410875	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
NCT02427893	Withdrawn	Drug: Cobimetinib\|Drug: Vemurafenib	Melanoma	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins\|Genentech Inc.	August 2015	Phase 3

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

常见问题及建议解决方法

问题 1：
How about the half-life of Vemurafenib(S1267)?
回答：
It was reported that the half-life of the compound is 57 hours.
问题 2：
The vemurafenib power, when prepared in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O solutions, form a pellet down the tube?
回答：
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.

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

选择性强的Raf抑制剂

SB590885 : B-Raf-selective, K_i=0.16 nM.
选择性强的Raf抑制剂

ZM 336372 : C-Raf-selective, IC50=70 nM.
FDA批准的Raf抑制剂

Sorafenib Tosylate : Approved by FDA for advanced renal cancer.
最新的Raf抑制剂

TAK-632 ^New : Potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf, respectively, showing less or no inhibition against other tested kinases.

研究领域

产品类型

定制您的化合物库

Vemurafenib (PLX4032)

客户使用Selleck生产的Vemurafenib (PLX4032)发表文献516篇：

产品安全说明书

Raf抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Vemurafenib (PLX4032) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-09-06)

技术支持

常见问题及建议解决方法

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

相关Raf产品