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477篇：

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PubMed: 22675422 ( click the link to review the publication )

PLoS One, 2012, 7(12):e52760

PubMed: 23285177 ( click the link to review the publication )

PLoS One, 2012, 7(10):e47696

PubMed: 23110092 ( click the link to review the publication )

J Invest Dermatol, 2011, 131(10):2087-95

PubMed: 21753785 ( click the link to review the publication )

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	MmHUSpVv[3Srb36gRZN{[Xl?	Mk[5OkDPxE1?	MUO0PEBp	NF;QdGRFVVOR	MojvWJJq\2encoOgSXIhe3S{ZYPz	M{HmblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|M{[yNlQxLz5{M{O2NlI1ODxxYU6=
VMM12	NEPiZmtHfW6ldHnvckBCe3OjeR?=	MlTRN{DPxE1?	M1PGZ\|Q5KGh?	MojXSG1UVw>?	NVLFSY5jUW6lcnXhd4V{KGOxbHzh[4VvKHO7boTo[ZNqeyCjbnSg[IVkemWjc3XzJGlNNTliZYjwdoV{e2mxbh?=	NXPqfFVXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5PFk2ODZpPkK1PVg6PTB4PD;hQi=>
C4	NGL3ZZlHfW6ldHnvckBCe3OjeR?=	NWX4Rlk3OyEQvF2=	NXz1bphoPDhiaB?=	MnLuSG1UVw>?	NXjYSJdJUW6lcnXhd4V{KGOxbHzh[4VvKHO7boTo[ZNqeyCjbnSg[IVkemWjc3XzJGlNNThiZYjwdoV{e2mxbh?=	MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl6OUWwOkc,OjV7OEm1NFY9N2F-
Calu-6	MVTGeY5kfGmxbjDBd5NigQ>?	MW[x5qCK\|ryP	MmnoNUBp	NWn1XFFCTE2VTx?=	NHTOfnVC[3SrdnH0[ZMhVUWNL1XST{BqdiClZXzsd{B4cXSqIIfpcIQufHmyZTDCVmFH	Mmf3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjBzN{m3NFUoRjJyMUe5O\|A2RC:jPh?=
PC	M13MXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NG\u[oI6PiCq		MmT5SWM2OD5iMUCwNEBvVQ>?	MmfxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6OEC3PVIoRjF7OEiwO\|kzRC:jPh?=
TPC-1 (RET/PTC1)	M2DIbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NFz3cVk6PiCq		M3rP[GVEPTEkibWxNFAxKG6P	M2TWVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEiwO\|kzLz5zOUi4NFc6OjxxYU6=
CAL62 (KRAS G12R) > 1000 > 1000	M3ntemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MWO5OkBp		MXrFR\|UxRiBzMECwJI5O	NIn2PXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi4NFc6Oid-MUm4PFA4QTJ:L3G+
HTH7 (NRAS Q61R)	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NXfFR\|NrQTZiaB?=		NYfMR5hyTUN3MPMJqUAyODByIH7N	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh6MEe5Nkc,OTl6OEC3PVI9N2F-
C643 (HRAS G13R)≥ 500	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MmfQPVYhcA>?		M2LGXmVEPTBi4polJFUxOCCwTR?=	M{HMUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEiwO\|kzLz5zOUi4NFc6OjxxYU6=
BCPAP (BRAF WT/V600E)	NU\jUVR6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NHHYSYo6PiCq		MojhSWM2OD15ODDuUS=>	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh6MEe5Nkc,OTl6OEC3PVI9N2F-
BHT101 (BRAF WT/V600E)	NFG3OFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MlPDPVYhcA>?		MW\FR\|UxRTl5IH7N	Ml33QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6OEC3PVIoRjF7OEiwO\|kzRC:jPh?=
SW1736 (BRAF WT/V600E)	NF\ScY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NE\WbWs6PiCq		NF7mTVBGSzVyPUK5JI5O	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh6MEe5Nkc,OTl6OEC3PVI9N2F-
8505C (BRAF V600E/V600E)	Mo\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		Mn\IPVYhcA>?		NVfpZZJyTUN3ME21O{BvVQ>?	Mnq1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6OEC3PVIoRjF7OEiwO\|kzRC:jPh?=
ARO	NXv1cYFUTnWwY4Tpc44hSXO\|YYm=	NF\JO3cyOCEQvF2=	MVm3NkBp	M4G1eWROW09?	NXTv[II{UW6mdXPld{B1cGVicnXlfJBz\XO\|aX;uJI9nKHSqZTDOTXMheHWvcB?=	NX;rV4FFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi0OVgxPTNpPkG4OFU5ODV\|PD;hQi=>
A375	MnfGRZBweHSxc3nzJGF{e2G7	MU[xNEDPxE1?		MkX6SG1UVw>?	NV;1VYNHWHKxbX;0[ZMh[XCxcITveIlkKGSnYYTo	NXS1VpZDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi0OVgxPTNpPkG4OFU5ODV\|PD;hQi=>
TPCI	NVfkNo5vT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mn7oNVAxKM7:TR?=	NV7mTZdCQTZiaB?=	NIfpT5hFVVOR	NHq1epVKSzVyPUGwMlc4KM7:TR?=	NWPDOoVMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi0OVgxPTNpPkG4OFU5ODV\|PD;hQi=>
ARO	NFXsWJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Ml7uNVAxKM7:TR?=	Mo\HPVYhcA>?	NV7QXotITE2VTx?=	NIXo[4pKSzVyPUKwOUBvVQ>?	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDR3OEC1N{c,OTh2NUiwOVM9N2F-
NPA	M3LKXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYSxNFAh\|ryP	M1;FVFk3KGh?	MmPISG1UVw>?	M{m2e2lEPTB;Mk[gcm0>	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDR3OEC1N{c,OTh2NUiwOVM9N2F-
A375	M1uzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlnrNVAxKM7:TR?=	NF[3cHo6PiCq	M3O5R2ROW09?	MnvTTWM2OD12NzDuUS=>	M1P1WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEW4NFU{Lz5zOES1PFA2OzxxYU6=
UKF-NB-3 (ABCB1)	M1vlN2Z2dmO2aX;uJGF{e2G7	Moq5NU4zPSEEtV2=	MUmyJIg>	NVP2WIpvTE2VTx?=	MnLaSY5p[W6lZYOgZYNkfW23bHH0bY9vKG:oIITo[UBndHWxcnXzZ4VvfCCDQlPCNUB{fWK\|dILheIUhemixZHHtbY5mKDF{Mx?=	M4CzelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{O1O\|Y3Lz5{NEezOVc3PjxxYU6=
UKF-NB-3	M4[4T2Z2dmO2aX;uJGF{e2G7	NFXEfIEyNjJ3INM1US=>	NVTPSFY{OiCq	NUOwUHdwTE2VTx?=	NFX3e3FUcWewaX\pZ4FvfGy7IHHm[oVkfHNib36gZYNkfW23bHH0bY9vKG:oIITo[UBndHWxcnXzZ4VvfCCDQlPCNUB{fWK\|dILheIUhemixZHHtbY5mKDF{Mx?=	M1nH[\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{O1O\|Y3Lz5{NEezOVc3PjxxYU6=
A375 (BRAFV600E)	Mlv6SpVv[3Srb36gRZN{[Xl?		NGnmTm05KGh?	M3vSZmROW09?	MmrnTY5kemWjc3XzJIlvfHKjY3XscJVt[XJiUl;TJIFv\CCQTzDs[ZZmdHN?	MmHYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV\|NkO2OFQoRjJ3M{[zOlQ1RC:jPh?=
A375P	MmLLRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?				MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF\|N{XQJINmdGy\|LDDJR\|UxKD1iMD6yOVQh\|ryPLh?=	NFPT[5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS2NFA{OCd-MkK0OlAxOzB:L3G+
A375	NIHW[JlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=				MlW1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCDM{e1JINmdGy\|IHX4dJJme3OrbnegRk1T[WZiVk[wNGUhdXW2YX70JIFv\CC5aXzkJJR6eGViUnHzMEBKSzVyIE2gNE4{OSEQvF2u	M{H6fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OEC4PVEyLz5{MkiwPFkyOTxxYU6=
A375P	MoPZRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NXq1S4Y2PDhiaILz		M3[5T2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OXAh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNlUh\|ryPLh?=	Mof0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzMki0NVAoRjJ2MUK4OFExRC:jPh?=
A375	NE\CdHREgXSxdH;4bYNqfHliYYPzZZk>		NX3aNnZ4PzJiaILz		NIW5cIpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjF6IN88UU4>	NEHDfms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKxOVgyQCd-MkSyNVU5OTh:L3G+
SK-MEL-28	MkS2R5l1d3SxeHnjbZR6KGG\|c3H5				NXWzVVJjS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTVXMMVI5KGOnbHzzJIV5eHKnc4PpcochSi2{YX[gWlYxOEVibYX0ZY51NCCLQ{WwJF0hOC5zIN88UU4>	M17KR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEexOFY3Lz5{NES3NVQ3PjxxYU6=
M229	M{e0VGN6fG:2b4jpZ4l1gSCjc4PhfS=>				NHzxTFNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOOjJ7IHPlcIx{KGW6cILld5NqdmdiQj3yZYYhXjZyMFWgcZV1[W62LDDJR\|UxKD1iMD6xJO69VS5?	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR5MUS2Okc,OjR2N{G0OlY9N2F-
M263	NE\2S2pEgXSxdH;4bYNqfHliYYPzZZk>				NF\IUWpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOOjZ\|IHPlcIx{KGW6cILld5NqdmdiQj3yZYYhXjZyMFWgcZV1[W62LDDJR\|UxKD1iMD6xJO69VS5?	MnPSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{G0OlYoRjJ2NEexOFY3RC:jPh?=
M321	M3nsRmN6fG:2b4jpZ4l1gSCjc4PhfS=>				NF3sRo9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOOzJzIHPlcIx{KGW6cILld5NqdmdiQj3yZYYhXjZyMFWgcZV1[W62LDDJR\|UxKD1iMD6xJO69VS5?	M3PSTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEexOFY3Lz5{NES3NVQ3PjxxYU6=
M238	MV\DfZRwfG:6aXPpeJkh[XO\|YYm=				MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNNlM5KGOnbHzzJIV5eHKnc4PpcochSi2{YX[gWlYxOEVibYX0ZY51NCCLQ{WwJF0hOC5zIN88UU4>	NG\CZng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES3NVQ3Pid-MkS0O\|E1PjZ:L3G+
M262	NECwT3JEgXSxdH;4bYNqfHliYYPzZZk>				M1vNO2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG0zPjJiY3XscJMh\XiycnXzd4lv\yCELYLh[kBXPjByRTDteZRidnRuIFnDOVAhRSByLkGg{txONg>?	MnTNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{G0OlYoRjJ2NEexOFY3RC:jPh?=
M249	NVjESYdOS3m2b4TvfIlkcXS7IHHzd4F6				Moj1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUVI1QSClZXzsd{BmgHC{ZYPzbY5oKEJvcnHmJHY3ODCHIH31eIFvfCxiSVO1NEA:KDBwMTFOwG0v	Ml3GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{G0OlYoRjJ2NEexOFY3RC:jPh?=
M14	NVzVWmFyS3m2b4TvfIlkcXS7IHHzd4F6				NXTO[G13S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVTF2IHPlcIx{KGW6cILld5NqdmdiTmLBV{BIOTKFIH31eIFvfCxiSVO1NEA:KDBwMUWg{txONg>?	NEDiWHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES3NVQ3Pid-MkS0O\|E1PjZ:L3G+
SK-MEL-28	MlS1RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NWLNNI95PjhiaILz		NYC0WpB7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiaHHyZo9zcW6pIFLSRWYhXjZyMFWgcZV1[W62IHHmeIVzKDZ6IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkS4JO69VS5?	NWnmSWRVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PFgxPzNpPkK0OVg5ODd\|PD;hQi=>
insect cell	M4DWeWZ2dmO2aX;uJIF{e2G7		MXO2NEBucW6\|		M2nNOWlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigbJVu[W5iQj3SZYYhXjZyMFWgcZV1[W62IHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCrboPlZ5Qh[2WubIOgZZN{\XO\|ZXSgZZMhY2ejbX3hMVM{WF2rbnPvdpBwemG2aX;uJIlvfG9iTVXLJIFnfGW{IE[wJI1qdnNiYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NEA:KDBwMEOxJO69VS5?	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEOxOUc,OjR7MECzNVU9N2F-
MALME-3M	NYrSVWdFTnWwY4Tpc44h[XO\|YYm=		NEnEeYYyKGi{		NG\uR4hKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdD3t[YRq[XSnZDDFdosheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1CVE2HLUPNJINmdGy\|IHHmeIVzKDFiaIKgZpkh\my3b4Lld4NmdmOnIHHuZYx6e2m\|LDDJR\|UxKD1iMD6wOlEh\|ryPLh?=	M1nHSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwN\|E2Lz5{NEmwNFMyPTxxYU6=
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HepG2	NEL4bJNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NV\BUph7PzJiaILz		M1jN[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCudX3pcoV{[2WwY3WgZZN{[XluIFnDOVAhRSB3LkS4JO69VS5?	MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ2MkW1N{c,Ojh{NEK1OVM9N2F-
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UACC-903	NVLKSWw2SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M3rOZVczKGi{cx?=		MoDyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCXQVPDMVkxOyClZXzsd{Bp[XKkb4LpcochSlKDRjDWOlAxTSCvdYThcpQh[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFIvPyEQvF2u	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR3OEGzOEc,Ojh2NUixN\|Q9N2F-
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UACC-903	M1X6W2FvfGmycn;sbYZmemG2aY\lJIF{e2G7		NFXYUnM1QCCqcoO=		MnnhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCXQVPDMVkxOyClZXzsd{Bp[XKkb4LpcochSlKDRjDWOlAxTSCvdYThcpQh[W[2ZYKgOFghcHK\|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFEzNjNizszNMi=>	NELYbWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OES1PFE{PCd-Mki0OVgyOzR:L3G+
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UACC-903	M2DGXWN6fG:2b4jpZ4l1gSCjc4PhfS=>	NEDCTIEzPSC3TR?=	MVO0PEBpenN?		M2WxVGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHVCS0NvOUCzJINmdGy\|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHH0JFI2KHWPIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XlicnXsZZRqfmVidH:gZ49vfHKxbDygTWM2OCB;IEOuOkDPxE1w	NXf4SW1xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxN\|MxOzVpPkK5NVM{ODN3PD;hQi=>
CHL-1	NFzFT5NCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NWGwS\|hWPzJiaILz		NG\TVpBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPIUE0yKGOnbHzzJIhiemKxcnnu[{B4cWymIIT5dIUhSlKDRjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR\|UxKD1iMUOuO{DPxE1w	Mn7QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzM{OwN\|UoRjJ7MUOzNFM2RC:jPh?=
A375	NEi0eWtHfW6ldHnvckBie3OjeR?=		MY[5OkBpenN?		NHu0ZXFKdmirYnn0bY9vKG:oIFLSRWYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIFGzO\|Uh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwheHKxbHnm[ZJifGmxbjDpcoN2[mG2ZXSg[o9zKDl4IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkGyO{DPxE1w	Mk\EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2MEe5O\|coRjJ7NEC3PVc4RC:jPh?=
A375	M1y1dGZ2dmO2aX;uJIF{e2G7				NVLUZml6UW6qaXLpeIlwdiCxZjDCVmFHKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDBN\|c2KGOnbHzzJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjDFVmsheGixc4Doc5J6dGG2aX;uJIJ6KEGucHjhV4Nz\WWwIHHzd4F6NCCLQ{WwJF0hOC5yM{Kg{txONg>?	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR4MUiyO{c,Ojl2NkG4Nlc9N2F-
SK-MEL-32	Mo\zR5l1d3SxeHnjbZR6KGG\|c3H5				MmrmR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2suVUWOLUOyJINmdGy\|LDDJR\|UxKD1iMD6zNUDPxE1w	NUCxS5p2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OlE5OjdpPkK5OFYyQDJ5PD;hQi=>
WM266.4	NVHmbWN3SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MVm0PEBpenN?		M2TOPGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iV12yOlYvPCClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG\|c3H5MEBIUTVyIE2gNE4zOSEQvF2u	NYXNZVlxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFA1PjNpPkK5PVQxPDZ\|PD;hQi=>
A375	MXnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		M2XHTVQ5KGi{cx?=		NIe4fGpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO\|Uh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygS2k2OCB;IECuPVUh\|ryPLh?=	NWTNNolIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFA1PjNpPkK5PVQxPDZ\|PD;hQi=>
HT-29	NWO5UHczSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M{HoVlQ5KGi{cx?=		MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy\|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFfJOVAhRSBzLki4JO69VS5?	MlPYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NEC0OlMoRjJ7OUSwOFY{RC:jPh?=
WM1361	MnnFRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MmrhOFghcHK\|		NHnaRXlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGfNNVM3OSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG\|c3H5MEBIUTVyIE2gNlAvQCEQvF2u	MnrzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NEC0OlMoRjJ7OUSwOFY{RC:jPh?=
HCT116	M3TG[mFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NXy4RYJPPDhiaILz		NU[3VXFwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOFghcHK\|IHL5JG1VXCCjc4PhfUwhT0l3MDC9JFI2NjJizszNMi=>	MkXEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NEC0OlMoRjJ7OUSwOFY{RC:jPh?=
A673	NG\GV5hyUFSVIHHzd4F6				MlPKdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN?	NV3EfYxyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
DAOY	M1TZWZFJXFNiYYPzZZk>				MX7xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhTEGRWTDj[Yxtew>?	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
RD	NETpUY9yUFSVIHHzd4F6				MUnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM>	MnHEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH	M3O3R5FJXFNiYYPzZZk>				NVj0R4l{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM>	MnfJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R)	NFe1NVRyUFSVIHHzd4F6				MlTzdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy\|	NFjGO3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
NB1643	NGDBZpVyUFSVIHHzd4F6				MVfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy\|	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
OHS-50	NGTmV5FyUFSVIHHzd4F6				MYjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy\|	NH\DcI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
A673	MVfxTHRUKGG\|c3H5				NULBdFZweUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl?	NFfUN2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
U-2 OS	M3fQ[pFJXFNiYYPzZZk>				NHvLdZRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBWNTJiT2OgZ4VtdHN?	MoXIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Rh41	NVPDUWp4eUiWUzDhd5NigQ>?				Mkf2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVog1OSClZXzsdy=>	MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SJ-GBM2	M1rYPJFJXFNiYYPzZZk>				MnvqdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO=	MlHQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC	NIP4UYVyUFSVIHHzd4F6				M{PuPZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz	MkfaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
LAN-5	MXvxTHRUKGG\|c3H5				MkTsdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy\|	M1zaV\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC	MW\xTHRUKGG\|c3H5				NVPtUXJieUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	NXHndWpsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32	NV7FSYNieUiWUzDhd5NigQ>?				Mm\JdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWGM{OiClZXzsdy=>	MmXYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=

... 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、MSDS / 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、MSDS / 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 2021-01-06)

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477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 2021-01-06)

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