Vemurafenib (PLX4032, RG7204)

目录号:S1267 别名: RO5185426

Vemurafenib (PLX4032, RG7204) Chemical Structure

Molecular Weight(MW): 489.92

Vemurafenib (PLX4032, RG7204)是一种新型有效的B-RafV600E抑制剂,IC50为31 nM。Vemurafenib对B-RafV600E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。

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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 Vemurafenib (PLX4032, RG7204)是一种新型有效的B-RafV600E抑制剂,IC50为31 nM。Vemurafenib对B-RafV600E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。
特性 PLX4032是新型有效的B-RAFV600E 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)
18 nM 19 nM 31 nM 48 nM 51 nM
体外研究

PLX4032抑制B-RAFV600E, 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-RAFV600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-RAFV600E。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
A375 Ml;KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUGxNFAh|ryP M1rGcVk3KGh? NUTu[3pITE2VTx?= MYTJR|UxRTR5IH7N MWqxPFQ2QDB3Mx?=
ARO MkT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHZNVAxKM7:TR?= NInxXHM6PiCq M2LGVGROW09? MoDwTWM2OD1{MEWgcm0> MnLrNVg1PThyNUO=
NPA M{LGeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\VbXgyODBizszN NV;MSGc5QTZiaB?= NVO1TZFbTE2VTx?= NXOzVmd1UUN3ME2yOkBvVQ>? NF7nNZYyQDR3OEC1Ny=>
TPCI NVTLXY5OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUexNFAh|ryP NUXZV3VPQTZiaB?= Mny5SG1UVw>? M2qycmlEPTB;MUCuO|ch|ryP M1Hrc|E5PDV6MEWz
A375 MWnBdI9xfG:|aYOgRZN{[Xl? M3XwOFExKM7:TR?= NGHRcI1FVVOR MWfQdo9ud3SnczDhdI9xfG:2aXOg[IVifGh? NXjGR3k5OTh2NUiwOVM>
ARO NIXqPWFHfW6ldHnvckBCe3OjeR?= M1jDblExKM7:TR?= MWm3NkBp MlXVSG1UVw>? M1fMWWlv\HWlZYOgeIhmKHKnZYjwdoV{e2mxbjDv[kB1cGViTlnTJJB2dXB? MVGxPFQ2QDB3Mx?=
8505C (BRAF V600E/V600E) MmTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHGSZZKQTZiaB?= M4PubGlEPTB;NUegcm0h M4HsRlIxOTR7MUO2
SW1736 (BRAF WT/V600E) NHXkVWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PuU|k3KGh? NIK5XIdKSzVyPUK5JI5O M1fsXlIxOTR7MUO2
BHT101 (BRAF WT/V600E) MnvjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWq5OkBp M2\WcmlEPTB;OUegcm0> NVH5blU6OjBzNEmxN|Y>
BCPAP (BRAF WT/V600E) MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnVPVYhcA>? MVnJR|UxRTd6IH7N MVyyNFE1QTF|Nh?=
C643 (HRAS G13R)≥ 500 NVjYN4NLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\0PVYhcA>? Mn71TWM2OCEkibWgOVAxKG6P MWOyNFE1QTF|Nh?=
HTH7 (NRAS Q61R) MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVS5OkBp MXvJR|Ux6onnIEGwNFAhdk1? M1jjd|IxOTR7MUO2
CAL62 (KRAS G12R) > 1000 > 1000 MoDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHiy[pI6PiCq MWDJR|UxRiBzMECwJI5O MX2yNFE1QTF|Nh?=
TPC-1 (RET/PTC1) NV3UVndTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TTSVk3KGh? MnXTTWM2OOLLpUGwNFAhdk1? NGrRXogzODF2OUGzOi=>
PC NVHsWJRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYe5OkBp NE\2dZNKSzVyPjCxNFAxKG6P MWWyNFE1QTF|Nh?=
Calu-6 MlTmSpVv[3Srb36gRZN{[Xl? M3j6WVHjiIoQvF2= MofZNUBp M2n6WWROW09? MWLBZ5RqfmG2ZYOgUWVMN0WUSzDpckBk\WyuczD3bZRpKHerbHSteJlx\SCEUlHG NX60Z|R[OjBzN{m3NFU>
C4 NYTBXJl[TnWwY4Tpc44hSXO|YYm= MmLIN{DPxE1? NYTNOGJPPDhiaB?= NV\MeYJPTE2VTx?= NEXwOmVKdmO{ZXHz[ZMh[2:ubHHn[Y4he3mwdHjld4l{KGGwZDDk[YNz\WG|ZYOgTWwuQCCneIDy[ZN{cW:w MUOyOVk5QTVyNh?=
VMM12 NFKxS4tHfW6ldHnvckBCe3OjeR?= NGW3fYI{KM7:TR?= MUG0PEBp NHT1XY1FVVOR M1:5dGlv[3KnYYPld{Bkd2yuYXflckB{gW62aHXzbZMh[W6mIHTlZ5Jm[XOnczDJUE06KGW6cILld5Nqd25? M1TI[lI2QTh7NUC2
SKMEL19 M1z0NWZ2dmO2aX;uJGF{e2G7 MnWwOkDPxE1? M1fOfFQ5KGh? NFTQe2xFVVOR M2TuTnRzcWepZYLzJGVTKHO2cnXzdy=> MWmyN|M3OjJ2MB?=
UKF-NB-3 (ABCB1) M1XCbGZ2dmO2aX;uJGF{e2G7 MljXNU4zPSEEtV2= NH[4[WczKGh? NFLsRoZFVVOR MlLvSY5p[W6lZYOgZYNkfW23bHH0bY9vKG:oIITo[UBndHWxcnXzZ4VvfCCDQlPCNUB{fWK|dILheIUhemixZHHtbY5mKDF{Mx?= NI\hbo8zPDd|NUe2Oi=>
UKF-NB-3 NEDZVnhHfW6ldHnvckBCe3OjeR?= M1fFeFEvOjViwsXN NVX1XVE3OiCq NUPieFZGTE2VTx?= MlPOV4lodmmoaXPhcpRtgSCjZn\lZ5R{KG:wIHHjZ5VufWyjdHnvckBw\iC2aHWg[ox2d3Knc3PlcpQhSUKFQkGgd5Vje3S{YYTlJJJpd2SjbXnu[UAyOjN? MoPKNlQ4OzV5Nk[=
A375 (BRAFV600E) NUD2ZWZ3TnWwY4Tpc44hSXO|YYm= NXjGTIwzQCCq MVjEUXNQ NH7FOGZKdmO{ZXHz[ZMhcW62cnHj[YxtfWyjcjDSU3Mh[W6mIF7PJIxmfmWuczC= NGHMR4szPTN4M{[0OC=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-ERK / p-CRAF; 

PubMed: 22448344     


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     


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     


Change of Bcl-2 family proteins following Vemurafenib treatment for 24 h.

22448344 22194965 28382170
Growth inhibition assay
Cell viability; 

PubMed: 29179510     


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     


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     


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-RAFV600E-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]

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)

激酶实验:

[1]

+ 展开

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]

+ 展开
  • 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]

+ 展开
  • Animal Models: 携带LOX, Colo829, 和A375移植瘤细胞的无胸腺裸鼠
  • Formulation: 配制成微沉淀散粉 (MBP), 按指定浓度悬浮在含2% Klucel LF的水溶液中,然后使用HCl调节pH为4
  • Dosages: 12.5 mg/kg–100 mg/kg
  • Administration: 口服饲喂,每天两次
    (Only for Reference)

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+ddH2O (suspension)
5mg/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

分子量 489.92
化学式

C23H18ClF2N3O3S

CAS号 918504-65-1
稳定性 powder
in solvent
别名 RO5185426

计算器

摩尔浓度计算器

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 (g) = 浓度 (mol/L) x 体积 (L) 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

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

  • 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

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03878524 Not yet recruiting Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation March 14 2019 Phase 1
NCT03878524 Not yet recruiting Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation March 14 2019 Phase 1
NCT03625141 Recruiting Metastatic Melanoma Hoffmann-La Roche December 13 2018 Phase 2
NCT03625141 Recruiting Metastatic Melanoma Hoffmann-La Roche December 13 2018 Phase 2
NCT03727763 Recruiting Colorectal Cancer Shanghai Changzheng Hospital October 8 2018 Phase 2
NCT03727763 Recruiting Colorectal Cancer Shanghai Changzheng Hospital October 8 2018 Phase 2

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID