VS-5584 (SB2343)

For research use only. Not for use in humans.

目录号:S7016

VS-5584 (SB2343) Chemical Structure

CAS No. 1246560-33-7

VS-5584 (SB2343)是一种有效的,选择性,PI3K/mTOR双重抑制剂,抑制mTORPI3Kα/β/δ/γIC50分别为3.4 nM和2.6-21 nM。Phase 1。

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客户使用Selleck生产的VS-5584 (SB2343)发表文献11篇:

客户使用该产品的5个实验数据:

  • Effect of VS-5584 on platelet adhesion. A-F: WP (A, B) and PRP (D, E) were treated with DMSO as vehicle (A, D; n = 3) or with 20 nM (B; n = 3) and 20 μM (E; n = 3) of VS-5584 and seeded on siliconized coverslips for the quantitative analysis of WP (C) and PRP adhesion (F). Scale bars: A, B, D, E = 50 μm; Data are given in % of vehicle. Mean ± SEM. *p < 0.05 vs. vehicle. G, H: Representative images of WP treated with vehicle (G) or 20 nM of VS-5584 (H). The number of non-spread cells (arrows) is higher in VS-5584-treated WP. Scale bars: 20 μm. I: Quantification of spread platelets based on their morphology. Data are given in % of vehicle. Mean ± SEM. *p < 0.05 vs. vehicle.

    Platelets, 2017, 29(3):277-287. VS-5584 (SB2343) purchased from Selleck.

    HCT116 cells were treated with Go 6983 (0.75 μM) or VS-5584 (0.6 μM) alone or in combination with cobimetinib (0.15 μM) for 48 h. Then, cell viability was evaluated by MTT.

    Cell Physiol Biochem, 2018, 47(2):680-693. VS-5584 (SB2343) purchased from Selleck.

  • Effects of either VS-5584 or ATO alone and their combination on inhibition of PI3K/Akt/mTOR pathway. (A) Western blot analysis for phosphorylation levels of two downstream components of the PI3K/Akt/mTOR network. NALM-6 cells were treated with 10 μM VS-5584 or 0.2 μM ATO alone and their co-treatment for 60 h. Cell-lysates were prepared, SDS–PAGE and western blot analysis were carried out using p-IκBα and p-S6 specific Abs. Actin serves as loading control. One representative of three independent experiments is shown. (B) qRTPCR analysis for evaluation the effects of VS-5584 and ATO and their combination on expression of Akt downstream target genes. NALM-6 cells were treated with 10 μM VS-5584 and 0.2 μM ATO alone and in combination for 60 h. RNA extraction and cDNA synthesis were carried out, expression of indicated genes measured using quantitative RT–PCR and normalized to the expression of β-actin mRNA. The results are expressed as mean ± SD of at least three independent experiments (*p < 0.05, **p < 0.01, ***p < 0.001. p values in single agent treatment groups are calculated compared to control and in combined group compared to ATO).

    Biomed Pharmacother, 2018, 428-437. VS-5584 (SB2343) purchased from Selleck.

    VS-5584 inhibits melanoma cell survival and proliferation-Established melanoma cell lines (A375, A-2058 and SK-MEL-3), patient-derived primary melanoma cells, B10BR melanocytes and primary human keratinocytes (“Kera”) were treated with applied concentration of VS-5585 (“VS”) or vehicle control (“C”, 0.1% of DMSO), cell survival was tested by MTT assay (A, E and F) and trypan blue exclusion assay (B, for A375 cells); Cell proliferation was analyzed by through [H3] Thymidine incorporation assay (C, for A375 cells) and clonogenicity assay (D, for A375 cells). Data were expressed as mean ± SD, experiments were repeated three times. *p<0.05 vs group “C”.

    PLoS One, 2015, 10(7):e0132655.. VS-5584 (SB2343) purchased from Selleck.

  • Effect of VS-5584 on platelet viability. A, B: WP (A) and PRP (B) were incubated with different concentrations of VS-5584 (black bars, n = 4) or DMSO as vehicle (white bars, n = 4) for 30 min. Untreated WP or PRP served as negative control (grey bars, n = 4). Platelet viability was assessed by flow cytometric detection of calcein/CD42b-staining. Data are given in % of vehicle. Mean ± SEM. *p < 0.05 vs. vehicle; § p < 0.05 vs. 5 and 10 nM or µM VS-5584; °p < 0.05 vs. 5, 10 and 20 nM or µM VS-5584; $ p < 0.05 vs. 5, 10, 20 and 50 nM or µM VS-5584; +p < 0.05 vs. 5, 10, 20, 50 and 200 nM or µM VS-5584. C, D: WP (C) and PRP (D) were incubated with different concentrations of VS-5584 (black bars, n = 3) or DMSO as vehicle (white bars, n = 3) for 30 min. Untreated WP or PRP served as negative control (grey bars, n = 3) and PAR-1-AP-activated platelets served as positive control (crosshatched bars,n=3). Platelet viability was assessed by flow cytometric detection of annexin staining. Data are given in % of vehicle. Mean ± SEM. *p < 0.05 vs. vehicle; °p < 0.05 vs. 5, 10 and 20 nM or µM VS-5584; $ p < 0.05 vs. 5, 10, 20 and 50 nM or µM VS-5584; ~p < 0.05 vs. 5, 10, 20, 50, 200 and 500 nM or µM VS-5584.

    Platelets, 2018, 29(3):277-287. VS-5584 (SB2343) purchased from Selleck.

产品安全说明书

PI3K抑制剂选择性比较

生物活性

产品描述 VS-5584 (SB2343)是一种有效的,选择性,PI3K/mTOR双重抑制剂,抑制mTORPI3Kα/β/δ/γIC50分别为3.4 nM和2.6-21 nM。Phase 1。
靶点
PI3Kα [1]
(Cell-free assay)
PI3Kδ [1]
(Cell-free assay)
PI3Kγ [1]
(Cell-free assay)
mTOR [1]
(Cell-free assay)
PI3Kβ [1]
(Cell-free assay)
2.6 nM 2.7 nM 3.0 nM 3.4 nM 21 nM
体外研究

VS-5584是ATP竞争性抑制剂,选择性抑制PI3K/mTOR信号通路,作用效果和抑制所有人PI3K的亚型和mTOR激酶相当。VS-5584对HMLE乳腺癌细胞的选择性高于癌症干细胞约10倍, EC50值是15 nM。VS-5584优先降低HMLER永生乳腺癌细胞系中CD44Hi/CD24Lo细胞量。在SUM159细胞中,VS-5584有效地减少癌干细胞侧群。[1] 大量人类癌症细胞系(436株)表现广泛的抗增殖敏感性,含PI3KCA突变的细胞通常对VS-5584治疗更敏感。在FLT3-ITD突变的MV4-11细胞中,VS-5584抑制了pAkt(S473)和pAKT(T308),IC50分别为12 nM和13 nM。VS-5584抑制pS6 (S240/244), pAkt (S473)和pAkt (T308),IC50分别是20 nM,23 nM,和15 nM。[2]

体内研究 在三阴性乳腺癌的小鼠中,VS-5584的口服剂量减少肿瘤干细胞,并诱导紫杉烷抗性的模型中肿瘤消退。[1] 在PTENnull人前列腺癌PC3异种移植模型中,VS-5584在11毫克/千克和25毫克/千克时导致显著肿瘤生长抑制(TGI),抑制率分别为79%和113%。在FLT3-ITD AML移植瘤模型中,VS-5584治疗诱导剂量依赖性抑制肿瘤生长(3.7毫克/千克时为28%和11毫克/千克时为76%)。[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:[2]
- 合并

体外mTOR激酶测定:

反应混合物是由含有下列成分的10μL的测定缓冲液组成 (50 mM Hepes pH 7.5, 10 mM 氯化镁, 3 mM 氯化锰, 1 mM EGTA, 2 mM DTT, 0.01%吐温20):自制的0.10微克/毫升的mTOR酶,0.05 μM ULight-eIF4E-结合蛋白1(Thr37/46)和10 μM ATP。将混合物室温温育60分钟。10μL检测混合物包括16 mM EDTA,0.004mM Eu-W1024-标记的抗磷酸化的eIF4E结合蛋白1-(Thr37/46)抗体和1X的LANCE®检测缓冲液,然后加入温育60分钟。
细胞实验:[2]
- 合并
  • Cell lines: SNU-478, SNU-1196, SNU-245, SNU-1079, SNU-308和SNU-869
  • Concentrations: ~10 μM
  • Incubation Time: 48 小时
  • Method: CellTiter格洛分析
    (Only for Reference)
动物实验:[2]
- 合并
  • Animal Models: 雄性(PC3和COLO205)或雌性(MV4-11和的HuH7)的BALB/c裸小鼠或雌性SCID小鼠(NCI-N87)。
  • Dosages: 11 毫克/千克, 25 毫克/千克 每天一次
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 71 mg/mL (200.33 mM)
Ethanol 3 mg/mL (8.46 mM)
Water 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):
0.5% methylcellulose+0.2% Tween 80
30 mg/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 354.41
化学式

C17H22N8O

CAS号 1246560-33-7
储存条件 粉状
溶于溶剂
别名 N/A

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 g 每只动物给药体积 ul 动物数量
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 (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

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

  • 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02372227 Terminated Drug: VS-5584 and VS-6063 Relapsed Malignant Mesothelioma Verastem Inc. January 2015 Phase 1
NCT01991938 Terminated Drug: VS-5584 Non Hematologic Cancers|Metastatic Cancer|Lymphoma Verastem Inc. November 2013 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID