SP-96

For research use only. Not for use in humans.

目录号:S9658

SP-96 Chemical Structure

CAS No. 2682114-54-9

SP-96 是一种有效的、选择性的、非ATP竞争性 Aurora B的抑制剂,其IC50值为0.316 nM。SP-96 可用于三阴性乳腺癌 (TNBC)的研究。

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产品安全说明书

Aurora Kinase抑制剂选择性比较

生物活性

产品描述 SP-96 是一种有效的、选择性的、非ATP竞争性 Aurora B的抑制剂,其IC50值为0.316 nM。SP-96 可用于三阴性乳腺癌 (TNBC)的研究。
靶点
Aurora B [1]
(Cell-free assay)
0.316 nM
体外研究

SP-96 shows sub-nanomolar potency in Aurora B enzymatic assays (IC50 = 0.316 ± 0.031 nM). SP-96 shows >2000 fold selectivity against FLT3 and KIT which is important for normal hematopoiesis. Enzyme kinetics of SP-96 shows non-ATP competitive inhibition which makes it a first-in-class inhibitor. SP-96 shows selective growth inhibition in NCI60 screening, including inhibition of MDA-MD-468, a Triple Negative Breast Cancer cell line.[1]

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]

- 合并

Aurora Kinase B enzymatic assay:

Kinase inhibition assay is done by measuring kinase activity in a microfluidics assay. The separation of a phosphorylated product from substrate is monitored. The assay is run using a 12-sipper chip on a Caliper EZ Reader II. The recipe used for separation buffer is 100 mM HEPES, 10 mM EDTA, 0.015% Brij-35, 0.1% CR-3. The compound stocks (20 mM in DMSO) are diluted into kinase buffer. 1 μL of desired stock solution is transferred into a 384-well microtiter assay plate. The Aurora B enzyme is diluted in kinase buffer to a concentration of 2 nM. 5 μL of the enzyme mixture is transferred to the assay plate. The inhibitors/Aurora B enzyme are incubated for 60 min with minor shaking. A substrate mix is prepared containing ATP and 5FAM tagged peptide dissolved in kinase buffer described above. 5 μL of the substrate solution is added to the assay plate. Running concentrations are as follows: peptide (1.5 μM), ATP (190 μM), and compound 12-point ½log dilutions (0.2 mM-0.632 nM). No inhibitor is added for positive control, and no enzymewas added for negative control. For running control, barasertib is used. Percentage inhibition is measured by comparing starting peptide to phosphorylated productpeaks.
细胞实验:

[1]

- 合并
  • Cell lines: MCF-7 cells
  • Concentrations: --
  • Incubation Time: 24 h
  • Method:

    The growth inhibition of 60 cell lines is obtained by submitting the compound to National Cancer Institute’s NCI60 panel. MCF-7 cells are cultured in RPMI-1640 medium with 5% FBS in an incubator maintained at 37 ℃ and 5% CO2. The media is changed on alternate days. After reaching confluency, the media is aspirated, cells are washed with PBS, detached using 0.25% trypsin and centrifuged. The collected cells are seeded in 96-well microtiter plates at a density of 5000 cells/well. The cells are allowed to adhere to plate overnight. The test compounds, vehicle control and positive controls are added 24 h after the cells are plated and allowed to incubate. Following 24 h of incubation, the media is aspirated, and the cells are washed with PBS. 40 mL of the media and 10 mL of 5 mg/mL of MTT solution prepared in PBS is added to the cells and incubated for 4 h at 37 ℃ and 5% CO2. After incubation, 150 mL of DMSO is added to each well and the cell viability is measured at 570 nM by an ELISA plate reader.


    (Only for Reference)

溶解度 (25°C)

体外 DMSO 91 mg/mL (200.67 mM)
Ethanol 2 mg/mL (4.41 mM)
Water Insoluble

* 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 453.47
化学式

C25H20FN7O

CAS号 2682114-54-9
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID