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  3. AZ960

AZ960 

目录号: HY-10411 纯度: 97.15%
产品使用指南

AZ960是高效选择性的JAK2激酶抑制剂,Ki值为0.45 nM。

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AZ960 Chemical Structure

AZ960 Chemical Structure

CAS No. : 905586-69-8

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1559
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1 mg ¥700
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5 mg ¥2000
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10 mg ¥3000
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50 mg ¥9000
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100 mg ¥14000
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500 mg   询价  

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查看 JAK 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZ960 is a potent and specific inhibitor of the JAK2 kinase with a Ki of 0.45 nM.

IC50 & Target[4]

JAK2

0.45 nM (Ki)

JAK2

<3 nM (IC50)

JAK3

9 nM (IC50)

体外研究
(In Vitro)

AZ960 inhibits Jak2 kinase with a Ki of 0.45 nM. Z960 possesses much less potent activity against Jak1, 3, and TYK2. AZ960 is active against other kinases, including TrkA, Aurora-A, and FAK, with IC50 of around 0.1 μM. AZ960 effectively induces growth arrest and apoptosis of human T-cell lymphotropic virus type 1, HTLV-1–infected T cells (MT-1 and MT-2) in parallel with downregulation of the phosphorylated forms of Jak2 and Bcl-2 family proteins including Bcl-2 and Mcl-1[2]. AZ960 potently inhibits the clonogenic growth and induces apoptosis of freshly isolated acute myelogenous leukemia cells from patients in association with cleavage of caspase 3 and down regulation of anti-apoptotic Bcl-xL proteins[1]. AZ960 has a Ki of 1.25 μM for T. brucei extracellular signal-regulated kinase 8 (TbERK8). It inhibits TbERK8 with an IC50 of 120 nM[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

354.36

Formula

C18H16F2N6

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 30 mg/mL (84.66 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8220 mL 14.1099 mL 28.2199 mL
5 mM 0.5644 mL 2.8220 mL 5.6440 mL
10 mM 0.2822 mL 1.4110 mL 2.8220 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.05 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.05 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Cell Assay
[2]

AZ960 is dissolved in 100% DMSO to a 0.01 M. HTLV-1–infected T cells and MOLT-4 cells are cultured with various concentrations of AZ960 (0.03-1 μM) for 2 days in 96-well plates. Peripheral blood lymphocytes are activated by phytohemagglutinin (PHA; 5 ng/mL) for 1 hour, then cultured with various concentrations of AZ960 (0.03–1 μM) for 2 days in 96-well plates. After culture, cell number and viability are evaluated by measuring the mitochondrial-dependent conversion of the MTT to a colored formazan product[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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