化合物 AZ 960|T6309|TargetMol

AZ960
905586-69-8

￥578 1mg 起订

￥885 2mg 起订

￥1660 5mg 起订

上海更新日期：2024-09-30

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 AZ 960

英文名称：: AZ960

CAS号：: 905586-69-8

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 98.51%

产品类别：: 抑制剂

货号：: T6309

Product Introduction

Bioactivity

Name	AZ960
Description	AZ960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
Cell Research	Cellular proliferation is evaluated using the fluorometric/colorimetric BIOSOURCE AlamarBlue Assay and read in the Spectra Max Gemini EM microplate reader. SET-2 cells are plated at 20,000 cells/well, TEL-JAK2 Ba/F3 cells at 2000 cells/well, and all other TEL-JAKs at 5000 cells/well in 96-well plates. Cells are treated with AZ 960 24 hours after plating and grown for 72 hours for SET-2 and 48 hours for TEL-JAK Ba/F3 cells. Following the indicated growth period Alamar Blue (10 μL/well) is added, cells are incubated at 37 °C in 5% CO2 for 2 hours, and fluorescence is measured at 545 (excitation) and 600 nm (emission). Data are normalized to percent of the control, and GI50 values (the concentration that causes 50% growth inhibition) are calculated using Xlfit4 version 4.2.2 for Microsoft Excel. (Only for Reference)
Kinase Assay	Enzyme Biochemical Assay and Kinase Profiling: Inhibition studies of AZ 960 are performed using a recombinant JAK2 kinase (amino acids 808–1132) at a peptide (Tyk2 peptide) concentration of 100 nM and an ATP concentration of 15 μM. Concentrations of AZ 960 ranging from 0.003 μM to 30 μM are used. The mode of inhibition and inhibition constant (Ki) of AZ960 against JAK2 kinase are further evaluated by inhibition kinetics. Specifically, a series of JAK2-catalyzed reactions are set up in HEPES buffer (75 mM, pH 7.3) with a fixed concentration of peptide (FL-Ahx-IPTSPITTTYFFFKKK-COOH), and varied concentrations of ATP and AZ 960. The progress of each reaction is subsequently monitored by the Caliper LC3000 system, and the initial velocity of each reaction is extracted from the corresponding reaction time course. To define the mode of inhibition, initial velocities are plotted against corresponding ATP concentrations using Lineweaver-Burk plots and the characteristic convergence of the lines on the y axis demonstrates the competitiveness of AZ 960 to ATP. Initial inspection of Ki using the Michealis-Menten equation revealed that AZ960 is a tight-binding inhibitor of JAK2. AZ960 is profiled against 83 kinases at three inhibitor concentrations (0.01 μM, 0.10 μM, and 1.0 μM).
In vivo	AZ960（0.1 μM）对83 种激酶中的31种也有抑制作用,如 JAK3(IC50：9 nM),Aurora,TrkA,和ARK5。AZ 960明显抑制 TEL-JAK2,-JAK1,-JAK3和-Tyk2细胞增殖（GI50：25/230/279/214 nM）。AZ 960还可降低 STAT3/5磷酸化水平,从而有效抑制SET-2 细胞增殖（GI50：~33 nM）。AZ 960可抑制TEL-JAK2细胞中STAT5磷酸化（IC50：15 nM）,对TEL-JAK2驱动的STAT5磷酸化比对其他JAK激酶家族成员(TEL-JAK1, -JAK3和 -TYK2)驱动的细胞系选择性高15到30倍。AZ 960还使人类 T-细胞淋巴嗜淋巴细胞病毒1型感染的T细胞生长停滞和凋亡,且通过小干扰RNA增强AZ 960对MT-1细胞的抗增殖效果,从而抑制Bcl-xL。AZ 960显著抑制患者新分离的AML细胞克隆性生长,并诱导细胞凋亡。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	Ethanol : 3 mg/mL (8.46 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 55 mg/mL (155.21 mM), Sonication is recommended.
Keywords	AZ960 \| Virus Protease \| Apoptosis \| Parasite \| JAK \| inhibit \| Inhibitor \| Janus kinase \| AZ-960
Inhibitors Related	Doxycycline \| Metronidazole \| Hydroxychloroquine \| 5-Fluorouracil \| Stavudine \| Tributyrin \| Dextran sulfate sodium salt (MW 4500-5500) \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Sodium 4-phenylbutyrate \| Phenytoin sodium
Related Compound Libraries	Inhibitor Library \| Anti-Cancer Active Compound Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Kinase Inhibitor Library \| Anti-Aging Compound Library \| Anti-Viral Compound Library \| Anti-Parasitic Compound Library \| Tyrosine Kinase Inhibitor Library \| Anti-Prostate Cancer Compound Library

AZ 960|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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