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  • 化合物 AMG319|T6757|TargetMol

化合物 AMG319|T6757|TargetMol

AMG319
1608125-21-8
298 1mg 起订
428 2mg 起订
690 5mg 起订
上海 更新日期:2024-12-12

TargetMol中国(陶术生物)

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联系人:邵小姐
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邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
化合物 AMG319
英文名称:
AMG319
CAS号:
1608125-21-8
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:
98.9%
产品类别:
抑制剂
货号:
T6757

Product Introduction

Bioactivity

名称AMG319
描述AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
激酶实验PI3K Enzyme Assays: A PI3K Alphascreen assay is used to measure the activity of a panel of four phosphoinositide 3-kinases: PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ. Enzyme reaction buffer is prepared using sterile water and 50 mM Tris-HCl, pH 7, 14 mM MgCl2, 2 mM sodium cholate, and 100 mM NaCl. 2 mM DTT is added fresh on the day of the experiment. The Alphascreen buffer is made using sterile water and 10 mM Tris-HCl, pH 7.5, 150 mM NaCl, 0.10% Tween 20, and 30 mM EDTA. Then 1 mM DTT is added fresh on the day of the experiment. Compound source plates used for this assay are 384-well Greiner clear polypropylene plates containing test compounds at 5 mM and diluted 1:2 over 22 concentrations. Columns 23 and 24 contained only DMSO, as these wells comprised the positive and negative controls, respectively. Source plates are replicated by transferring 0.5 μL per well into 384-well Optiplates. Each PI3K isoform is diluted in enzyme reaction buffer to 2× working stocks. PI3Kα is diluted to 1.6 nM, PI3Kβ is diluted to 0.8 nM, PI3Kγ is diluted to 15 nM, and PI3Kδ is diluted to 1.6 nM. PI(4,5)P2 is diluted to 10 μM, and ATP was diluted to 20 μM. This 2× stock is used in the assays for PI3Kα and PI3Kβ. For assay of PI3Kγ and PI3Kδ, PI(4,5)P2 is diluted to 10 μM and ATP was diluted to 8 μM to prepare a similar 2× working stock. Alphascreen reaction solutions are made using beads from the anti-GST Alphascreen kit. Two 4× working stocks of the Alphascreen reagents are made in Alphascreen reaction buffer. In one stock, biotinylated-IP4 is diluted to 40 nM and streptavadin-donor beads are diluted to 80 μg/mL. In the second stock, PIP3-binding protein is diluted to 40 nM and anti-GST-acceptor beads were diluted to 80 μg/mL. As a negative control, a reference inhibitor at a concentration ?Ki (40 μM) is included in column 24 as a negative (100% inhibition) control. Using a 384-well Multidrop, 10 μL/well of 2× enzyme stock is added to columns 1–24 of the assay plates for each isoform.An amount of 10 μL/well of the appropriate substrate 2× stock (containing 20 μM ATP for the PI3Kα and -β assays and containing 8 μM ATP for the PI3Kγ and -δ assays) is then added to columns 1–24 of all plates. Plates are then incubated at room temperature for 20 min. In the dark, 10 μL/well of the donor bead solution is added to columns 1–24 of the plates to quench the enzyme reaction. The plates are incubated at room temperature for 30 min. Still in the dark, 10 μL/well of the acceptor bead solution is added to columns 1–24 of the plates. The plates are then incubated in the dark for 1.5 h. The plates are read on an Envision multimode plate reader using a 680 nm excitation filter and a 520–620 nm emission filter.
体外活性AMG319以8.6 nM的IC50抑制抗IgM/CD40L诱导的B细胞增殖,并以1.5 nM的IC50降低pAkt水平。AMG319还抑制HWB中由抗IgD诱导的CD-69表达。[1]
体内活性在雌性Lewis大鼠中,AMG319(3 mg/kg,口服)通过88%抑制了KLH诱导的炎症反应。在转基因(IgMm)小鼠中,AMG319(口服)抑制体内pAKT,IC50为1.9 nM。[1]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 71 mg/mL (184.2 mM)
Ethanol : 71 mg/mL (184.2 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字AMG 319 | AMG-319 | Inhibitor | inhibit | PI3K | Phosphoinositide 3-kinase | AMG319
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AMG319|TargetMol

公司简介

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。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

化合物 AMG319相关厂家报价

  • AMG-319
  • AMG-319
  • 德阳思诺生物科技有限公司 VIP
  • 2024-10-21
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