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网站主页 化工产品目录 生物化工 抑制剂 代谢(Metabolism) Dehydrogenase 抑制剂 AGI-5198 (IDH-C35) 化合物 AGI-5198
  • 化合物 AGI-5198|T2104|TargetMol

化合物 AGI-5198|T2104|TargetMol

AGI-5198
1355326-35-0
￥297 5mg 起订
￥493 10mg 起订
￥726 50mg 起订
上海 更新日期：2024-09-23

TargetMol中国（陶术生物）

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联系人：邵小姐
电话：021-021-33632979拨打
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邮箱：marketing@targetmol.com

产品详情:

中文名称：
化合物 AGI-5198
英文名称：
AGI-5198
CAS号：
1355326-35-0
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：
99.23%
产品类别：
抑制剂
货号：
T2104

Product Introduction

Bioactivity

NameAGI-5198
DescriptionAGI-5198 (IDH-C35) is a potent and selective inhibitor of IDH1 R132H and R132C mutants, with IC50 values of 0.07 μM and 0.16 μM, respectively.
Cell ResearchAGI-5198 is dissolved in DMSO.TS603 cells are grown in medium containing either AGI-5198 (1.5 μM) or DMSO vehicle control.One week prior to harvest cells are ransferred to differentiation medium (DMEM F12; 15 mM HEPES; 0.06% glucose; B27 without vitamin A; N2; Insulin/transferrin; 1% FBS) containing freshly added retinoic acid (1 μM).ChIP of non-crosslinked cells is then carried out using established ChIP methods.350 μg of lysate is immunoprecipitated-using anti-H3K9Me3,H3K27me3 or Rabbit Control IgG.After washing,ChIP DNA is eluted from protein G beads and analyzed by RT-PCR using SYBR green.Relative occupancy is calculated using the standard curve method and fold enrichment versus IgG.Enrichment in AGI- 5198-treated cells is normalized to vehicle control.Means and standard deviation are calculated from 4 technical replicates.
Kinase AssayIDH enzyme activity: Compound is prepared as 10 mM stock in DMSO and diluted to 50X final concentration in DMSO, for a 50 μL reaction mixture. IDH enzyme activity converting alpha-ketogluta rate to 2-hydroxyglutarate is measured using a NADPH depletion assay. In the assay the remaining cofactor is measured at the end of the reaction with the addition of a catalytic excess of diaphorase and resazurin, to generate a fluorescent signal in proportion to the amount of NADPH remaining. IDH enzyme activity in the direction of isocitrate to alpha-ketoglutarate conversion is measured by direct coupling of the NADPH production to conversion of resazurin to resorufin by diaphorase. In both cases, resorufin is measured fluorometrically at Ex544 Em 590.
In vitro在带有Ki-67蛋白抗体染色的小鼠体内,AGI-5198可使其肿瘤减少.但空白对照组和AGI-5198处理组的小鼠肿瘤中裂解的caspase-3无显著差异.AGI-5198（450 mg/kg/day）治疗R132H-IDH1胶质瘤移植瘤三周,可抑制50-60％的生长,但不影响IDH1野生型胶质瘤移植瘤的生长.
In vivoAGI-5198对TS603胶质瘤细胞系有一定抗肿瘤疗效,且剂量依赖性抑制R-2HG产生。在R-2HG几乎被完全抑制的条件下,AGI-5198对组蛋白H3K9me3去甲基化有诱导作用,且诱导与胶质基因分化相关的基因表达。在全基因组DNA甲基化中,AGI-5198对mIDH1受损的IDH1突变型生长具有抑制作用,但野生型生长几乎没有受到影响。AGI-5198对突变型IDH1(R132H-IDH1 和 R132C-IDH1)有明显抑制作用,但对野生型IDH1 (IC50>100 μM) 或任何IDH2亚型(R140Q, R172K, 野生型) (IC50>100 μM)抑制作用非常弱。
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 23 mg/mL (49.7 mM)
Ethanol : 12 mg/mL (25.9 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
KeywordsInhibitor | Isocitrate Dehydrogenase (IDH) | inhibit | AGI 5198 | AGI5198 | AGI-5198
Inhibitors RelatedSodium Oxamate | ALDH1A3-IN-3 | Benzyl alcohol | Isoniazid | Rotenone | Isomalt | 4-Diethylaminobenzaldehyde | Mycophenolate Mofetil | Ivosidenib | Methotrexate | Ribavirin | Disulfiram
Related Compound LibrariesInhibitor Library | Bioactive Compound Library | Bioactive Compounds Library Max | Metabolism Compound Library | Fluorochemical Library | Highly Selective Inhibitor Library | NO PAINS Compound Library | Glutamine Metabolism Compound Library | Glycometabolism Compound Library | Anti-Metabolism Disease Compound Library
IDH-C35|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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  • 2024-09-29
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