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网站主页 2-(2-氯-5-(苯基磺酰基)苯甲酰氨基)苯甲酸 化合物 BAY-8002
  • 化合物 BAY-8002|T5208|TargetMol

化合物 BAY-8002|T5208|TargetMol

BAY-8002
724440-27-1
278 1mg 起订
653 5mg 起订
987 10mg 起订
上海 更新日期:2024-09-29

TargetMol中国(陶术生物)

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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 BAY-8002
英文名称:
BAY-8002
CAS号:
724440-27-1
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:
99.13%
产品类别:
抑制剂
货号:
T5208

Product Introduction

Bioactivity

名称BAY-8002
描述BAY-8002 is a potent dual MCT1/2 inhibitor (IC50 values are 3, 8, and 12 nM at rat (C6), human (DLD-1) and mouse (4T1) MCT1 respectively).
细胞实验Cells were seeded at 3000- 6000 cells per well in a 90 μl volume in 96-well plates. Triplicates were treated in a dose range of 0-10 μmol/L. Cells were continuously exposed to the drug at 37°C and 5 % CO2. After 72 h, cell viability was measured using the CellTiter Glo cell viability assay. For the generation of resistant cell lines, cells were treated at IC50 and upon regrowth treated with increasing concentrations of the drug.
动物实验For in vivo studies, tumor cells were subcutaneously (s.c.) injected in 0.1 ml suspension to the left flank of 7-10 weeks old immunocompromised female mice (3 x 10^6 Raji cells in 10% Matrigel) to NOD SCID mice, 2 x 10^6 Colo320DM cells in 50% MatrigelTM to NMRI nu/nu mice, 3 x 10^6 WSU-DLCL2 cells or 1 x 10^7 Daudi cells in 50% MatrigelTM to CB17 SCID mice. Tumor area (length x width) and body weight was determined at least twice weekly. Tumors were allowed to establish before mice were allocated to different treatment and control groups by stratified randomization based on their primary tumor size. Oral treatments (p.o.) via gavage were performed as indicated. Final tumor weights were determined at the end of each study. For statistical analysis of tumor area as well as final tumor weights, data were analyzed using one-way ANOVA followed by Tukey's multiple comparisons test.
体外活性在DLD-1细胞中表达MCT1的情况下,BAY-8002以85 nM的IC50值抑制了细胞内SNARF-5的荧光变化,并且在抑制MCT4时表现出极佳的选择性(在EVSA-T细胞中的IC50>50 μmol/L)。
体内活性Raji肿瘤小鼠每日两次通过口服方式接受了80与160 mg/kg BAY-8002治疗。BAY-8002在抑制肿瘤生长方面显示出显著效果,但未观察到肿瘤退缩。Daudi Burkitt's淋巴瘤模型对MCT1抑制有所响应,尽管对于BAY-8002来说并不显著。
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 : 50 mg/mL (120.24 mM)
关键字Monocarboxylate Transporter | Inhibitor | inhibit | BAY-8002
相关产品D-Phenylalanine | 7ACC2 | AZD3965 | VB124 | AR-C155858 | Lactate transportor 1 | Niflumic acid | 7ACC1 | MSC-4381 | α-Cyano-4-hydroxycinnamic acid | MCT1-IN-3 | AZD0095
相关库抑制剂库 | 抗癌活性化合物库 | 经典已知活性库 | 抗癌化合物库 | 已知活性化合物库 | NO PAINS 化合物库 | 离子通道库 | 膜蛋白靶向化合物库 | 口服活性化合物库 | 表型筛选靶点鉴定库
BAY8002|||BAY 8002|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

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