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网站主页 化工产品目录 生物化工 生化试剂 激动剂抑制剂 N,N'-双(2-溴乙基)二氨基膦酸 (1-甲基-2-硝基-1H-咪唑-5-基)甲酯 艾伏磷酰胺
  • 艾伏磷酰胺|T3615|TargetMol

艾伏磷酰胺|T3615|TargetMol

Evofosfamide
918633-87-1
422 1mg 起订
1160 5mg 起订
1530 10mg 起订
上海 更新日期:2024-12-12

TargetMol中国(陶术生物)

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产品详情:

中文名称:
艾伏磷酰胺
英文名称:
Evofosfamide
CAS号:
918633-87-1
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:
99.75%
产品类别:
抑制剂
货号:
T3615

Product Introduction

Bioactivity

名称Evofosfamide
描述Evofosfamide (TH-302) is a hypoxia-activated prodrug of the cytotoxin bromo-isophosphoramide mustard (Br-IPM) conjugated with 2-nitroimidazole, with potential antineoplastic activity. When exposed to hypoxic conditions, such as those found in hypoxic tumors, the 2-nitroimidazole moiety of evofosfamide is reduced. This releases the DNA-alkylating Br-IPM moiety, which introduces intra- and inter-strand DNA crosslinks in nearby cells; the crosslinks inhibit both DNA replication and cell division and may lead to apoptosis of cells in the tumor. The inactive form of the prodrug is stable under normoxic conditions, which may limit systemic toxicity.
细胞实验Exponentially growing human H460 or HT29 cells are seeded into 60 mm notched glass plates at 3 × 105 cells per plate and grown in RPMI medium supplemented with 10% fetal bovine serum for 2 days prior to initiating treatment. On the day of the test, TH-302 stocks of known concentrations are prepared in complete medium and 2 mL of the desired stock is added to each plate. The plates are placed in either an anaerobic chamber or a standard tissue-culture incubator. The anaerobic chamber is evacuated and gassed with the anaerobic gas mixture (90% N2/5% CO2/5% H2) to create a hypoxic environment. Cells are then incubated with TH-302 for 2 hours at 37 °C. At the end of treatment, plates are removed from each vessel and washed with phosphate-buffered saline and a solution of trypsin-EDTA and then trypsinized for 5 min at 37 °C. Detached cells are neutralized with medium plus serum and spun for 5 min at 100 g. Cells are resuspended at approximately 1 × 106 cells/mL and diluted 10-fold for plating. The exact concentration of each stock is determined. Known numbers of cells are plated and placed undisturbed in an incubator for between 9 and 13 days. Colonies are fixed and stained with a solution of 95% ethanol with 0.25% crystal violet stain. Colonies of greater than 50 cells are counted, and the surviving fraction is determined. Plating efficiencies (PEs) are determined by dividing the number of colonies by the actual number of cells plated. Surviving fractions are calculated by dividing the PEs of treated cells by the PEs of untreate(Only for Reference)
体外活性Evofosfamide在低氧条件下选择性强,对肝微粒体稳定。3b中磷酸芥上氯与溴的替换增强了10倍的活性,并保持了高低氧选择性[Hypoxia cytotoxicity ratio (HCR) = 270]。在人类肺癌H460细胞和人类结肠癌HT29细胞中,Evofosfamide在N2环境下显示出强大的细胞毒性。Evofosfamide分别以IC90 0.1 μM和0.2 μM抑制H460细胞和HT29细胞。[1] 相比于常氧条件下的H460单层细胞,Evofosfamide在H460球状细胞中展现出极大增强的活性。[2] Evofosfamide对MM细胞表现出具有低氧选择性和剂量依赖性的强大细胞毒性。Evofosfamide可在低氧条件下诱导G0/G1期细胞周期阻滞,其对细胞周期机制的影响通过下调cyclin D1/2/3、CDK4/6、p21cip-1、p27kip-1和pRb表达实现,而CDK2表达不受影响。Evofosfamide能在低氧条件下诱导人类和小鼠MM细胞的剂量依赖性凋亡。Evofosfamide激活的凋亡通过下调抗凋亡蛋白BCL-2和BCL-xL,以及上调cleaved proapoptotic protein caspase-3、-8和-9以及poly ADP-ribose polymerase表达实现。与特异性低氧毒性相反,Evofosfamide在常氧条件下即使在高浓度下也显示出极低的毒性。[3]
体内活性Evofosfamide通过在植入后第25天抑制原发性肿瘤生长41%,而Evofosfamide加上吉西他滨(一种核苷类似物)在第25天可抑制原发性肿瘤生长96%。[1] 当TH-302在H460 NSCLC异种移植模型中以6.25、12.5、25或50 mg/kg剂量每周5天每天一次,连续2周内腹腔注射(i.p.),第22天时的肿瘤生长抑制率分别为43%、51%、75%和89%。TH-302在100 mg/kg剂量下,治疗结束后3天血细胞计数下降,但在治疗后7天完全恢复。在所有测试方案下,TH-302展示的肿瘤生长抑制效果介于58%至89%之间。TH-302诱导的细胞杀伤依赖于呼吸氧浓度,当肿瘤携带的小鼠暴露于低氧浓度时,最大的细胞毒性发生。与吸入95% O2相比,吸入10% O2的动物中TH-302显著减少了肿瘤生长。TH-302治疗后,在给药48小时后,pimonidazole阳性区域显著减少(对照组为6.3%,TH-302治疗组为1.8%)。[4]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度Ethanol : 83 mg/mL (184.8 mM)
DMSO : 83 mg/mL (184.8 mM)
H2O : 10 mg/mL (22.27 mM)
关键字TH302 | TH 302 | Inhibitor | inhibit | Evofosfamide | Apoptosis
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相关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 | ReFRAME 相关化合物库 | 细胞凋亡化合物库 | 抗衰老化合物库 | NO PAINS 化合物库 | 临床期小分子药物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库
艾伏磷酰胺|||TH-302|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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