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Raltitrexed

雷替曲塞,兰替特噻,ZD 1694,ZD1694,ZD-1694

Raltitrexed是胸苷酸合成酶抑制剂,是肿瘤化疗中的抗代谢剂。

目录号
EY1530
EY1530
EY1530
纯度
99.53%
99.53%
99.53%
规格
5 mg
25 mg
100 mg
原价
280
400
1200
售价
280
400
1200
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Raltitrexed is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth. Raltitrexed is a folate-based inhibitor of thymidylate synthase (TS) that is rapidly and extensively metabolized to its more potent polyglutamate derivatives. Raltitrexed is an inhibitor of DHFR.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Peters GJ, et al. Eur J Cancer, 2000, 36(7), 916-924.
    [2] Jodrell, D I., et al., 1991. The pharmacokinetics of the quinazoline antifolate ICI D 1694 in mice and rats. Cancer chemotherapy and pharmacology. 28(5): 331-8.
    [3] Jackman, A L., et al., . ZD1694 (Tomudex): a new thymidylate synthase inhibitor with activity in colorectal cancer. European journal of cancer (Oxford, England : 1990). 31A(7-8): 1277-82.

    分子式
    C21H22N4O6S
    分子量
    458.49
    CAS号
    112887-68-0
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    90 mg/mL
    Water
    <1 mg/mL
    Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02618356 Metastatic Colon Cancer Drug: Raltitrexed and S-1 Fudan University Phase 2 2015-12-01 2015-12-02
    NCT02562599 Nasopharyngeal Carcinoma Drug: raltitrexed-cisplatin|Radiation: Intensity-modulated radiotherapy (IMRT) Hubei Cancer Hospital Phase 2 2015-08-01 2015-09-28
    NCT02557490 Colon Cancer Liver Metastasis Drug: oxaliplatin and raltitrexed Zhu Xu|Beijing Cancer Hospital Phase 4 2015-01-01 2015-09-22
    NCT03053167 ColoRectal Cancer Drug: Irinotecan|Drug: Raltitrexed China Medical University, China|The First Affiliated Hospital of Dalian Medical University|The Second Affiliated Hospital of Dalian Medical University|Liaoning Tumor Hospital & Institute|Shengjing Hospital|General Hospital of Shenyang Military Region Phase 2 2016-12-01 2017-02-13
    NCT03083613 Gastric Cancer|Gastroesophageal Junction Adenocarcinoma Drug: Raltitrexed|Drug: Paclitaxel Chinese Academy of Medical Sciences Phase 2 2015-05-01 2017-03-14
    NCT02072317 Advanced Gastric Cancer Drug: taxel plus raltitrexed|Drug: taxol Fudan University Phase 2 2013-11-01 2014-02-24
    NCT01836120 Gastric Cancer Drug: Raltitrexed plus Docetaxel|Drug: Docetaxel Hebei Tumor Hospital Phase 2 2013-04-01 2013-04-18
    NCT00003528 Recurrent Childhood Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Myeloid Leukemia Drug: raltitrexed National Cancer Institute (NCI) Phase 1 1998-09-01 2013-01-15
    NCT01732380 Inoperable Esophageal Cancer Stage I-III Drug: Raltitrexed|Drug: Oxaliplatin|Radiation: Radiotherapy The First People's Hospital of Lianyungang|The East Hospital of Lianyungang|Donghai People's Hospital|People's Hospital of Ganyu Phase 2 2012-07-01 2012-11-19
    NCT01959061 Colorectal Cancer Metastatic Drug: Raltitrexed|Drug: Oxaliplatin|Drug: lipiodol Nanjing Chia-tai Tianqing Pharmaceutical Phase 4 2013-09-01 2017-03-09
    NCT02485548 Head and Neck Squamous Cell Cancer Drug: Raltitrexed|Drug: 5-fluorouracil|Drug: Cisplatin|Radiation: IMRT Jiangsu Cancer Institute & Hospital|Wuxi Cancer Hospital|Changzhou Cancer Hospital|Nanjing Cancer Hospital|Northern Jiangsu Province People's Hospital|The Second Hospital of Nanjing Medical University|Nanjing BenQ Hospital Phase 3 2015-06-01 2015-06-29
    NCT02992886 Rectal Neoplasms Malignant Radiation: Preoperative radiation|Drug: Raltitrexed|Procedure: Pelvic surgery Chinese Academy of Medical Sciences Phase 2 2016-09-01 2016-12-13
    NCT02821559 Metastatic Colorectal Cancer Drug: TOMOX|Drug: Bevacizumab Centre Hospitalier Universitaire de Besancon|Hospira, Inc. Phase 2 2012-07-01 2016-06-29
    NCT00590278 Inoperable or Recurrent Rectal Cancer Drug: Tomudex|Procedure: Radiotherapy|Procedure: Haematology|Procedure: Biochemistry AstraZeneca Phase 2 2002-08-01 2008-01-23
    NCT01348412 Colorectal Cancer|Liver Metastases Drug: oxaliplatin|Drug: raltitrexed|Drug: other intravenous chemotherapy drugs Centre Georges Francois Leclerc|National Cancer Institute, France|Hospira, Inc. Phase 2 2010-12-01 2016-04-22
    NCT00234429 Colorectal Cancer Drug: Gefitinib, raltitrexed AstraZeneca Phase 2|Phase 3 2003-11-01 2007-12-14
    NCT00004920 Malignant Mesothelioma Drug: cisplatin|Drug: raltitrexed European Organisation for Research and Treatment of Cancer - EORTC Phase 3 1999-11-01 2012-07-17
    NCT02631564 Colon Cancer Liver Metastasis Fudan University 2015-06-01 2015-12-14
    NCT00002828 Colorectal Cancer Drug: fluorouracil|Drug: raltitrexed Memorial Sloan Kettering Cancer Center Phase 1 1995-04-01 2013-06-20
    NCT02453490 Colorectal Cancer|Liver Metastasis Drug: Raltitrexed-based chemotherapy|Drug: Raltitrexed-based chemotherapy|Drug: 5-fluorouracil-based chemotherapy|Drug: 5-fluorouracil-based chemotherapy Zhejiang University Phase 3 2015-10-01 2017-03-10

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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