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Camptothecin

Camptothecin是一种特异性的DNA拓扑异构酶I (Topo I)抑制剂，IC50为0.68 μM。

目录号
EY1560
EY1560
EY1560
纯度
99.77%
99.77%
99.77%
规格
100 mg
200 mg
500 mg
原价
300
500
1000
售价
300
500
1000
库存
现货
现货
现货
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  • 生物活性

    Camptothecin could induce cell death in SMMC-7721, MCF-7, and HCT-116 tumor cells. Camptothecin has been reported to induce autophagy via AMPK-TSC2-mTOR pathway, at the mean time, induce premature senescence by ATM-Chk2-p53-p21 pathway.

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% Propylene glycol

  • 激酶实验

  • 细胞实验

    0.17 nM–10 mM

  • 动物实验

    0–8 mg/kg 肌肉注射或静脉注射，每周两次

  • 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 A的Km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] Wall ME, et al. J Am Chem Soc, 1966, 88 (16), 3888–3890.
    [2] Suzuki, A., et al. 1996. Exp. Cell Res. 227: 154-159.
    [3] Pommier, Y., et al. 1998. Biochim. Biophys. Acta. 1400: 83-105.
    [4] Sriram, D., et al. 2005. Nat. Prod. Res. 19: 393-412.
    [5] Chiou, W.F., et al. 2001. Life Sci. 69: 625-635.
    [6] Slichenmyer, W.J., et al. 1993. J. Natl. Cancer Inst. 85: 271-291.

    分子式
    C20H16N2O4    		 分子量
    348.36    		 CAS号
    7689-03-4    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    5 mM    		 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
    NCT00947739 Advanced Solid Tumors|Lymphomas Drug: Camptothecin-20-O-Propionate Hydrate (CZ48) New Mexico Cancer Care Alliance|Christus Stehlin Foundation for Cancer Research Phase 1 2008-09-01 2015-06-16
    NCT02575638 Malignant Lymphoma of Extranodal and/or Solid Organ Site|Solid Tumor Drug: CZ48 Cao Pharmaceuticals Inc.|The University of Texas Health Science Center at San Antonio Phase 1 2008-07-01 2015-10-12
    NCT00277082 Corpus Uteri|Lung Cancer Drug: 9-NC in aerosol reservoir University of New Mexico 2003-08-01 2010-01-06
    NCT00250068 Lung Diseases|Cancer Drug: Liposomal 9-Nitrocamptothecin University of New Mexico Phase 2 2003-04-01 2010-05-18
    NCT01803269 Extensive Stage Small Cell Lung Cancer|Recurrent Small Cell Lung Cancer Drug: topotecan hydrochloride|Drug: cyclodextrin-based polymer-camptothecin CRLX101 University of Chicago|National Cancer Institute (NCI) Phase 2 2013-01-01 2016-06-16
    NCT02769962 Solid Tumors|Small Cell Lung Carcinoma|Carcinoma, Non-Small-Cell Lung|Lung Neoplasms Drug: CRLX101|Drug: olaparib National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 1|Phase 2 2016-05-03 2017-01-24
    NCT00059917 Unspecified Adult Solid Tumor, Protocol Specific Drug: polyglutamate camptothecin Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) Phase 1 2003-01-01 2013-05-29
    NCT00250120 Lung Diseases|Cancer Drug: L9NC: Liposomal 9-Nitro-20 (S)-Camptothecin University of New Mexico Phase 2 2003-04-01 2016-05-10
    NCT00080002 Cancer of Stomach|Gastroesophageal Cancer Drug: Pegamotecan Enzon Pharmaceuticals, Inc. Phase 2 2003-12-01 2012-09-05
    NCT00249990 Corpus Uteri|Endometrial Cancer Drug: 9-NC in aerosol reservoir University of New Mexico|Baylor College of Medicine Phase 2 2003-04-01 2010-01-06
    NCT00250016 Corpus Uteri|Endometrial Cancer University of New Mexico 2003-08-01 2010-01-06
    NCT01612546 Adenocarcinoma of the Esophagus|Adenocarcinoma of the Gastroesophageal Junction|Diffuse Adenocarcinoma of the Stomach|Intestinal Adenocarcinoma of the Stomach|Mixed Adenocarcinoma of the Stomach|Recurrent Esophageal Cancer|Recurrent Gastric Cancer|Squamous Cell Carcinoma of the Esophagus|Stage IIIB Esophageal Cancer|Stage IIIB Gastric Cancer|Stage IIIC Esophageal Cancer|Stage IIIC Gastric Cancer|Stage IV Esophageal Cancer|Stage IV Gastric Cancer Drug: cyclodextrin-based polymer-camptothecin CRLX101|Other: Laboratory biomarker analysis|Other: Pharmacological studies City of Hope Medical Center|National Cancer Institute (NCI) 2012-11-01 2015-06-03
    NCT00492141 Ewing's Sarcoma Drug: Temozolomide|Drug: L9-NC M.D. Anderson Cancer Center Phase 1|Phase 2 2006-06-01 2012-08-01
    NCT01748019 Solid Tumors Drug: ST1968 sigma-tau i.f.r. S.p.A.|Southern Europe New Drug Organization Phase 1 2007-06-01 2012-12-10
    NCT01124539 Glioblastoma Multiforme|GBM|Gliosarcoma Drug: AR-67 (7-t-butyldimethylsiltyl-10-hydroxy-camptothecin) Arno Therapeutics Phase 2 2009-12-01 2014-12-08
    NCT00333502 Cancer|Solid Tumor Drug: Camptothecin (CPT) conjugated to a linear, cyclodextrin-based polymer Cerulean Pharma Inc. Phase 1|Phase 2 2006-05-01 2012-07-30
    NCT00079950 Sarcoma, Soft Tissue Drug: Pegamotecan Enzon Pharmaceuticals, Inc. Phase 2 2003-08-01 2012-09-05
    NCT00283556 Malignant Glioma Drug: Irinotecan (Camptosar, CPT-11) Kentuckiana Cancer Institute Phase 1|Phase 2 2001-08-01 2010-01-18
    NCT00291785 Colorectal Cancer Drug: CT-2106|Drug: Folinic acid|Drug: 5-FU (fluorouracil) CTI BioPharma Phase 1|Phase 2 2004-01-01 2011-06-06
    NCT01380769 Non-Small Cell Lung Cancer Drug: CRLX101|Other: Best Supportive Care Cerulean Pharma Inc. Phase 2 2011-06-01 2015-03-02
    NCT00249977 Solid Tumors|Cancer Drug: Capecitabine in Combination with Cisplatin and Irinotecan University of New Mexico Phase 1 2003-04-01 2010-01-06

    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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