|(1S,9S)-1-氨基-9-乙基-5-氟-9-羟基-4-甲基-2,3,12,15-四氢苯并[de]吡喃并[3',4':6,7]吲哚并[1,2-b]喹啉-10,13(1H,9H)-二酮甲磺酸盐|CsnPharm

CAS No.: 169869-90-3

依喜替康甲磺酸盐 Catalog No. CSN17998

Synonyms: DX8951f;Exatecan (mesylate);DX-8951

Exatecan mesylate is a totally synthetic analogue of the topoisomerase I-inhibitor camptothecin, which was synthesised to impart increased aqueous solubility, greater tumour efficacy, and less toxicity than camptothecin itself.

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描述DNA topoisomerases are enzymes that catalyze the alteration of DNA topology with transiently induced DNA strand breakage, essential for DNA replication^[3]. Exatecan mesylate is a totally synthetic analogue of the topoisomerase I-inhibitor camptothecin, which was synthesised to impart increased aqueous solubility, greater tumour efficacy, and less toxicity than camptothecin itself. Exatecan mesylate (DX-8951f) significantly inhibits the proliferation of several cancer cell lines, with mean GI50s of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast cancer cells, colon cancer cells, stomach cancer cells and lung cancer cells, respectively^[4]. Exatecan mesylate (DX-8951f, 3.325-50 mg/kg, i.v.) exhibits antitumor activities in the mice model bearing tumor cells, without toxic death. Exatecan mesylate (15, 25 mg/kg, i.v.) hightly inhibits MIA-PaCa, BxPC-3 primary tumor growth in the MIA-PaCa-2 early-stage model and early-stage model of BxPC-3. Exatecan mesylate (15, 25 mg/kg, i.v.) also significantly suppresses BxPC-3 lymphatic metastasis and completely eliminates lung metastasis in the BxPC-3 late-stage cancer model^[5]. Exatecan mesylate (DX-8951f) displays cytotoxic activities against PC-6, PC-6/SN2-5 cells, with mean GI50s of 0.186 and 0.395 ng/mL, respectively. Exatecan mesylate (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells^[6].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00004060	Fallopian Tube Cancer ... more >> Ovarian Cancer Primary Peritoneal Cavity Cancer Collapse <<	Phase 2	Completed	-	United States, Texas ... more >> University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030 Collapse <<
NCT00004046	Breast Cancer	Phase 2	Completed	-	United States, Texas ... more >> University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030-4009 Collapse <<
NCT00004047	Leukemia Myel... more >>odysplastic Syndromes Collapse <<	Phase 1	Completed	-	United States, Texas ... more >> University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8813 mL
- 9.4064 mL
- 18.8128 mL
- 5 mM
- 0.3763 mL
- 1.8813 mL
- 3.7626 mL
- 10 mM
- 0.1881 mL
- 0.9406 mL
- 1.8813 mL

技术信息

CAS号	169869-90-3	储存条件	粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C25H26FN3O7S	运输	蓝冰
分子量	531.55	别名	DX8951f;Exatecan (mesylate);DX-8951;依喜替康甲磺酸盐

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00004060	Fallopian Tube Cancer ... more >> Ovarian Cancer Primary Peritoneal Cavity Cancer Collapse <<	Phase 2	Completed	-	United States, Texas ... more >> University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030 Collapse <<
NCT00004046	Breast Cancer	Phase 2	Completed	-	United States, Texas ... more >> University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030-4009 Collapse <<
NCT00004047	Leukemia Myel... more >>odysplastic Syndromes Collapse <<	Phase 1	Completed	-	United States, Texas ... more >> University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030 Collapse <<
NCT00004045	Prostate Cancer	Phase 2	Completed	-	United States, Texas ... more >> U.S. Oncology Research Inc. Houston, Texas, United States, 77060 Institute for Drug Development San Antonio, Texas, United States, 78245-3217 Collapse <<
NCT00003951	Pancreatic Cancer	Phase 2	Completed	-	United States, Maryland ... more >> Johns Hopkins Oncology Center Baltimore, Maryland, United States, 21287 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 United States, Texas University of Texas Health Science Center at San Antonio San Antonio, Texas, United States, 78284 Collapse <<
NCT00004212	Brain and Central Nervous Syst... more >>em Tumors Lymphoma Unspecified Childhood Solid Tumor, Protocol Specific Collapse <<	Phase 1	Completed	-	United States, New York ... more >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 United States, Tennessee St. Jude Children's Research Hospital Memphis, Tennessee, United States, 38105-2794 United States, Texas Children's Medical Center of Dallas Dallas, Texas, United States, 75235 Institute for Drug Development San Antonio, Texas, United States, 78245-3217 Collapse <<
NCT00005091	Lung Cancer	Phase 2	Completed	-	Finland ... more >> Helsinki University Central Hospital Helsinki, Finland, FIN-0-0029 Germany Thoraxklinik Rohrbach Heidelberg, Germany, D-69126 Italy Ospedale Bellaria Bologna, Italy, I-40139 Netherlands Academisch Ziekenhuis der Vrije Universiteit Amsterdam, Netherlands, 1117 MB United Kingdom Christie Hospital N.H.S. Trust Manchester, England, United Kingdom, M20 4BX Oxford Radcliffe Hospital Oxford, England, United Kingdom, 0X3 7LJ Collapse <<
NCT00005938	Extrahepatic Bile Duct Cancer ... more >> Gallbladder Cancer Liver Cancer Collapse <<	Phase 2	Completed	-	United States, Colorado ... more >> University of Colorado Cancer Center Denver, Colorado, United States, 80262 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 United States, Texas Simmons Cancer Center - Dallas Dallas, Texas, United States, 75235-9154 University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030-4009 Cancer Therapy & Research Center San Antonio, Texas, United States, 78229 Collapse <<
NCT00004108	Liver Cancer	Phase 2	Completed	-	United States, Colorado ... more >> University of Colorado Cancer Center Denver, Colorado, United States, 80262 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 United States, Texas University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030-4009 Cancer Therapy & Research Center San Antonio, Texas, United States, 78229 Collapse <<
NCT00004866	Cervical Cancer	Phase 2	Completed	-	United States, New York ... more >> Albert Einstein Clinical Cancer Center Bronx, New York, United States, 10461 St. Luke's-Roosevelt Hospital New York, New York, United States, 10019 United States, Ohio Ruppert Health Center Toledo, Ohio, United States, 43614 United States, Tennessee Brookview Research, Inc. Nashville, Tennessee, United States, 37203 United States, Texas Texas Oncology PA (TOPA) at Baylor-Sammons Dallas, Texas, United States, 75246 University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030-4009 Collapse <<
NCT00017212	Esophageal Cancer ... more >> Gastric Cancer Collapse <<	Phase 2	Completed	-	United States, California ... more >> Pacific Shores Medical Group Long Beach, California, United States, 90813 United States, Colorado Rocky Mountain Cancer Centers Denver, Colorado, United States, 80218 United States, Texas Simmons Cancer Center - Dallas Dallas, Texas, United States, 75235-9154 University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030-4009 Cancer Therapy and Research Center San Antonio, Texas, United States, 78229-3264 Canada, Ontario Cancer Care Ontario-Hamilton Regional Cancer Centre Hamilton, Ontario, Canada, L8V 5C2 Collapse <<
NCT00023972	Pancreatic Cancer	Phase 3	Completed	-	-
NCT00055952	Sarcoma	Phase 2	Completed	-	United States, Colorado ... more >> University of Colorado Cancer Center at University of Colorado Health Sciences Center Denver, Colorado, United States, 80218 United States, Florida Nemours Children's Clinic Jacksonville, Florida, United States, 32207 United States, New Jersey Cancer Institute of New Jersey New Brunswick, New Jersey, United States, 08903 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 United States, Tennessee St. Jude Children's Research Hospital Memphis, Tennessee, United States, 38105 United States, Texas Medical City Dallas Hospital Dallas, Texas, United States, 75230 Simmons Cancer Center at University of Texas Southwestern Medical Center - Dallas Dallas, Texas, United States, 75390-9063 University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030-4009 Canada, Ontario Hospital for Sick Children Toronto, Ontario, Canada, M5G 1X8 Collapse <<
NCT00045318	Unspecified Adult Solid Tumor,... more >> Protocol Specific Collapse <<	Phase 1	Completed	-	United States, California ... more >> Jonsson Comprehensive Cancer Center, UCLA Los Angeles, California, United States, 90095 United States, Texas Brooke Army Medical Center Fort Sam Houston, Texas, United States, 78234 Cancer Therapy and Research Center San Antonio, Texas, United States, 78229 St. Luke's Lutheran Hospital San Antonio, Texas, United States, 78229 Veterans Affairs Medical Center - San Antonio (Murphy) San Antonio, Texas, United States, 78284 Collapse <<
NCT00055939	Sarcoma	Phase 2	Completed	-	United States, Colorado ... more >> University of Colorado Cancer Center at University of Colorado Health Sciences Center Denver, Colorado, United States, 80218 United States, Florida Nemours Children's Clinic Jacksonville, Florida, United States, 32207 United States, New Jersey Cancer Institute of New Jersey New Brunswick, New Jersey, United States, 08903 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 United States, Tennessee St. Jude Children's Research Hospital Memphis, Tennessee, United States, 38105 United States, Texas Medical City Dallas Hospital Dallas, Texas, United States, 75230 Simmons Cancer Center at University of Texas Southwestern Medical Center - Dallas Dallas, Texas, United States, 75390-9063 University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030-4009 Canada, Ontario Hospital for Sick Children Toronto, Ontario, Canada, M5G 1X8 Collapse <<
NCT00041236	Sarcoma	Phase 2	Completed	-	Belgium ... more >> Cliniques Universitaires Saint-Luc Brussels, Belgium, 1200 U.Z. Gasthuisberg Leuven, Belgium, B-3000 Denmark Aarhus University Hospital - Aarhus Sygehus - Norrebrogade Aarhus, Denmark, DK-8000 Germany Robert Roessle Comprehensive Cancer Center at University of Berlin - Charite Campus Buch Berlin, Germany, D-13122 Universitatsklinikum Carl Gustav Carl Carus Dresden, Germany, D-01307 Universitaetsklinikum Essen Essen, Germany, D-45122 Universitaets-Krankenhaus Eppendorf Hamburg, Germany, D-20246 Medizinische Hochschule Hannover Hannover, Germany, D-30625 Eberhard Karls Universitaet Tuebingen, Germany, D-72076 Slovakia National Cancer Institute - Bratislava Bratislava, Slovakia, 833 10 Collapse <<

依喜替康甲磺酸盐 Catalog No. CSN17998

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