169869-90-3,MFCD23102386
Catalog No.:AA00ABHC

169869-90-3 | Exatecan Mesylate

Pack Size
Purity
Availability
Price(USD)
Quantity
  
10mg
99%
in stock  
$78.00   $54.00
- +
25mg
99%
in stock  
$156.00   $109.00
- +
250mg
99%
in stock  
$173.00   $121.00
- +
500mg
99%
in stock  
$239.00   $167.00
- +
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
Technical Information
Catalog Number:
AA00ABHC
Chemical Name:
Exatecan Mesylate
CAS Number:
169869-90-3
Molecular Formula:
C25H26FN3O7S
Molecular Weight:
531.5532
MDL Number:
MFCD23102386
SMILES:
CS(=O)(=O)O.CC[C@@]1(O)C(=O)OCc2c1cc1c3nc4cc(F)c(c5c4c(c3Cn1c2=O)[C@@H](N)CC5)C
Properties
Computed Properties
 
Complexity:
1040  
Covalently-Bonded Unit Count:
2  
Defined Atom Stereocenter Count:
2  
Defined Bond Stereocenter Count:
0  
Formal Charge:
0  
Heavy Atom Count:
37  
Hydrogen Bond Acceptor Count:
10  
Hydrogen Bond Donor Count:
3  
Isotope Atom Count:
0  
Rotatable Bond Count:
1  
Undefined Atom Stereocenter Count:
0  
Undefined Bond Stereocenter Count:
0  

Downstream Synthesis Route
Exatecanmesylate 
  57294-38-9   
tert-butyl(4-(1S,9S)-9-ethyl-5-fluoro-9-hydroxy-4-methyl-10,13-dioxo-2,3,9,10,13,15-hexahydro-1H,12H-benzodepyrano3’,4’:6,7indolizino1,2-bquinolin-1-ylamino}-4-oxobutyl)carbamate 

[1]CurrentPatentAssignee:DAIICHISANKYOCOMPANY,LIMITED-WO2015/155998,2015,A1Locationinpatent:Paragraph0203;0204

[2]Nakada,Takashi;Masuda,Takeshi;Naito,Hiroyuki;Yoshida,Masao;Ashida,Shinji;Morita,Koji;Miyazaki,Hideki;Kasuya,Yuji;Ogitani,Yusuke;Yamaguchi,Junko;Abe,Yuki;Honda,Takeshi[BioorganicandMedicinalChemistryLetters,2016,vol.26,#6,p.1542-1545]

Literature

Title: Key role of topoisomerase I inhibitors in the treatment of recurrent and refractory epithelial ovarian carcinoma.

Journal: Expert review of anticancer therapy 20080501

Title: Relationship between drug release of DE-310, macromolecular prodrug of DX-8951f, and cathepsins activity in several tumors.

Journal: Biological & pharmaceutical bulletin 20071201

Title: Does consolidation with autologous stem cell transplantation improve the outcome of children with metastatic or relapsed Ewing sarcoma?

Journal: Pediatric blood & cancer 20070801

Title: Exatecan in pretreated adult patients with advanced soft tissue sarcoma: results of a phase II--study of the EORTC Soft Tissue and Bone Sarcoma Group.

Journal: European journal of cancer (Oxford, England : 1990) 20070401

Title: Quantitative acid hydrolysis of DE-310, a macromolecular carrier system for the camptothecin analog DX-8951f.

Journal: Journal of pharmaceutical and biomedical analysis 20070312

Title: Exatecan and gemcitabine: no better than gemcitabine only.

Journal: The Lancet. Oncology 20061101

Title: Randomized phase III study of exatecan and gemcitabine compared with gemcitabine alone in untreated advanced pancreatic cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20060920

Title: Chemotherapy for advanced pancreatic cancer.

Journal: Best practice & research. Clinical gastroenterology 20060401

Title: A phase II clinical and pharmacokinetic study of intravenous exatecan mesylate (DX-8951f) in patients with untreated metastatic gastric cancer.

Journal: Investigational new drugs 20051001

Title: DE-310, a macromolecular prodrug of the topoisomerase-I-inhibitor exatecan (DX-8951), in patients with operable solid tumors.

Journal: Investigational new drugs 20050801

Title: A Phase II study of intravenous exatecan administered daily for 5 days, every 3 weeks to patients with biliary tract cancers.

Journal: American journal of clinical oncology 20050801

Title: Chemotherapeutic gemcitabine doublets in pancreatic carcinoma.

Journal: Seminars in oncology 20050801

Title: Validation study of a method for assaying DE-310, a macromolecular carrier conjugate containing an anti-tumor camptothecin derivative, and the free drug in human plasma by HPLC and LC/MS/MS.

Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20050425

Title: A possible mechanism for the long-lasting antitumor effect of the macromolecular conjugate DE-310: mediation by cellular uptake and drug release of its active camptothecin analog DX-8951.

Journal: Cancer chemotherapy and pharmacology 20050401

Title: Validation study of a method for assaying DE-310, a macromolecular carrier conjugate containing an anti-tumor camptothecin derivative, and the free drug in tumor tissue by high performance liquid chromatography/atmospheric pressure chemical ionization tandem mass spectrometry.

Journal: Biomedical chromatography : BMC 20050101

Title: Combined coagulation phase-directed factor Xa inhibition with heparin compounds and DX-9065a - a direct and selective antagonist.

Journal: Thrombosis and haemostasis 20041201

Title: A phase IIA study of the topoisomerase I inhibitor, exatecan mesylate (DX-8951f), administered at two different dose schedules in patients with platinum- and taxane-resistant/refractory ovarian cancer.

Journal: Gynecologic oncology 20041001

Title: A predictive model of human myelotoxicity using five camptothecin derivatives and the in vitro colony-forming unit granulocyte/macrophage assay.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20041001

Title: Pharmacokinetics of DE-310, a novel macromolecular carrier system for the camptothecin analog DX-8951f, in tumor-bearing mice.

Journal: Die Pharmazie 20040501

Title: DE-310, a novel macromolecular carrier system for the camptothecin analog DX-8951f: potent antitumor activities in various murine tumor models.

Journal: Cancer science 20040201

Title: A phase II study of intravenous exatecan mesylate (DX-8951f) administered daily for 5 days every 3 weeks to patients with advanced ovarian, tubal or peritoneal cancer resistant to platinum, taxane and topotecan.

Journal: Cancer chemotherapy and pharmacology 20040101

Title: A phase II study of intravenous exatecan mesylate (DX-8951f) administered daily for five days every three weeks to patients with metastatic adenocarcinoma of the colon or rectum.

Journal: Investigational new drugs 20040101

Title: Are there any better camptothecins than the ones we have?

Journal: Clinical advances in hematology & oncology : H&O 20031001

Title: A Phase II study of intravenous exatecan mesylate (DX-8951f) administered daily for 5 days every 3 weeks to patients with metastatic breast carcinoma.

Journal: Cancer 20030901

Title: Phase II study of exatecan mesylate (DX-8951f) as first line therapy for advanced non-small cell lung cancer.

Journal: Lung cancer (Amsterdam, Netherlands) 20030801

Title: A Phase I and pharmocokinetic study of exatecan mesylate administered as a protracted 21-day infusion in patients with advanced solid malignancies.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20030701

Title: Phase I and pharmacokinetic study of the topoisomerase I inhibitor, exatecan mesylate (DX-8951f), using a weekly 30-minute intravenous infusion, in patients with advanced solid malignancies.

Journal: Annals of oncology : official journal of the European Society for Medical Oncology 20030601

Title: [A symphony for the camptothecins].

Journal: Bulletin du cancer 20030301

Title: Efficacy of camptothecin analog DX-8951f (Exatecan Mesylate) on human pancreatic cancer in an orthotopic metastatic model.

Journal: Cancer research 20030101

Title: The activity profile of the hexacyclic camptothecin derivative DX-8951f in experimental human colon cancer and ovarian cancer.

Journal: Biochemical pharmacology 20021015

Title: Induction of breast cancer resistance protein by the camptothecin derivative DX-8951f is associated with minor reduction of antitumour activity.

Journal: British journal of cancer 20020909

Title: Phase I and pharmacokinetic study of DX-8951f (exatecan mesylate), a hexacyclic camptothecin, on a daily-times-five schedule in patients with advanced leukemia.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20020701

Title: [Drug delivery systems for cancer chemotherapy].

Journal: Nihon Geka Gakkai zasshi 20020201

Title: O(6)-methylguanine-DNA methyltransferase (MGMT) as a determinant of resistance to camptothecin derivatives.

Journal: Japanese journal of cancer research : Gann 20020101

Title: Phase I study of topoisomerase I inhibitor exatecan mesylate (DX-8951f) given as weekly 24-hour infusions three of every four weeks.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20011201

Title: Validation study of assay method for DX-8951 and its metabolite in human plasma and urine by high-performance liquid chromatography/atmospheric pressure chemical ionization tandem mass spectrometry.

Journal: Biomedical chromatography : BMC 20010401

Title: Phase I and pharmacokinetic study of exatecan mesylate (DX-8951f): a novel camptothecin analog.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20010301

Title: High-Performance liquid chromatographic analysis of lactone and hydroxy acid of new antitumor drug, DX-8951 (exatecan), in mouse plasma.

Journal: Biological & pharmaceutical bulletin 20010201

Title: Morphological classification of dental lesions induced by various antitumor drugs in mice.

Journal: Toxicologic pathology 20010101

Title: Mitsui I, et al. A new water-soluble camptothecin derivative, DX-8951f, exhibits potent antitumor activity against human tumors in vitro and in vivo. Jpn J Cancer Res. 1995 Aug;86(8):776-82.

Title: Sun FX, et al. Efficacy of camptothecin analog DX-8951f (Exatecan Mesylate) on human pancreatic cancer in an orthotopic metastatic model. Cancer Res. 2003 Jan 1;63(1):80-5.

Title: Joto N, et al. DX-8951f, a water-soluble camptothecin analog, exhibits potent antitumor activity against a human lung cancer cell line and its SN-38-resistant variant. Int J Cancer. 1997 Aug 7;72(4):680-6.

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SDS
Tags:169869-90-3 Molecular Formula|169869-90-3 MDL|169869-90-3 SMILES|169869-90-3 Exatecan Mesylate
Catalog No.: AA00ABHC
169869-90-3,MFCD23102386
169869-90-3 | Exatecan Mesylate
Pack Size: 10mg
Purity: 99%
in stock
$78.00 $54.00
Pack Size: 25mg
Purity: 99%
in stock
$156.00 $109.00
Pack Size: 250mg
Purity: 99%
in stock
$173.00 $121.00
Pack Size: 500mg
Purity: 99%
in stock
$239.00 $167.00
Quantity
- +
Add to Card
Order Now
bulk Quotation Request
Technical Information
Catalog Number: AA00ABHC
Chemical Name: Exatecan Mesylate
CAS Number: 169869-90-3
Molecular Formula: C25H26FN3O7S
Molecular Weight: 531.5532
MDL Number: MFCD23102386
SMILES: CS(=O)(=O)O.CC[C@@]1(O)C(=O)OCc2c1cc1c3nc4cc(F)c(c5c4c(c3Cn1c2=O)[C@@H](N)CC5)C
Properties
Complexity: 1040  
Covalently-Bonded Unit Count: 2  
Defined Atom Stereocenter Count: 2  
Defined Bond Stereocenter Count: 0  
Formal Charge: 0  
Heavy Atom Count: 37  
Hydrogen Bond Acceptor Count: 10  
Hydrogen Bond Donor Count: 3  
Isotope Atom Count: 0  
Rotatable Bond Count: 1  
Undefined Atom Stereocenter Count: 0  
Undefined Bond Stereocenter Count: 0  
Downstream Synthesis Route
Exatecanmesylate 
  57294-38-9   
tert-butyl(4-(1S,9S)-9-ethyl-5-fluoro-9-hydroxy-4-methyl-10,13-dioxo-2,3,9,10,13,15-hexahydro-1H,12H-benzodepyrano3’,4’:6,7indolizino1,2-bquinolin-1-ylamino}-4-oxobutyl)carbamate 

[1]CurrentPatentAssignee:DAIICHISANKYOCOMPANY,LIMITED-WO2015/155998,2015,A1Locationinpatent:Paragraph0203;0204

[2]Nakada,Takashi;Masuda,Takeshi;Naito,Hiroyuki;Yoshida,Masao;Ashida,Shinji;Morita,Koji;Miyazaki,Hideki;Kasuya,Yuji;Ogitani,Yusuke;Yamaguchi,Junko;Abe,Yuki;Honda,Takeshi[BioorganicandMedicinalChemistryLetters,2016,vol.26,#6,p.1542-1545]

Literature fold

Title: Key role of topoisomerase I inhibitors in the treatment of recurrent and refractory epithelial ovarian carcinoma.

Journal: Expert review of anticancer therapy20080501

Title: Relationship between drug release of DE-310, macromolecular prodrug of DX-8951f, and cathepsins activity in several tumors.

Journal: Biological & pharmaceutical bulletin20071201

Title: Does consolidation with autologous stem cell transplantation improve the outcome of children with metastatic or relapsed Ewing sarcoma?

Journal: Pediatric blood & cancer20070801

Title: Exatecan in pretreated adult patients with advanced soft tissue sarcoma: results of a phase II--study of the EORTC Soft Tissue and Bone Sarcoma Group.

Journal: European journal of cancer (Oxford, England : 1990)20070401

Title: Quantitative acid hydrolysis of DE-310, a macromolecular carrier system for the camptothecin analog DX-8951f.

Journal: Journal of pharmaceutical and biomedical analysis20070312

Title: Exatecan and gemcitabine: no better than gemcitabine only.

Journal: The Lancet. Oncology20061101

Title: Randomized phase III study of exatecan and gemcitabine compared with gemcitabine alone in untreated advanced pancreatic cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology20060920

Title: Chemotherapy for advanced pancreatic cancer.

Journal: Best practice & research. Clinical gastroenterology20060401

Title: A phase II clinical and pharmacokinetic study of intravenous exatecan mesylate (DX-8951f) in patients with untreated metastatic gastric cancer.

Journal: Investigational new drugs20051001

Title: DE-310, a macromolecular prodrug of the topoisomerase-I-inhibitor exatecan (DX-8951), in patients with operable solid tumors.

Journal: Investigational new drugs20050801

Title: A Phase II study of intravenous exatecan administered daily for 5 days, every 3 weeks to patients with biliary tract cancers.

Journal: American journal of clinical oncology20050801

Title: Chemotherapeutic gemcitabine doublets in pancreatic carcinoma.

Journal: Seminars in oncology20050801

Title: Validation study of a method for assaying DE-310, a macromolecular carrier conjugate containing an anti-tumor camptothecin derivative, and the free drug in human plasma by HPLC and LC/MS/MS.

Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences20050425

Title: A possible mechanism for the long-lasting antitumor effect of the macromolecular conjugate DE-310: mediation by cellular uptake and drug release of its active camptothecin analog DX-8951.

Journal: Cancer chemotherapy and pharmacology20050401

Title: Validation study of a method for assaying DE-310, a macromolecular carrier conjugate containing an anti-tumor camptothecin derivative, and the free drug in tumor tissue by high performance liquid chromatography/atmospheric pressure chemical ionization tandem mass spectrometry.

Journal: Biomedical chromatography : BMC20050101

Title: Combined coagulation phase-directed factor Xa inhibition with heparin compounds and DX-9065a - a direct and selective antagonist.

Journal: Thrombosis and haemostasis20041201

Title: A phase IIA study of the topoisomerase I inhibitor, exatecan mesylate (DX-8951f), administered at two different dose schedules in patients with platinum- and taxane-resistant/refractory ovarian cancer.

Journal: Gynecologic oncology20041001

Title: A predictive model of human myelotoxicity using five camptothecin derivatives and the in vitro colony-forming unit granulocyte/macrophage assay.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research20041001

Title: Pharmacokinetics of DE-310, a novel macromolecular carrier system for the camptothecin analog DX-8951f, in tumor-bearing mice.

Journal: Die Pharmazie20040501

Title: DE-310, a novel macromolecular carrier system for the camptothecin analog DX-8951f: potent antitumor activities in various murine tumor models.

Journal: Cancer science20040201

Title: A phase II study of intravenous exatecan mesylate (DX-8951f) administered daily for 5 days every 3 weeks to patients with advanced ovarian, tubal or peritoneal cancer resistant to platinum, taxane and topotecan.

Journal: Cancer chemotherapy and pharmacology20040101

Title: A phase II study of intravenous exatecan mesylate (DX-8951f) administered daily for five days every three weeks to patients with metastatic adenocarcinoma of the colon or rectum.

Journal: Investigational new drugs20040101

Title: Are there any better camptothecins than the ones we have?

Journal: Clinical advances in hematology & oncology : H&O20031001

Title: A Phase II study of intravenous exatecan mesylate (DX-8951f) administered daily for 5 days every 3 weeks to patients with metastatic breast carcinoma.

Journal: Cancer20030901

Title: Phase II study of exatecan mesylate (DX-8951f) as first line therapy for advanced non-small cell lung cancer.

Journal: Lung cancer (Amsterdam, Netherlands)20030801

Title: A Phase I and pharmocokinetic study of exatecan mesylate administered as a protracted 21-day infusion in patients with advanced solid malignancies.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research20030701

Title: Phase I and pharmacokinetic study of the topoisomerase I inhibitor, exatecan mesylate (DX-8951f), using a weekly 30-minute intravenous infusion, in patients with advanced solid malignancies.

Journal: Annals of oncology : official journal of the European Society for Medical Oncology20030601

Title: [A symphony for the camptothecins].

Journal: Bulletin du cancer20030301

Title: Efficacy of camptothecin analog DX-8951f (Exatecan Mesylate) on human pancreatic cancer in an orthotopic metastatic model.

Journal: Cancer research20030101

Title: The activity profile of the hexacyclic camptothecin derivative DX-8951f in experimental human colon cancer and ovarian cancer.

Journal: Biochemical pharmacology20021015

Title: Induction of breast cancer resistance protein by the camptothecin derivative DX-8951f is associated with minor reduction of antitumour activity.

Journal: British journal of cancer20020909

Title: Phase I and pharmacokinetic study of DX-8951f (exatecan mesylate), a hexacyclic camptothecin, on a daily-times-five schedule in patients with advanced leukemia.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research20020701

Title: [Drug delivery systems for cancer chemotherapy].

Journal: Nihon Geka Gakkai zasshi20020201

Title: O(6)-methylguanine-DNA methyltransferase (MGMT) as a determinant of resistance to camptothecin derivatives.

Journal: Japanese journal of cancer research : Gann20020101

Title: Phase I study of topoisomerase I inhibitor exatecan mesylate (DX-8951f) given as weekly 24-hour infusions three of every four weeks.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research20011201

Title: Validation study of assay method for DX-8951 and its metabolite in human plasma and urine by high-performance liquid chromatography/atmospheric pressure chemical ionization tandem mass spectrometry.

Journal: Biomedical chromatography : BMC20010401

Title: Phase I and pharmacokinetic study of exatecan mesylate (DX-8951f): a novel camptothecin analog.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology20010301

Title: High-Performance liquid chromatographic analysis of lactone and hydroxy acid of new antitumor drug, DX-8951 (exatecan), in mouse plasma.

Journal: Biological & pharmaceutical bulletin20010201

Title: Morphological classification of dental lesions induced by various antitumor drugs in mice.

Journal: Toxicologic pathology20010101

Title: Mitsui I, et al. A new water-soluble camptothecin derivative, DX-8951f, exhibits potent antitumor activity against human tumors in vitro and in vivo. Jpn J Cancer Res. 1995 Aug;86(8):776-82.

Title: Sun FX, et al. Efficacy of camptothecin analog DX-8951f (Exatecan Mesylate) on human pancreatic cancer in an orthotopic metastatic model. Cancer Res. 2003 Jan 1;63(1):80-5.

Title: Joto N, et al. DX-8951f, a water-soluble camptothecin analog, exhibits potent antitumor activity against a human lung cancer cell line and its SN-38-resistant variant. Int J Cancer. 1997 Aug 7;72(4):680-6.

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