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Losoxantrone_88303-60-0_产品详情
88303-60-0
  • names:

    7-Hydroxy-2-[2-(2-hydroxyethylamino)ethyl]-5-[2-(2-hydroxyethylamino)ethylamino]anthra[1,9-cd]pyrazol-6(2H)-one

  • CAS号:

    88303-60-0

    MDL Number:
  • MF(分子式): C22H27N5O4 MW(分子量): 425.48088
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
Losoxantrone
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中文别名 Losoxantrone
英文别名 Losoxantrone; Biantrazole; CI941; DuP941.
CAS号 88303-60-0
Inchi InChI=1S/C22H27N5O4/c28-12-9-23-6-7-25-15-4-5-16-20-19(15)22(31)18-14(2-1-3-17(18)30)21(20)26-27(16)11-8-24-10-13-29/h1-5,23-25,28-30H,6-13H2
InchiKey YROQEQPFUCPDCP-UHFFFAOYSA-N
分子式 Formula C22H27N5O4
分子量 Molecular Weight 425.48088
溶解度Solubility
性状 Solid powder
储藏条件 Storage conditions Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).
产品说明 Losoxantrone(CAS:88303-60-0):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。
IntroductionLosoxantrone is a DNA intercalator that was developed with the potential to replace anthracyclines. Losoxantrone is also a bioreductive drugs. In phase II trials, losoxantrone demonstrated a partial biochemical response rate of 25%, response in measurable disease sites in 22%, and improvement in clinical symptoms in one-third of patients.
Application1
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[1]Liang H, Wu X, Guziec LJ, Guziec FS Jr, Larson KK, Lang J, Yalowich JC, Hasinoff BB. A structure-based 3D-QSAR study of anthrapyrazole analogues of the anticancer agents losoxantrone and piroxantrone. J Chem Inf Model. 2006 Jul-Aug;46(4):1827-35. PubMed PMID: 16859314.
[2]Renner UD, Piperopoulos G, Gebhardt R, Ehninger G, Zeller KP. The oxidative biotransformation of losoxantrone (CI-941). Drug Metab Dispos. 2002 Apr;30(4):464-78. PubMed PMID: 11901102.
[3] Goh BC, Vokes EE, Joshi A, Ratain MJ. Phase I study of the combination of losoxantrone and cyclophosphamide in patients with refractory solid tumours. Br J Cancer. 2002 Feb 12;86(4):534-9. PubMed PMID: 11870533; PubMed Central PMCID: PMC2375276.
[4] Joshi AS, Pieniaszek HJ Jr, Vokes EE, Vogelzang NJ, Davidson AF, Richards LE, Chai MF, Finizio M, Ratain MJ. Elimination pathways of [14C]losoxantrone in four cancer patients. Drug Metab Dispos. 2001 Feb;29(2):96-9. PubMed PMID: 11159796.
[5] Huan SD, Natale RB, Stewart DJ, Sartiano GP, Stella PJ, Roberts JD, Symes AL, Finizio M. A multicenter phase II trial of losoxantrone (DuP-941) in hormone-refractory metastatic prostate cancer. Clin Cancer Res. 2000 Apr;6(4):1333-6. PubMed PMID: 10778959.
6: Hasinoff BB, Tran KT. The displacement of iron(III) from its complexes with the anticancer drugs piroxantrone and losoxantrone by the hydrolyzed form of the cardioprotective agent dexrazoxane. J Inorg Biochem. 1999 Nov-Dec;77(3-4):257-9. PubMed PMID: 10643663.7: Diab SG, Baker SD, Joshi A, Burris HA, Cobb PW, Villalona-Calero MA, Eckhardt SG, Weiss GR, Rodriguez GI, Drengler R, Kraynak M, Hammond L, Finizio M, Von Hoff DD, Rowinsky EK. A phase I and pharmacokinetic study of losoxantrone and paclitaxel in patients with advanced solid tumors. Clin Cancer Res. 1999 Feb;5(2):299-308. PubMed PMID: 10037178.8: Herman EH, Zhang J, Hasinoff BB, Tran KT, Chadwick DP, Clark JR Jr, Ferrans VJ. Comparison of the chronic toxicity of piroxantrone, losoxantrone and doxorubicin in spontaneously hypertensive rats. Toxicology. 1998 Jun 26;128(1):35-52. PubMed PMID: 9704904.9: Shea JA, Shamrock WF, Abboud CA, Woodeshick RW, Nguyen LQ, Rubino JT, Segretario J. Validation of cleaning procedures for highly potent drugs. I. Losoxantrone. Pharm Dev Technol. 1996 Apr;1(1):69-75. PubMed PMID: 9552333.10: Richards LE, Sun JH. Identification of two regioisomeric monocarboxylic acid metabolites of losoxantrone (DuP 941; Biantrazole) excreted in human urine. Drug Metab Dispos. 1995 May;23(5):600-2. PubMed PMID: 7587938.1
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