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219923-05-4
  • names:

    (5S)-5-acetamido-9,10,11-trimethoxy-6,7-dihydro-5H-dibenzo[a,c][7]annulen-3-yl dihydrogen phosphate

  • CAS号:

    219923-05-4

    MDL Number:
  • MF(分子式): C20H24NO8P MW(分子量): 437.38
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
AZD-6126
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中文别名 AZD-6126
英文别名 AZD6126; AZD 6126; AZD-6126; ANG453; ANG-453; ANG 453.
CAS号 219923-05-4
SMILES O=P(O)(OC1=CC=C(C2=C(OC)C(OC)=C(OC)C=C2CC[C@@H]3NC(C)=O)C3=C1)O
Inchi InChI=1S/C20H24NO8P/c1-11(22)21-16-8-5-12-9-17(26-2)19(27-3)20(28-4)18(12)14-7-6-13(10-15(14)16)29-30(23,24)25/h6-7,9-10,16H,5,8H2,1-4H3,(H,21,22)(H2,23,24,25)/t16-/m0/s1
InchiKey UGBMEXLBFDAOGL-INIZCTEOSA-N
分子式 Formula C20H24NO8P
分子量 Molecular Weight 437.38
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
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 AZD-6126(CAS:219923-05-4):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。
IntroductionAZD6126, also known as ANG-453, a water-soluble phosphate prodrug of N-acetylcolchinol with potential antiangiogenesis and antineoplastic activities. AZD-6126 is an angiogenesis inhibitor and tubulin inhibitor potentially for the treatment of solid tumours. AZD6126 is converted in vivo into N-acetylcolchinol. N-acetylcolchinol binds to and destabilizes the tubulin cytoskeleton of endothelial cells in tumor blood vessels, which may result in tumor endothelial cel apoptosis, the selective occlusion of tumor blood vessels, cessation of tumor blood flow, and tumor necrosis.
Application1
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危险性警示
安全声明
安全防护
备注
[1]Eichhorn ME, Klotz LV, Luedemann S, Strieth S, Kleespies A, Preissler G, Lindner M, Jauch KW, Reiser MF, Clevert DA. Vascular targeting tumor therapy: Non-invasive contrast enhanced ultrasound for quantitative assessment of tumor microcirculation. Cancer Biol Ther. 2010 May 8;9(10). [Epub ahead of print] PubMed PMID: 20234173.
[2]Wang H, Li J, Chen F, De Keyzer F, Yu J, Feng Y, Nuyts J, Marchal G, Ni Y. Morphological, functional and metabolic imaging biomarkers: assessment of vascular-disrupting effect on rodent liver tumours. Eur Radiol. 2010 Aug;20(8):2013-26. Epub 2010 Feb 25. PubMed PMID: 20182730.
[3] Elice F, Rodeghiero F, Falanga A, Rickles FR. Thrombosis associated with angiogenesis inhibitors. Best Pract Res Clin Haematol. 2009 Mar;22(1):115-28. Review. PubMed PMID: 19285278.
[4] Fens MH, Hill KJ, Issa J, Ashton SE, Westwood FR, Blakey DC, Storm G, Ryan AJ, Schiffelers RM. Liposomal encapsulation enhances the antitumour efficacy of the vascular disrupting agent ZD6126 in murine B16.F10 melanoma. Br J Cancer. 2008 Oct 21;99(8):1256-64. Epub 2008 Sep 16. PubMed PMID: 18797467; PubMed Central PMCID: PMC2570501.
[5] Valentini G, D'Andrea C, Ferrari R, Pifferi A, Cubeddu R, Martinelli M, Natoli C, Ubezio P, Giavazzi R. In vivo measurement of vascular modulation in experimental tumors using a fluorescent contrast agent. Photochem Photobiol. 2008 Sep-Oct;84(5):1249-56. Epub 2008 Apr 12. PubMed PMID: 18422875.
6: Partridge EA, D'Souza RA, Lenz EM, Smith SM, Clarkson-Jones J, Roberts DW. Disposition and metabolism of the colchicine derivative [14C]-ZD6126 in rat and dog. Xenobiotica. 2008 Apr;38(4):399-421. PubMed PMID: 18340564.7: Cai SX. Small molecule vascular disrupting agents: potential new drugs for cancer treatment. Recent Pat Anticancer Drug Discov. 2007 Jan;2(1):79-101. Review. PubMed PMID: 18221055.8: LoRusso PM, Gadgeel SM, Wozniak A, Barge AJ, Jones HK, DelProposto ZS, DeLuca PA, Evelhoch JL, Boerner SA, Wheeler C. Phase I clinical evaluation of ZD6126, a novel vascular-targeting agent, in patients with solid tumors. Invest New Drugs. 2008 Apr;26(2):159-67. Epub 2008 Jan 25. PubMed PMID: 18219445.9: Gould S, Westwood FR, Curwen JO, Ashton SE, Roberts DW, Lovick SC, Ryan AJ. Effect of pretreatment with atenolol and nifedipine on ZD6126-induced cardiac toxicity in rats. J Natl Cancer Inst. 2007 Nov 21;99(22):1724-8. Epub 2007 Nov 13. PubMed PMID: 18000220.10: Mocanu JD, Yip KW, Skliarenko J, Shi W, Busson P, Lo KW, Bastianutto C, Liu FF. Imaging and modulating antisense microdistribution in solid human xenograft tumor models. Clin Cancer Res. 2007 Oct 1;13(19):5935-41. PubMed PMID: 17908990.
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