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Etacstil_155701-61-4_产品详情
155701-61-4
  • names:

    (E)-3-(4-((E)-1,2-diphenylbut-1-en-1-yl)phenyl)acrylic acid

  • CAS号:

    155701-61-4

    MDL Number:
  • MF(分子式): C25H22O2 MW(分子量): 354.449
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
Etacstil
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中文别名 Etacstil
英文别名 GW5638; GW-5638; GW 5638; DPC974; DPC-974; DPC 974; Etacstil.
CAS号 155701-61-4
Inchi InChI=1S/C25H22O2/c1-2-23(20-9-5-3-6-10-20)25(21-11-7-4-8-12-21)22-16-13-19(14-17-22)15-18-24(26)27/h3-18H,2H2,1H3,(H,26,27)/b18-15+,25-23+
InchiKey HJQQVNIORAQATK-LXFXVVTESA-N
分子式 Formula C25H22O2
分子量 Molecular Weight 354.449
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 Etacstil(CAS:155701-61-4):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。
IntroductionEtacstil, also known as GW5638 and DPC974, is a estrogen receptor ligand. Similar to tamoxifen, GW5638 is considered as a prodrug of its active metabolite GW7604. GW5638 appears to function as an antagonist in these in vitro systems, although in a manner distinct from other known ER modulators. GW5638 is also classified as a pseudo-SERD, which could form the basis of a new paradigm of breast cancer hormonal therapy in its own right.
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备注
[1]Laxmi YR, Liu X, Suzuki N, Kim SY, Okamoto K, Kim HJ, Zhang G, Chen JJ, Okamoto Y, Shibutani S. Anti-breast cancer potential of SS1020, a novel antiestrogen lacking estrogenic and genotoxic actions. Int J Cancer. 2010 Oct 1;127(7):1718-26. doi: 10.1002/ijc.25167. PubMed PMID: 20073065.
[2]Wittmann BM, Sherk A, McDonnell DP. Definition of functionally important mechanistic differences among selective estrogen receptor down-regulators. Cancer Res. 2007 Oct 1;67(19):9549-60. PubMed PMID: 17909066.
[3] Fan M, Rickert EL, Chen L, Aftab SA, Nephew KP, Weatherman RV. Characterization of molecular and structural determinants of selective estrogen receptor downregulators. Breast Cancer Res Treat. 2007 May;103(1):37-44. PubMed PMID: 17033922.
[4] Tong S, Chen Q, Shan SQ, Dewhirst MW, Yuan F. Quantitative comparison of the inhibitory effects of GW5638 and tamoxifen on angiogenesis in the cornea pocket assay. Angiogenesis. 2006;9(2):53-8. PubMed PMID: 16622786.
[5] Ariazi EA, Ariazi JL, Cordera F, Jordan VC. Estrogen receptors as therapeutic targets in breast cancer. Curr Top Med Chem. 2006;6(3):181-202. Review. PubMed PMID: 16515478.
6: Wu YL, Yang X, Ren Z, McDonnell DP, Norris JD, Willson TM, Greene GL. Structural basis for an unexpected mode of SERM-mediated ER antagonism. Mol Cell. 2005 May 13;18(4):413-24. PubMed PMID: 15893725.7: Farnell YZ, Ing NH. Myometrial effects of selective estrogen receptor modulators on estradiol-responsive gene expression are gene and cell-specific. J Steroid Biochem Mol Biol. 2003 Apr;84(5):527-36. PubMed PMID: 12767277.8: Farnell YZ, Ing NH. Endometrial effects of selective estrogen receptor modulators (SERMs) on estradiol-responsive gene expression are gene and cell-specific. J Steroid Biochem Mol Biol. 2003 Apr;84(5):513-26. PubMed PMID: 12767276.9: Dardes RC, O'Regan RM, Gajdos C, Robinson SP, Bentrem D, De Los Reyes A, Jordan VC. Effects of a new clinically relevant antiestrogen (GW5638) related to tamoxifen on breast and endometrial cancer growth in vivo. Clin Cancer Res. 2002 Jun;8(6):1995-2001. PubMed PMID: 12060645.10: Gutman M, Couillard S, Roy J, Labrie F, Candas B, Labrie C. Comparison of the effects of EM-652 (SCH57068), tamoxifen, toremifene, droloxifene, idoxifene, GW-5638 and raloxifene on the growth of human ZR-75-1 breast tumors in nude mice. Int J Cancer. 2002 May 10;99(2):273-8. PubMed PMID: 11979444.1
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