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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
SMILES O=C(O)/C=C/C1=CC=C(/C(C2=CC=CC=C2)=C(C3=CC=CC=C3)\CC)C=C1
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
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 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.
Application1
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警示图
危险性 Warning
危险性警示
安全声明
安全防护
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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