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S81006

Galeterone

源叶(MedMol) ≥98%
  • 英文名:
  • Galeterone
  • 别名:
  • VN124-1;(3S,10R,13S)-17-(1H-benzo[d]imidazol-1-yl)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol
  • CAS号:
  • 851983-85-2
  • 分子式:
  • C26H32N2O
  • 分子量:
  • 388.56
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S81006-5mg ≥98% ¥500.00元 5 - - - EA 加入购物车
源叶(MedMol) S81006-25mg ≥98% ¥900.00元 6 - - - EA 加入购物车
源叶(MedMol) S81006-100mg ≥98% ¥2000.00元 8 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).
  • 靶点: IC50: 47 nM (CYP17);P450; AndrogenReceptor
  • 体内研究:
    Mice inoculated with LAPC-4 tumors are treated subcutaneously with 0.15 mmol/kg of Galeterone (TOK-001) twice daily. Mice treated with TOK-001 have smaller average tumor volume on day 31 when compared to control (p= 0.0001). Galeterone (TOK-001) treatment also significantly reduces the growth rate of tumor growth compared to control (p<0.0001). Upon excision, final tumor weights are also significantly reduced in animals treated with Galeterone (TOK-001) compared to animals treated with control, and castration (p<0.05)
  • 参考文献:
    1. Bruno RD, et al. Synthesis and biological evaluations of putative metabolically stable analogs of VN/124-1 (TOK-001): head to head anti-tumor efficacy evaluation of VN/124-1 (TOK-001) and abiraterone in LAPC-4 human prostate cancer xenograft model.Steroid 2. DeVore NM, et al. Structures of cytochrome P450 17A1 with prostate cancer drugs abiraterone and TOK-001.Nature. 2012 Jan 22;482(7383):116-9. 3. Soifer HS, et al. Direct regulation of androgen receptor activity by potent CYP17 inhibitors in prostate cancer cells.J Biol Chem. 2012 Feb 3;287(6):3777-87. Epub 2011 Dec 15.
  • 溶解性: DMSO  :  25  mg/mL  (64.34  mM;  Need  ultrasonic)
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.574 ml 12.868 ml 25.736 ml
    5 mM 0.515 ml 2.574 ml 5.147 ml
    10 mM 0.257 ml 1.287 ml 2.574 ml
    50 mM 0.051 ml 0.257 ml 0.515 ml
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