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S81235

3-Deazaneplanocin A Hydrochloride

源叶(MedMol) 96%
  • 英文名:
  • 3-Deazaneplanocin A Hydrochloride
  • 别名:
  • 3-Deazaneplanocin A (DZNep) hydrochloride; CS-0870; 3-deazaneplanocin A (DZNeP) HCl; 3-Deazaneplanocin A hydrochloride;
  • CAS号:
  • 120964-45-6
  • 分子式:
  • C12H15ClN4O3
  • 分子量:
  • 298.73
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源叶(MedMol) S81235-1mg 96% ¥476.00元 2 - - - EA 加入购物车
源叶(MedMol) S81235-5mg 96% ¥1496.00元 2 - - - EA 加入购物车
源叶(MedMol) S81235-10mg 96% ¥2856.00元 4 - - - EA 加入购物车
源叶(MedMol) S81235-25mg 96% ¥5440.00元 2 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: 3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities
  • 靶点: Histone Methyltransferase;Orthopoxvirus;Others; HistoneMethyltransferase
  • 体内研究:
    The survival of NOD/SCID mice with acute myeloid leukemia (AML) due to HL-60 cells is significantly higher, if treated with 3-Deazaneplanocin A (DZNep) and LBH589 (PS) compare to treatment with PS, 3-Deazaneplanocin A, or vehicle alone (P<0.05). Median survival is as follows: control, 36 days; PS, 42 days; 3-Deazaneplanocin A, 43 days; and 3-Deazaneplanocin A plus PS, 52 days. There is a progressive increase in weight of rats treated with physiological saline in a time-dependent manner (the mean growth rate=3.19% per day). Administration of 20 mg/kg 3-Deazaneplanocin A (DZNep) not only markedly reduces the relative weight of the rats compare to the initial weight (−2.0%, −4.9% and −1.2%) in the first three days post-treatment, but also suppresses the weight growth rate to 2.6% per day from the fourth day onwards post-dose
  • 参考文献:
    1. Fiskus W, et al. Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor LBH589 against human AML cells. Blood, 2009, 114(13), 2733-2743. 2. Avan A, et al. Molecular mechanisms involved in the synergistic interaction of the EZH2 inhibitor 3-deazaneplanocin A with LY 188011 in pancreatic cancer cells. Mol Cancer Ther. 2012 Aug;11(8):1735-46. 3. Kikuchi J, et al. Epigenetic therapy with 3-deazaneplanocin A, an inhibitor of the histone methyltransferase EZH2, inhibits growth of non-small cell lung cancer cells. Lung Cancer. 2012 Nov;78(2):138-43. 4. Sun F, et al. Preclinical pharmacokinetic studies of 3-deazaneplanocin A, a potent epigenetic anticancer agent, and its human pharmacokinetic prediction using GastroPlus?. Eur J Pharm Sci. 2015 Sep 18;77:290-302. 5. Noriko Uchiyama, et al. Aristeromycin and DZNeP cause growth inhibition of prostate cancer via induction of mir-26a. Eur J Pharmacol. 2017 Oct 5;812:138-146. 6. Robert O Baker, et al. Potential antiviral therapeutics for smallpox, monkeypox and other orthopoxvirus infections. Antiviral Res. 2003 Jan;57(1-2):13-23.
  • 溶解性: H2O  :  50  mg/mL  (167.38  mM;  Need  ultrasonic)
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 3.348 ml 16.738 ml 33.475 ml
    5 mM 0.67 ml 3.348 ml 6.695 ml
    10 mM 0.335 ml 1.674 ml 3.348 ml
    50 mM 0.067 ml 0.335 ml 0.67 ml
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