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• 产品描述： Pracinostat is a potent histone deacetylase (HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research. Pracinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC50 below 10 nM

• 靶点： HDAC10:40 nM (IC50);HDAC3:43 nM (IC50);HDAC5:47 nM (IC50);HDAC1:49 nM (IC50);HDAC4;56 nM (IC50);HDAC9:70 nM (IC50);HDAC11:93 nM (IC50);HDAC2:96 nM (IC50);HDAC7:137 nM (IC50);HDAC8:140 nM (IC50);HDAC6:1008 nM (IC50);MBLAC2:<10 nM (EC50)

• 体内研究：
  Pracinostat (SB939, 25-100 mg/kg) shows significant dose-dependent growth inhibition of HCT-116 xenografts. SB939 selectively accumulates in tumor tissue. SB939 (50 or 75 mg/kg) exhibits anti-tumor activities in the Apcmin genetic colon cancer mouse model. Pracinostat (25 or 50 mg/kg per day for 21 days) induces significant inhibition of tumor growth (TGI), by 59 and 116%, respectively, in mice bearing MV4-11 xenografts. Pracinostat (75 mg/kg, q.o.d) in combination with pacritinib is efficacious and synergistic in vivo in two different models of human AML. Pracinostat and pacritinib have synergistic effects on AML-induced plasma cytokines/growth factors/chemokines.

• 参考文献：
  1. Novotny-Diermayr V, et al. SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer. Mol Cancer Ther. 2010 Mar;9(3):642-52. 2. Wang H, et al. Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. J Med Chem. 2011 Jul 14;54(13):4694-720. 3. Novotny-Diermayr V, et al. The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML. Blood Cancer J. 2012 May;2(5):e69. 4. Lechner S, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Aug;18(8):812-820.

• 溶解性： DMSO  :  250  mg/mL  (697.39  mM;  Need  ultrasonic)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.79 ml	13.948 ml	27.896 ml
  5 mM	0.558 ml	2.79 ml	5.579 ml
  10 mM	0.279 ml	1.395 ml	2.79 ml
  50 mM	0.056 ml	0.279 ml	0.558 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

• 1. [IF=4.8] Jiazhen Huang et al."ALDH1A3 contributes to tumorigenesis in high-grade serous ovarian cancer by epigenetic modification."CELLULAR SIGNALLING.2024 Apr;116:111044

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *