| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S81112-1mg买3赠1 |
98.70% | ￥140.00 |
9 | - | - | - | - |
|
S81112-2mg买3赠1 |
98.70% | ￥200.00 |
9 | - | - | - | - |
|
S81112-5mg买3赠1 |
98.70% | ￥310.00 |
>10 | - | - | - | - |
|
S81112-10mg买3赠1 |
98.70% | ￥500.00 |
10 | - | - | - | - |
|
S81112-50mg促销 |
98.70% | ￥780.00 ￥624.00 |
10 | - | - | - | - |
|
S81112-25mg买3赠1 |
98.70% | ￥680.00 |
9 | - | - | - | - |
|
| 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 | ||||||||||||||||||||
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| 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);Apoptosis; HDAC | ||||||||||||||||||||
| 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： |
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| 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。 |
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