GlpBio

Pracinostat (SB939)

目录号: GC16734纯度: >99.50%同义词: (2E)-3-[2-丁基-1-[2-(二乙基氨基)乙基]-1H-苯并咪唑-5-基]-N-羟基丙烯酰胺,SB-939, SB 939

A pan-HDAC inhibitor

Pracinostat (SB939)
Cas No.: 929016-96-6
规格价格库存数量操作
5mg¥788.00现货
1
10mg¥1,512.00现货
1
50mg¥4,316.00现货
1
10mM (in 1mL DMSO)¥998.00现货
1
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文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
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    641, 529–536 (2025)
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    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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    31, 1291–1307 (2021)

产品描述 Description

Pracinostat, also known as SB939, is a potent and orally available inhibitor of histone deacetylase (HDAC) with a relatively stronger selectivity (more than 1000-fold) for class I, class II and class IV HDACs rather than class III HDACs. Pracinostat potently suppresses proliferation in a wide range of cancer cell lines, including colon cancer, ovarian cancer, prostate carcinomas, acute myeloid leukaemia (AML) and B cell lymphoma. Recent study results have shown that SB939 induces the accumulation of acetylated histone H3 (AcH3) and acetylated α-tubulin and increases the expression of the cyclin dependent kinase inhibitor p21 in cancer cells.

Reference

[1].Razak AR, Hotte SJ, Siu LL, Chen EX, Hirte HW, Powers J, Walsh W, Stayner LA, Laughlin A, Novotny-Diermayr V, Zhu J, Eisenhauer EA. Phase I clinical, pharmacokinetic and pharmacodynamic study of SB939, an oral histone deacetylase (HDAC) inhibitor, in patients with advanced solid tumours. Br J Cancer. 2011;104(5):756-762.

实验参考方法 Experimental Reference Method

Cell experiment:

Cell lines

Ovarian (A2780) , colon (HCT-116), and prostate (PC-3) cell lines

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

96 h; IC50=0.48±0.21 μM (A2780), 0.48±0.27 μM (HCT-116), 0.34±0.06 μM (PC-3)

Applications

SB939 showed broad anti-proliferative activity against representative tumor cells from ovarian (A2780) , colon (HCT-116), and prostate (PC-3) with cellular IC50 values of 0.48±0.21, 0.48±0.27 and 0.34±0.06 μM, respectively.
Animal experiment:

Animal models

Athymic nude mice

Dosage form

200 mg/kg, 100 mg/kg, 50 mg/kg; oral taken.

Applications

SB939 was clearly toxic at the highest dose tested (200 mg/kg); however, at the MTD dose of 100 mg/kg and at 50mg/kg, it demonstrated very significant antitumor effects on day 21 with TGI = 90% (p < 0.001 ) and 66% ( p < 0.001), respectively, with acceptable body weight loss.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Wang H, Yu N, Chen D, et al. Discovery of (2 E)-3-{2-butyl-1-[2-(diethylamino) ethyl]-1 H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile[J]. Journal of medicinal chemistry, 2011, 54(13): 4694-4720.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
929016-96-6
同义词
(2E)-3-[2-丁基-1-[2-(二乙基氨基)乙基]-1H-苯并咪唑-5-基]-N-羟基丙烯酰胺,SB-939, SB 939
化学名
(E)-3-[2-butyl-1-[2-(diethylamino)ethyl]benzimidazol-5-yl]-N-hydroxyprop-2-enamide
SMILES
CCCCC1=NC2=C(N1CCN(CC)CC)C=CC(=C2)C=CC(=O)NO
分子式
C20H30N4O2
分子量
358.48 g/mol
溶解性
≥ 11.4 mg/mL in DMSO, ≥ 24.8 mg/mL in EtOH with ultrasonic
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol