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Pracinostat

SB939,SB 939,SB-939

Pracinostat是广泛的HDAC抑制剂，对HDAC1，3，4，5,9,和10的IC50分别是49 nM，43 nM，56 nM，47 nM，70 nM和40 nM。

目录号
EY0713
EY0713
EY0713
EY0713
纯度
99.15%
99.15%
99.15%
99.15%
规格
1 mg
5 mg
25 mg
50 mg
原价
420
980
2600
3986.00
售价
420
980
2600
3986.00
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Phase 2.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    1.5 nM -100 μM.

  • 动物实验

    25, 50, 75, 或100 mg/kg. 口服饲喂或者静脉注射处理

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Novotny-Diermayr V, et al. Mol Cancer Ther, 2010, 9(3), 642-652.
    [2] Wang H et al. Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylami de (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. J Med Chem. 2011 Jul 14;54(13):4694-720.
    [3] Jayaraman R, Pilla Reddy V, Pasha MK, Wang H, Sangthongpitag K, Yeo P, Hu CY, Wu X, Xin L, Goh E, New LS, Ethirajulu K. Preclinical metabolism and disposition of SB939 (Pracinostat), an orally active histone deacetylase inhibitor, and prediction of human pharmacokinetics. Drug Metab Dispos. 2011 Dec;39(12):2219-32.

    分子式
    C20H30N4O2    		 分子量
    358.48    		 CAS号
    929016-96-6    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    ≥70 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    ≥20 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01912274 Acute Myeloid Leukemia Drug: pracinostat with azacitadine Helsinn Healthcare SA Phase 2 2013-10-01 2017-02-23
    NCT02118909 Healthy Volunteers|Non-smokers Drug: Pracinostat|Drug: Itraconazole|Drug: Ciprofloxacin Helsinn Healthcare SA Phase 1 2014-05-01 2017-02-22
    NCT02058784 Healthy Volunteers|Moderate to Heavy Smokers|Non-smokers Drug: pracinostat Helsinn Healthcare SA|Celerion Early Phase 1 2014-02-01 2017-02-22
    NCT02267278 Myeloproliferative Diseases Drug: Ruxolitinib|Drug: Pracinostat|Behavioral: Questionnaire M.D. Anderson Cancer Center|MEI Pharma, Inc. Phase 2 2015-01-12 2017-01-24
    NCT01993641 Myelodysplastic Syndrome|MDS Drug: pracinostat|Drug: Azacitidine|Drug: Decitabine Helsinn Healthcare SA Phase 2 2013-12-01 2017-02-22
    NCT01873703 Myelodysplastic Syndrome Drug: pracinostat|Drug: Placebo|Drug: Azacitidine Helsinn Healthcare SA Phase 2 2013-06-01 2017-02-22
    NCT01112384 Metastatic Sarcoma Drug: SB939 NCIC Clinical Trials Group|Canadian Cancer Trials Group Phase 2 2010-03-01 2016-11-25
    NCT00741234 Solid Tumors|Hematologic Malignancies|Myelodysplastic Syndrome Drug: SB939|Drug: Azacitidine S*BIO Phase 1 2007-04-01 2012-04-19
    NCT01075308 Prostate Cancer Drug: HDAC inhibitor SB939 NCIC Clinical Trials Group|Canadian Cancer Trials Group Phase 2 2010-02-01 2015-07-10
    NCT01200498 Myeloproliferative Disorders Drug: SB939 M.D. Anderson Cancer Center|S*BIO Phase 2 2010-11-01 2013-12-13
    NCT01184274 Leukemia|Solid Tumours Drug: SB939 NCIC Clinical Trials Group|Canadian Cancer Trials Group Phase 1 2010-09-01 2014-01-16
    NCT00504296 Unspecified Adult Solid Tumor, Protocol Specific Drug: HDAC inhibitor SB939|Other: immunoenzyme technique|Other: immunohistochemistry staining method|Other: immunologic technique|Other: laboratory biomarker analysis|Other: liquid chromatography|Other: mass spectrometry|Other: pharmacological study NCIC Clinical Trials Group|Canadian Cancer Trials Group Phase 1 2007-06-01 2012-05-31

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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