Home > HDAC & HDAC & HDAC & > Romidepsin

Romidepsin

罗米地辛,FR-901228,NSC-630176,FK-228,Depsipeptide

Romidepsin (FK228, Depsipeptide)是一种HDAC1和HDAC2抑制剂，IC50分别为36 nM和47 nM。

目录号
EY1745
EY1745
EY1745
纯度
99.64%
99.64%
99.64%
规格
1 mg
5 mg
10 mg
原价
960
2800
4765
售价
960
2800
4765
库存
现货
现货
现货
订购
订购
订购
订购
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  • 生物活性

    Romidepsin, also known as FK228 or depsipeptide, is potent and selective inhibitor of histone deacetylases (HDACs) which are associated with the regulation of re-expression of silenced tumor suppressor genes. It was the first HDAC inhibitor to manifest anti-tumor activity and originally isolated from a rod-shaped Gram-negative bacterium, Chromobacterium violaceum, found in a Japanese soil sample. Romidepsin exhibits a stronger inhibition towards HDAC1 and HDAC2 enzymes (class I), removing acetyl groups from the lysine residues of N-terminal histone tails and maintaining a more open and transcriptionally active chromatin state, than HDAC4 and HDAC6 enzymes (class II). Besides HDAC inhibition, romidepsin is also able to induce cell cycle arrest, cellular differentiation, apoptosis and alteration of gene expression in adult malignancies.

  • 体外研究

  • 体内研究

    1% DMSO+30% polyethylene glycol+1% Tween 80

  • 激酶实验

  • 细胞实验

    1 ng/mL

  • 动物实验

    1.2 mg/kg 腹腔注射

  • 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] Furumai R, et al. Cancer Res, 2002, 62(17), 4916-4921.

    分子式
    C24H36N4O6S2    		 分子量
    540.7    		 CAS号
    128517-07-7    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    10 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 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
    NCT00426764 Peripheral T-cell Lymphoma Drug: Romidepsin Celgene Phase 2 2007-06-01 2017-01-19
    NCT01913119 Histologically Proven Extranodal NKTcell Lymphoma Drug: Romidepsin Samsung Medical Center|Celgene Corporation Early Phase 1 2013-07-01 2013-07-29
    NCT02296398 Cutaneous T-cell Lymphoma Drug: Romidepsin Northwestern University 2015-01-01 2016-03-10
    NCT01537744 Solid Tumors|Virally Mediated Cancers and Liposarcoma Drug: oral 5-azacitidine in combination with romidepsin Sidney Kimmel Comprehensive Cancer Center|Celgene Corporation Phase 1 2012-02-01 2017-03-21
    NCT01353664 Lymphoma|Cancer Drug: Romidepsin Celgene Corporation Phase 2 2011-05-01 2016-04-15
    NCT01324310 Hematologic Malignancy|Malignant Lymphoma Drug: Romidepsin|Drug: Ketoconazole Celgene Corporation Phase 1 2011-04-01 2016-03-30
    NCT00765102 Multiple Myeloma Drug: Bortezomib|Drug: Romidepsin Celgene Corporation Phase 2 2008-09-01 2016-03-30
    NCT01822886 Peripheral T-cell Lymphoma Drug: Romidepsin, Gemcitabine Fondazione Italiana Linfomi ONLUS Phase 2 2013-01-01 2017-02-14
    NCT01324323 Hematologic Malignancy|Malignant Lymphoma Drug: Romidepsin|Drug: Rifampin Celgene Corporation Phase 1 2011-04-01 2016-03-30
    NCT01979276 Multiple Myeloma Drug: Romidepsin|Drug: pomalidomide|Drug: Dexamethasone Weill Medical College of Cornell University|Celgene Corporation Phase 1|Phase 2 2013-11-01 2017-02-07
    NCT01638533 Glioma|Lymphoma|Metastatic Malignant Solid Neoplasm|Neuroendocrine Neoplasm|Recurrent Adult Soft Tissue Sarcoma|Recurrent Bladder Carcinoma|Recurrent Breast Carcinoma|Recurrent Chronic Lymphocytic Leukemia|Recurrent Colorectal Carcinoma|Recurrent Cutaneous T-Cell Non-Hodgkin Lymphoma|Recurrent Head and Neck Carcinoma|Recurrent Lung Carcinoma|Recurrent Malignant Solid Neoplasm|Recurrent Melanoma|Recurrent Pancreatic Carcinoma|Recurrent Prostate Carcinoma|Recurrent Renal Cell Carcinoma|Recurrent Thyroid Gland Carcinoma|Refractory Chronic Lymphocytic Leukemia|Refractory Cutaneous T-Cell Non-Hodgkin Lymphoma|Refractory Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma|Stage III Lung Cancer|Stage III Pancreatic Cancer|Stage III Prostate Cancer|Stage III Renal Cell Cancer|Stage III Soft Tissue Sarcoma|Stage IIIA Breast Cancer|Stage IIIA Colorectal Cancer|Stage IIIA Skin Melanoma|Stage IIIB Breast Cancer|Stage IIIB Colorectal Cancer|Stage IIIB Skin Melanoma|Stage IIIC Breast Cancer|Stage IIIC Colorectal Cancer|Stage IIIC Skin Melanoma|Stage IV Breast Cancer|Stage IV Lung Cancer|Stage IV Pancreatic Cancer|Stage IV Prostate Cancer|Stage IV Renal Cell Cancer|Stage IV Skin Melanoma|Stage IV Soft Tissue Sarcoma|Stage IVA Colorectal Cancer|Stage IVB Colorectal Cancer|Unresectable Solid Neoplasm Other: Pharmacological Study|Drug: Romidepsin National Cancer Institute (NCI)|Celgene Corporation Phase 1 2012-06-01 2017-03-23
    NCT01938833 HER2-negative Breast Cancer|Inflammatory Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer Drug: Romidepsin|Drug: Abraxane Sidney Kimmel Cancer Center at Thomas Jefferson University|Celgene Corporation|Thomas Jefferson University Phase 1|Phase 2 2014-04-01 2016-10-19
    NCT02203578 Graft Versus Host Disease Drug: romidepsin|Other: laboratory biomarker analysis Rutgers, The State University of New Jersey|National Cancer Institute (NCI)|Rutgers Cancer Institute of New Jersey 2014-11-01 2017-02-01
    NCT00085540 Adult Anaplastic Astrocytoma|Adult Anaplastic Oligodendroglioma|Adult Giant Cell Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Tumor Drug: depsipeptide National Cancer Institute (NCI) Phase 1|Phase 2 2005-01-01 2016-11-15
    NCT01590732 Lymphoma Drug: Romidepsin|Drug: Ifosfamide|Drug: Mesna|Drug: Carboplatin|Drug: Etoposide M.D. Anderson Cancer Center|Celgene Corporation Phase 1 2012-10-01 2016-09-28
    NCT02512497 Cutaneous T-cell Lymphoma|T-Prolymphocytic Leukemia|T-Large Granulocytic Leukemia|T-Lymphoblastic Leukemia/Lymphoma|Peripheral T-Cell Lymphoma Drug: Romidepsin|Drug: Busulfan|Drug: Fludarabine|Procedure: Stem Cell Transplant|Drug: Thymoglobulin M.D. Anderson Cancer Center|Celgene Corporation Phase 1|Phase 2 2015-10-01 2017-01-09
    NCT01456039 Lymphoma, T-cell, Peripheral Drug: Romidepsin Celgene Phase 1|Phase 2 2011-12-01 2017-02-01

    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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