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Givinostat

ITF2357

Givinostat (ITF2357)是一种有效的HDAC抑制剂，作用于HDAC2， HDAC1B和HDAC1A时，IC50分别为10 nM， 7.5 nM和16 nM。

目录号
EY1840
EY1840
EY1840
EY1840
EY1840
纯度
99.52%
99.52%
99.52%
99.52%
99.52%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
350
890
1560
5520
8820
售价
350
890
1560
5520
8820
库存
现货
现货
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Givinostat (ITF2357) is a potent HDAC inhibitor for maize HD2, HD1B and HD1A with IC50 of 10 nM, 7.5 nM and 16 nM in cell-free assays.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    1 nM - 1 μM

  • 动物实验

    0.01-50 mg/kg溶于100 μL水，口服处理

  • 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] Leoni F, et al. Mol Med, 2005, 11(1-12), 1-15.

    分子式
    C24H27N3O4.HCl.H2O    		 分子量
    475.97    		 CAS号
    732302-99-7    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    98 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    5 mg/mL

    体内溶解度
    d

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

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01775553 Relapse Multiple Myeloma|Refractory Multiple Myeloma Drug: Carfilzomib Ajai Chari|Onyx Pharmaceuticals|Icahn School of Medicine at Mount Sinai Phase 2 2013-09-01 2016-09-16
    NCT02442648 Transplants and Implants Drug: Carfilzomib E. Steve Woodle|Onyx Pharmaceuticals|University of Cincinnati Phase 1 2014-12-01 2016-12-15
    NCT00721734 Multiple Myeloma|Renal Insufficiency Drug: Carfilzomib Onyx Therapeutics, Inc.|Onyx Pharmaceuticals Phase 2 2008-11-01 2016-01-08
    NCT02474927 Lung Transplant Rejection Drug: Carfilzomib John F. McDyer, MD|University of Pittsburgh Phase 2 2015-11-01 2017-03-03
    NCT02302495 Multiple Myeloma Drug: Carfilzomib University Hospital, Lille|Amgen Phase 2 2014-01-01 2017-02-23
    NCT02257476 Neoplasms|Malignancies Drug: Carfilzomib|Drug: Dexamethasone Emory University|Onyx Pharmaceuticals Phase 1 2014-08-01 2017-02-03
    NCT02572492 Multiple Myeloma Drug: Induction with CAR-CY-DEX and conditioning with carfilzomib and highdose melphalan|Drug: Carfilzomib/dexamethasone maintenance|Drug: Observation without carfilzomib/dexamethasone maintenance Henrik Gregersen|Nordic Myeloma Study Group|Aalborg Universitetshospital Phase 2 2015-01-01 2015-10-07
    NCT01926665 Lymphoma Drug: Carfilzomib|Drug: Dexamethasone M.D. Anderson Cancer Center|Onyx Pharmaceuticals Phase 1 2014-06-01 2016-06-29
    NCT01949532 Relapsed Multiple Myeloma|End-stage Renal Disease Drug: Carfilzomib Onyx Therapeutics, Inc.|Onyx Pharmaceuticals Phase 1 2014-01-01 2016-12-20
    NCT01949545 Solid Tumors|Hematologic Malignancies|Hepatic Impairment Drug: Carfilzomib Onyx Therapeutics, Inc.|Onyx Pharmaceuticals Phase 1 2013-10-01 2016-08-25
    NCT01336920 Adult Nasal Type Extranodal NK/T-cell Lymphoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Peripheral T-cell Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma Drug: carfilzomib University of Nebraska|National Cancer Institute (NCI)|Onyx Pharmaceuticals Phase 1 2011-06-01 2015-08-11
    NCT02042950 Lymphoma Drug: Carfilzomib M.D. Anderson Cancer Center|Onyx Therapeutics, Inc. Phase 2 2014-07-01 2016-04-06
    NCT02318784 Neuroendocrine Cancer Drug: Carfilzomib SCRI Development Innovations, LLC|Onyx Pharmaceuticals Phase 2 2015-07-01 2016-10-13
    NCT02142530 Non-Hodgkin Lymphoma|Diffuse Large B-cell Lymphoma|Mantle Cell Lymphoma|Follicular Lymphoma|Peripheral T-cell Lymphoma Drug: Carfilzomib|Drug: Belinostat Massachusetts General Hospital|National Comprehensive Cancer Network Phase 1 2014-10-01 2016-12-17
    NCT01813227 Waldenstrom|Prior Bortezomib Therapy Acceptable. Drug: Carfilzomib|Drug: Rituximab|Drug: Dexamethasone Hackensack University Medical Center|Onyx Therapeutics, Inc. Phase 2 2013-04-01 2015-08-21
    NCT02867618 Hodgkin Disease|Lymphoma, Non-hodgkin Drug: Carfilzomib|Drug: TGR-1202 Changchun Deng|Columbia University Phase 1|Phase 2 2016-10-16 2017-02-16
    NCT01775930 Kidney Cancer Drug: Carfilzomib M.D. Anderson Cancer Center|Onyx Therapeutics, Inc. Phase 2 2013-10-01 2016-12-05
    NCT01738594 Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Stage I Cutaneous T-cell Non-Hodgkin Lymphoma|Stage IA Mycosis Fungoides/Sezary Syndrome|Stage IB Mycosis Fungoides/Sezary Syndrome|Stage II Cutaneous T-cell Non-Hodgkin Lymphoma|Stage IIA Mycosis Fungoides/Sezary Syndrome|Stage IIB Mycosis Fungoides/Sezary Syndrome|Stage III Cutaneous T-cell Non-Hodgkin Lymphoma|Stage IIIA Mycosis Fungoides/Sezary Syndrome|Stage IIIB Mycosis Fungoides/Sezary Syndrome|Stage IV Cutaneous T-cell Non-Hodgkin Lymphoma|Stage IVA Mycosis Fungoides/Sezary Syndrome|Stage IVB Mycosis Fungoides/Sezary Syndrome Drug: carfilzomib|Drug: romidepsin|Other: laboratory biomarker analysis Northwestern University|Onyx Pharmaceuticals Phase 1 2013-01-01 2015-11-10
    NCT02145403 Hematologic Malignancies|Relapse|Graft-Versus-Host Disease Drug: Carfilzomib|Drug: Tacrolimus University of Michigan Cancer Center Phase 1|Phase 2 2014-09-01 2016-07-22
    NCT01496118 Multiple Myeloma Drug: carfilzomib and panobinostat SCRI Development Innovations, LLC|Onyx Therapeutics, Inc.|Novartis Phase 1|Phase 2 2011-12-01 2017-01-03
    NCT00884312 Multiple Myeloma Drug: Carfilzomib Onyx Therapeutics, Inc.|Onyx Pharmaceuticals Phase 2 2009-04-01 2017-03-14

    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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