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Veliparib

NSC 737664,ABT-888

Veliparib (ABT-888)是一种有效的PARP1和PARP2抑制剂,Ki分别为5.2 nM和2.9 nM,抑制SIRT2。

目录号
EY1819
EY1819
EY1819
EY1819
纯度
99.16%
99.16%
99.16%
99.16%
规格
5 mg
10 mg
50 mg
100 mg
原价
560
840
1980
3800
售价
560
840
1980
3800
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    ABT-888, also named as Veliparib, is poly (ADP-ribose) polymerase (PARP) inhibitor and has demonstrated excellent in vivo efficacy in a broad spectrum of preclinical tumor models in combination with a variety of cytotoxic agents. PARP is involved in DNA repair and elevated PARP levels can result in resistance to cytotoxic chemotherapy and radiation. So, PARP inhibitors hold promise as chemotherapy and radiation sensitizers. ABT-888 is also active on microsatellite instability (MSI) cell lines harboring mutations in both MRE11 and RAD50 genes compared to microsatellite stable (MSS) cell lines (wild-type for both genes).

  • 体外研究

  • 体内研究

    0.5% methylcellulose+0.2% Tween 80

  • 激酶实验

  • 细胞实验

    10 μM

  • 动物实验

    25或3.125 mg/kg 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 AKm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] Donawho CK, et al, Clin Cancer Res, 2007, 13 (9), 2728-2737.

    分子式
    C13H16N4O
    分子量
    244.29
    CAS号
    912444-00-9
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    20 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
    NCT02210663 Advanced Solid Tumors Drug: veliparib (ABT-888) AbbVie Phase 1 2014-07-01 2016-07-19
    NCT02158507 Metastatic Triple Negative Breast Cancer Drug: Combination of Veliparib + Lapatinib University of Alabama at Birmingham|Scariot Foundation|GlaxoSmithKline|AbbVie 2014-07-01 2016-12-28
    NCT02289690 Small Cell Lung Cancer Drug: Veliparib|Drug: Carboplatin|Drug: Etoposide AbbVie Phase 2 2014-10-01 2017-02-22
    NCT01853306 Oncology|BRCA Mutated|High Grade Serous Ovarian Cancer|BRCA Mutated Breast Cancer Drug: Veliparib AbbVie Phase 1 2013-03-01 2017-02-06
    NCT01123876 Gastric Cancer Drug: Veliparib AbbVie (prior sponsor, Abbott)|AbbVie Phase 1 2010-03-01 2015-01-20
    NCT01690598 Ovarian Cancer Drug: Veliparib|Drug: Topotecan Vejle Hospital|Abbott Phase 1|Phase 2 2012-11-01 2015-06-09
    NCT01199224 Solid Tumors Drug: veliparib|Drug: veliparib|Drug: veliparib|Drug: veliparib Abbott Phase 1 2010-06-01 2011-02-03
    NCT02723864 Neoplasms Drug: Veliparib + VX-970 + Cisplatin National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 1 2016-03-22 2017-03-21
    NCT00892736 Basal-Like Breast Carcinoma|BRCA1 Mutation Carrier|BRCA2 Mutation Carrier|Breast Carcinoma|Estrogen Receptor Negative|HER2/Neu Negative|Hereditary Breast and Ovarian Cancer Syndrome|Ovarian Carcinoma|Pancreatic Carcinoma|Progesterone Receptor Negative|Prostate Carcinoma|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Solid Neoplasm|Triple-Negative Breast Carcinoma Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Veliparib National Cancer Institute (NCI) Phase 1 2009-04-01 2016-06-30
    NCT01351909 HER2/Neu Negative|Recurrent Breast Carcinoma|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Drug: Cyclophosphamide|Other: Laboratory Biomarker Analysis|Drug: Veliparib National Cancer Institute (NCI) Phase 1 2011-05-01 2017-02-16
    NCT01540565 BRCA1 Mutation Carrier|BRCA2 Mutation Carrier|Ovarian Epithelial Tumor|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma Other: Laboratory Biomarker Analysis|Drug: Veliparib National Cancer Institute (NCI) Phase 2 2012-04-01 2017-02-02
    NCT01193140 Solid Tumor Cancers Drug: veliparib|Drug: Temozolomide Abbott Phase 2 2010-07-01 2012-11-16
    NCT01434316 BRCA1 Mutation Carrier|BRCA2 Mutation Carrier|Solid Neoplasm Drug: Dinaciclib|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Veliparib National Cancer Institute (NCI) Phase 1 2011-11-01 2017-01-31
    NCT01908478 Pancreatic Cancer Drug: Veliparib|Drug: Gemcitabine|Radiation: Intensity modulated radiation therapy Cedars-Sinai Medical Center|AbbVie Phase 1 2013-07-01 2017-02-17
    NCT01589419 Locally Advanced Rectal Cancer Drug: veliparib|Drug: capecitabine|Radiation: radiation AbbVie (prior sponsor, Abbott)|AbbVie Phase 1 2012-06-01 2015-01-20
    NCT02860819 Testicular Cancer Drug: Veliparib|Drug: Gemcitabine|Drug: Carboplatin National Cancer Institute, Slovakia Phase 2 2016-07-01 2016-08-04
    NCT01472783 Recurrent, Epithelial Ovarian Cancer Drug: Veliparib Vejle Hospital|Abbott Phase 1|Phase 2 2011-11-01 2016-11-15

    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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