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  • 维利帕尼

    Veliparib (ABT-888)

    维利帕尼
    产品编号 CFN60055
    CAS编号 912444-00-9
    分子式 = 分子量 C13H16N4O = 244.29
    产品纯度 >=98%
    物理属性 Powder
    化合物类型 Alkaloids
    植物来源
    ChemFaces的产品在影响因子大于5的优秀和顶级科学期刊中被引用
    提供自定义包装
    产品名称 产品编号 CAS编号 包装 QQ客服
    维利帕尼 CFN60055 912444-00-9 1mg QQ客服:215959384
    维利帕尼 CFN60055 912444-00-9 5mg QQ客服:215959384
    维利帕尼 CFN60055 912444-00-9 10mg QQ客服:215959384
    维利帕尼 CFN60055 912444-00-9 20mg QQ客服:215959384
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    ChemFaces的产品在许多优秀和顶级科学期刊中被引用

    Cell. 2018 Jan 11;172(1-2):249-261.e12.
    doi: 10.1016/j.cell.2017.12.019.
    IF=36.216(2019)

    PMID: 29328914

    Cell Metab. 2020 Mar 3;31(3):534-548.e5.
    doi: 10.1016/j.cmet.2020.01.002.
    IF=22.415(2019)

    PMID: 32004475

    Mol Cell. 2017 Nov 16;68(4):673-685.e6.
    doi: 10.1016/j.molcel.2017.10.022.
    IF=14.548(2019)

    PMID: 29149595

    ACS Nano. 2018 Apr 24;12(4): 3385-3396.
    doi: 10.1021/acsnano.7b08969.
    IF=13.903(2019)

    PMID: 29553709

    Nature Plants. 2016 Dec 22;3: 16206.
    doi: 10.1038/nplants.2016.205.
    IF=13.297(2019)

    PMID: 28005066

    Sci Adv. 2018 Oct 24;4(10): eaat6994.
    doi: 10.1126/sciadv.aat6994.
    IF=12.804(2019)

    PMID: 30417089
    我们的产品现已经出口到下面的研究机构与大学,并且还在增涨
  • Korea Intitute of Science and Technology (KIST) (Korea)
  • Pennsylvania State University (USA)
  • University of British Columbia (Canada)
  • Funda??o Universitária de Desenvolvimento (Brazil)
  • University of Pretoria (South Africa)
  • Institute of Pathophysiology Medical University of Vienna (Austria)
  • Universidad de La Salle (Mexico)
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  • 国外学术期刊发表的引用ChemFaces产品的部分文献
  • Org Biomol Chem.2017, 15(31):6483-6492
  • Enzyme Microb Technol.2022, 153:109941.
  • Korean J of Food Science&Technology 2017, 49(2):146-150
  • Inflammation.2015, 38(4):1502-16
  • Appl. Sci. 2021, 11(17),7829
  • Chinese Pharmacological Bulletin2019, 35(8):1120-1125
  • China Pharmacy2015, 26(27)
  • Nutrients.2019, 12(1):E40
  • Carbohydrate Polymer Technologies & App.2021, 2:100049.
  • Cells.2022, 11(8), 1311.
  • Front Pharmacol.2021, 12:762829.
  • Saudi Pharm J.2019, 27(1):145-153
  • J Adv Res.2019, 17:85-94
  • Plants (Basel).2021, 10(12):2795.
  • BMC Plant Biol.2022, 22(1):128.
  • J Herbmed Pharmacol.2018, 7(4):280-286
  • Separation Science Plus2022, sscp.202200048.
  • Chem Biol Interact.2018, 290:44-51
  • Antimicrob Agents Chemother.2020, AAC.01921-20.
  • Evid Based Complement Alternat Med.2020, 2020:1970349.
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  • Toxicol Res.2019, 35(4):371-387
  • ...
  • 生物活性
    Description: Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis.
    Targets: PARP1/ PARP2 | Autophagy
    In vitro:
    J Med Chem,2009 Jan 22;52(2):514-23.
    Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer.[Pubmed: 19143569]
    We have developed a series of cyclic amine-containing benzimidazole carboxamide PARP inhibitors with a methyl-substituted quaternary center at the point of attachment to the benzimidazole ring system.
    METHODS AND RESULTS:
    These compounds exhibit excellent PARP enzyme potency as well as single-digit nanomolar cellular potency. These efforts led to the identification of 3a (2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide, ABT-888), currently in human phase I clinical trials. Compound 3a displayed excellent potency against both the PARP-1 and PARP-2 enzymes with a K(i) of 5 nM and in a C41 whole cell assay with an EC(50) of 2 nM. In addition, 3a is aqueous soluble, orally bioavailable across multiple species, and demonstrated good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with temozolomide (TMZ) and in an MX-1 breast cancer xenograft model in combination with either carboplatin or cyclophosphamide.
    In vivo:
    Clin Cancer Res, 2007 May 15;13(10):3033-42.
    Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models.[Pubmed: 17505006]
    Poly(ADP-ribose) polymerase-1 (PARP-1) is the founding member of a family of enzymes that catalyze the addition of ADP-ribose units to proteins that mediate DNA repair pathways. Ionizing radiation induces DNA strand breaks, suggesting that PARP-1 inhibition may sensitize tumor cells to radiation.
    METHODS AND RESULTS:
    We investigated the combination of PARP-1 inhibition with radiation in lung cancer models. ABT-888, a novel potent PARP-1 inhibitor, was used to explore the effects of PARP-1 inhibition on irradiated tumors and tumor vasculature.ABT-888 reduced clonogenic survival in H460 lung cancer cells, and inhibited DNA repair as shown by enhanced expression of DNA strand break marker histone gamma-H2AX. Both apoptosis and autophagy contributed to the mechanism of increased cell death. Additionally, ABT-888 increased tumor growth delay at well-tolerated doses in murine models. For a 5-fold increase in tumor volume, tumor growth delay was 1 day for ABT-888 alone, 7 days for radiation alone, and 13.5 days for combination treatment. Immunohistochemical staining of tumor sections revealed an increase in terminal deoxyribonucleotide transferase-mediated nick-end labeling apoptotic staining, and a decrease in Ki-67 proliferative staining after combination treatment. Matrigel assay showed a decrease in in vitro endothelial tubule formation with ABT-888/radiation combination treatment, and von Willebrand factor staining of tumor sections revealed decreased vessel formation in vivo, suggesting that this strategy may also target tumor angiogenesis.
    CONCLUSIONS:
    We conclude that PARP-1 inhibition shows promise as an effective means of enhancing tumor sensitivity to radiation, and future clinical studies are needed to determine the potential of ABT-888 as a radiation enhancer.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 4.0935 mL 20.4675 mL 40.935 mL 81.8699 mL 102.3374 mL
    5 mM 0.8187 mL 4.0935 mL 8.187 mL 16.374 mL 20.4675 mL
    10 mM 0.4093 mL 2.0467 mL 4.0935 mL 8.187 mL 10.2337 mL
    50 mM 0.0819 mL 0.4093 mL 0.8187 mL 1.6374 mL 2.0467 mL
    100 mM 0.0409 mL 0.2047 mL 0.4093 mL 0.8187 mL 1.0234 mL
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    部分图片展示
    产品名称 产品编号 CAS编号 分子式 = 分子量 位单 联系QQ
    4,2'-Dihydroxy-4'-methoxychalcone ; 4,2'-Dihydroxy-4'-methoxychalcone CFN89427 63529-06-6 C16H14O4 = 270.28 5mg QQ客服:215959384
    异葫芦素 B; Isocucurbitacin B CFN91003 17278-28-3 C32H46O8 = 558.7 10mg QQ客服:215959384
    欧天芥菜碱; Heleurine CFN00239 488-00-6 C16H27NO4 = 297.39 5mg QQ客服:3257982914
    (+)-白花前胡甲素; (+)-Praeruptorin A CFN98141 73069-27-9 C22H22O8 = 414.41 5mg QQ客服:1457312923

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