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Luminespib

VER-52296,AUY-922,NVP-AUY922

AUY922 (NVP-AUY922)是高活性HSP90α和β抑制剂，IC50为13 nM和21 nM，对GRP94和 TRAP-1的活性较低。

目录号
EY1021
EY1021
EY1021
EY1021
EY1021
纯度
99.29%
99.29%
99.29%
99.29%
99.29%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
225
482
680
1700
3300
售价
225
482
680
1700
3300
库存
现货
现货
现货
现货
现货
订购
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  • 生物活性

    AUY922 (NVP-AUY922) is a small molecule Heat Shock Protein 90 (HSP90) inhibitor with IC50 values of 13 and 21 nM for HSP90α and HSP90β respectively. NVP-AUY922 inhibits proliferation of various human cancer cell lines in vitro, with an average GI50 of 9 nM. The IC50 values of NVP-AUY922 fall in the range of 2 to 40 nM in these gastric cancer cell lines. IC50 value for the BEAS-2B cells is 28.49 nM. Treatment with NVP-AUY922 does not influence the expression of Hsp90, but expression of HSP70 gets elevated by NVP-AUY922 treatment.

  • 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 μM

  • 动物实验

    50 mg/kg静脉注射或腹腔注射

  • 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] Lee KH, et al. Cancer Sci, 2011, 102(7), 1388-1395.
    [2] Moser C, Lang SA, Hackl C, Wagner C, Scheiffert E, Schlitt HJ, Geissler EK, Stoeltzing O.Targeting HSP90 by the novel inhibitor NVP-AUY922 reduces growth and angiogenesis of pancreatic cancer.Anticancer Res. 2012 Jul;32(7):2551-61.
    [3] Walsby E, Pearce L, Burnett AK, Fegan C, Pepper C.The Hsp90 inhibitor NVP-AUY922-AG inhibits NF-κB signaling, overcomes microenvironmental cytoprotection and is highly synergistic with fludarabine in primary CLL cells.Oncotarget. 2012 May;3(5):525-34.

    分子式
    C26H31N3O5    		 分子量
    465.54    		 CAS号
    747412-49-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    100 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
    NCT01854034 Non Small Cell Lung Cancer Drug: AUY922 Massachusetts General Hospital Phase 2 2013-07-01 2017-03-10
    NCT01668173 Myeloproliferative Neoplasms Drug: AUY922 Memorial Sloan Kettering Cancer Center|Novartis Phase 2 2012-08-01 2016-04-11
    NCT01485536 Lymphoma Drug: AUY922 M.D. Anderson Cancer Center|Novartis Phase 2 2012-08-01 2016-11-28
    NCT01484860 Adenocarcinoma of the Pancreas|Metastatic Disease Drug: AUY922 University Health Network, Toronto|Novartis Pharmaceuticals Phase 2 2012-01-01 2014-07-03
    NCT01602627 Unspecified Adult Solid Tumor, Protocol Specific Drug: Hsp90 inhibitor AUY922|Other: pharmacological study|Other: laboratory biomarker analysis Dale Shepard, MD, PhD|National Cancer Institute (NCI)|Case Comprehensive Cancer Center Phase 1 2011-09-01 2013-02-06
    NCT01389583 Gastrointestinal Stromal Tumor Drug: AUY922 National Health Research Institutes, Taiwan|National Taiwan University Hospital|Taipei Veterans General Hospital, Taiwan|Mackay Memorial Hospital|Taichung Veterans General Hospital|China Medical University Hospital|National Cheng-Kung University Hospital|Chang Gung Memorial Hospital Phase 2 2011-10-01 2015-02-23
    NCT00708292 Relapsed or Refractory Multiple Myeloma Drug: AUY922|Drug: Bortezomib|Drug: Dexamethasone Novartis Pharmaceuticals|Novartis Phase 1|Phase 2 2008-07-01 2015-06-30
    NCT01361945 Breast Cancer|Metastatic Breast Cancer|HER-2 Positive Breast Cancer|ER Positive Breast Cancer Drug: AUY922 Texas Tech University Health Sciences Center, El Paso Phase 1|Phase 2 2011-07-01 2015-12-08
    NCT01294826 Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IV Colon Cancer|Stage IV Rectal Cancer|Adenocarcinoma of the Colon|Adenocarcinoma of the Rectum Drug: AUY922|Drug: Cetuximab Swedish Medical Center|Novartis Pharmaceuticals Phase 1 2011-02-01 2015-06-04
    NCT00526045 Breast Cancer|Hematologic Neoplasms Drug: AUY922 Novartis Pharmaceuticals|Novartis Phase 1|Phase 2 2007-07-01 2013-05-10
    NCT01402401 Advanced Gastric Cancer Drug: AUY922 + Trastuzumab Novartis Pharmaceuticals|Novartis Phase 2 2011-11-01 2014-02-20
    NCT01404650 Gastrointestinal Stromal Tumor Drug: AUY922 SCRI Development Innovations, LLC|Novartis Phase 2 2011-12-01 2016-08-10
    NCT01613950 Stomach Neoplasms Esophageal Neoplasms Metastatic Gastric Cancer Mutated PI3KCA Protein Overexpressed HER2 Protein Drug: AUY922|Drug: BYL719 Novartis Pharmaceuticals|Novartis Phase 1 2012-12-01 2017-02-13
    NCT01271920 Advanced HER2-positive Breast Cancer Drug: AUY922|Drug: Trastuzumab Novartis Pharmaceuticals|Novartis Phase 2 2010-09-01 2017-02-21
    NCT01132625 Advanced Solid Tumors Drug: AUY922 Novartis Pharmaceuticals|Novartis Phase 1 2008-11-01 2013-02-21
    NCT01752400 Non Small Cell Lung Cancer Drug: AUY922 Massachusetts General Hospital Phase 2 2013-01-01 2016-09-12
    NCT01124864 Non-small-cell Lung Cancer Drug: AUY922 Novartis Pharmaceuticals|Novartis Phase 2 2010-10-01 2016-02-02
    NCT01772797 Anaplastic Lymphoma Kinase (ALK)|Non-small Cell Lung Cancer Drug: LDK378|Drug: AUY922 Novartis Pharmaceuticals|Novartis Phase 1 2013-06-01 2016-09-21
    NCT01081600 Breast Cancer Other: Imaging with 89Zr-trastuzumab PET University Medical Center Groningen 2010-02-01 2013-05-13
    NCT01784640 Recurrent Non-small Cell Lung Cancer|Squamous Cell Lung Cancer|Stage IV Non-small Cell Lung Cancer Drug: Hsp90 inhibitor AUY922|Drug: pemetrexed disodium|Other: pharmacological study|Other: laboratory biomarker analysis Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) Phase 1 2014-01-01 2016-11-08
    NCT01646125 Advanced Non Small Cell Lung Cancer (NSCLC) Drug: AUY922|Drug: Docetaxel|Drug: Pemetrexed Novartis Pharmaceuticals|Novartis Phase 2 2012-11-01 2017-01-23
    NCT01259089 Adenocarcinoma of the Lung|Non-small Cell Lung Cancer Drug: erlotinib hydrochloride|Drug: Hsp90 inhibitor AUY922|Other: laboratory biomarker analysis|Procedure: needle biopsy|Genetic: mutation analysis|Other: pharmacological study Northwestern University|Robert H. Lurie Cancer Center Phase 1|Phase 2 2011-03-01 2016-06-30

    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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