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BKM120

NVP-BKM 120,NVP-BKM-120,Buparlisib

NVP-BKM120(BKM120)是PI3K抑制剂，对于p110α、β、δ、γ的IC50分别为52 nM、166 nM、116 nM、262 nM。而对于VPS34、mTOR、DNAPK则抑制性较小，对于PI4Kβ则几乎无抑制性。

目录号
EY0935
EY0935
EY0935
EY0935
纯度
98.74%
98.74%
98.74%
98.74%
规格
5 mg
10 mg
50 mg
100 mg
原价
620
930
1800
2750
售价
620
930
1800
2750
库存
现货
现货
现货
现货
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订购
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  • 生物活性

    BKM120 is an oral bioactive, selective and reversible inhibitor of PI3K p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. BKM120 reduces potency against VPS34, mTOR, DNAPK and is little activity to PI4Kβ.

  • 体外研究

  • 体内研究

    0.5% CMC Na

  • 激酶实验

  • 细胞实验

    0-6.6 μM

  • 动物实验

    ~60 mg/kg每天口服处理

  • 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] Burger MT, et al. ACS Med Chem Lett, 2011, 2 (10), 774–779.
    [2] Zheng Y, et al. Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity with dexamethasone. J Mol Med (Berl), 2011 Dec 30.

    分子式
    C18H21F3N6O2    		 分子量
    410.39    		 CAS号
    944396-07-0    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    82 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    2 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
    NCT02128724 Carcinoma, Non-Small-Cell Lung Drug: BKM120 University of Oxford|Cancer Research UK|Novartis Phase 1 2013-04-01 2017-03-03
    NCT01570296 Non-Small Cell Lung Cancer|Solid Tumors Drug: Gefitinib and BKM120 National Cancer Centre, Singapore|Novartis Phase 1 2011-10-01 2016-03-21
    NCT01550380 Endometrial Cancer Drug: BKM120 University of Utah|Novartis Phase 2 2014-05-01 2014-07-28
    NCT01513356 Breast Cancer Drug: BKM120 Sofia Perea, Director Clinical Trials Unit.|Novartis|Grupo Hospital de Madrid Early Phase 1 2012-10-01 2014-04-01
    NCT01385293 Prostate Cancer|Metastatic (Spread to Other Areas of the Body) Drug: BKM120 Andrew J. Armstrong, MD|Novartis Pharmaceuticals|Duke University Phase 2 2011-08-01 2016-09-14
    NCT01487265 Non Small Cell Lung Cancer Drug: BKM120 and Erlotinib SCRI Development Innovations, LLC|Novartis Phase 2 2014-03-01 2017-02-13
    NCT01527877 Head Neck Cancer Squamous Cell Metastatic|Head Neck Cancer Squamous Cell Recurrent Drug: BKM120 Yonsei University Phase 2 2012-09-01 2012-10-04
    NCT01589861 Breast Cancer Drug: BKM120 + lapatinib Institut Paoli-Calmettes Phase 1|Phase 2 2011-12-01 2015-11-30
    NCT01695473 High Risk Prostate Cancer Drug: BKM120 Charles Ryan|Novartis|University of California, San Francisco Phase 2 2012-10-01 2015-10-01
    NCT02487823 Non Castrate Metastatic Prostate Cancer Drug: BKM120 in combination with LH-RH agonists (suprefact) and bicalutamide Institut Paoli-Calmettes|Novartis Phase 1 2014-10-01 2017-03-01
    NCT01830504 Thyroid Cancers Drug: BKM120 Hospices Civils de Lyon Phase 2 2013-04-01 2016-10-04
    NCT02439489 Solid Tumors Drug: BKM120-CIS|Drug: BKM120-CARBO Fondazione Michelangelo Phase 1 2012-12-01 2016-04-07
    NCT01833169 PI3K Pathway Activated Tumors Drug: BKM120 Novartis Pharmaceuticals|Novartis Phase 2 2013-03-01 2016-12-30
    NCT01396499 Leukemia Drug: BKM120 M.D. Anderson Cancer Center|Novartis Phase 1 2012-07-01 2016-10-31
    NCT02113878 Carcinoma, Squamous Cell of Head and Neck|HPV Positive Oropharyngeal Squamous Cell Carcinoma|Hypopharyngeal Cancer|Early Invasive Cervical Squamous Cell Carcinoma|Carcinoma of Larynx|Cancer of Nasopharynx Drug: BKM120|Drug: Cisplatin|Radiation: Intensity-modulated radiotherapy (IMRT) Dana-Farber Cancer Institute|Novartis Pharmaceuticals Phase 1 2014-10-01 2016-12-29
    NCT01806649 Esophageal Cancer Drug: BKM120 Prince of Songkla University Phase 2 2013-01-01 2015-10-19
    NCT01304602 Colorectal Cancer Drug: Irinotecan|Drug: BKM120 University of Kansas Medical Center Phase 1 2011-02-01 2017-01-04
    NCT01623349 Ovarian Cancer|Breast Cancer Drug: BKM120 and Olaparib|Drug: BYL719 and Olaparib Dana-Farber Cancer Institute|Novartis|AstraZeneca Phase 1 2012-09-01 2017-03-22
    NCT02301364 Lymphoma|Primary Central Nervous System Lymphoma|Recurrent/Refractory Secondary Central Nervous System Lymphoma Drug: Buparlisib (BKM120) Memorial Sloan Kettering Cancer Center|Novartis Phase 2 2014-11-20 2017-02-09
    NCT01068483 Breast Cancer|Colon Cancer|Ovarian Cancer|Endometrium Cancer Drug: BKM120 Novartis Pharmaceuticals|Novartis Phase 1 2008-11-01 2013-04-09
    NCT01349660 Glioblastoma Multiforme Drug: Bevacizumab|Drug: BKM120 SCRI Development Innovations, LLC|Novartis Phase 1|Phase 2 2011-12-01 2017-01-16
    NCT01953445 Breast Neoplasms Drug: paclitaxel|Drug: BKM120 Washington University School of Medicine Phase 2 2014-08-01 2014-12-05
    NCT01468688 3rd Line GIST Drug: STI571|Drug: BKM120 Novartis Pharmaceuticals|Novartis Phase 1 2012-04-19 2017-02-03

    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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