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BEZ235

NVP-BEZ-235,NVP-BEZ 235,Dactolisib

BEZ235 (NVP-BEZ235, Dactolisib)是一种 ATP竞争性的PI3K和mTOR抑制剂，对p110α/γ/δ/β和mTOR(p70S6K)均有抑制作用，IC50分别为4 nM/5 nM/7 nM/75 nM/6 nM，对ATR也有抑制作用，IC50为21 nM；但对Akt和PDK1抑制作用微弱。

目录号
EY1391
EY1391
EY1391
EY1391
纯度
99.11%
99.11%
99.11%
99.11%
规格
5 mg
10 mg
50 mg
100 mg
原价
220
370
780
1050
售价
220
370
780
1050
库存
现货
现货
现货
现货
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  • 生物活性

    BEZ235 is an imidazoquinoline derivative inhibiting both PI3K and mTOR kinases with low nanomolar IC50s. It was well tolerated in preclinical animal studies as well as in clinical trials with manageable gastrointestinal side-effects. It competes with ATP by binding to the ATP-binding site of kinases and reversibly reduces enzyme activity, resulting in growth arrest of tumor cells in G1 phase. Besides the inhibition of cell growth, BEZ235 blocks VEGF-induced angiogenesis. It may also inhibit DNA-PKcs。BEZ235 has shown potential anti-tumor activity both in vitro and in vivo. It inhibited growth of multiple cancer cell lines independently of mutation status in PI3K pathway. In xenograft mice models, it blocked PI3K signaling and showed antitumor activity. Combination study demonstrated that it enhances the efficacy of temozolomide.

  • 体外研究

  • 体内研究

    NMP+polyethylene glycol 300 (10+90, v+v)

  • 激酶实验

  • 细胞实验

    0-1 μM

  • 动物实验

    45 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 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] Maira SM, et al. Mol Cancer Ther, 2008, 7(7), 1851-1863.
    [2] Cho, D.C. et al. 2010. Clin. Cancer Res. 16(14): 3628-3638.
    [3] Roulin, D. et al. 2011. Mol. Cancer. 10 : 90.
    [4] Roper, J. et al. 2011. PLoS ONE. 6(9): e25132.
    [5] Zhang, Y. et al. 2012. J. Cell. Physiol. 227(1): 35-43.
    [6] Shoji, K. et al. 2012. PLoS ONE. 7(5): e37431.
    [7] Grasso, C.S. et al. 2015. Nat. Med. 21(6): 555-559.
    [8] Fallahi-Sichani, M. et al. 2013. Nat. Chem. Biol. 9(11): 708-714.

    分子式
    C30H23N5O    		 分子量
    469.55    		 CAS号
    915019-65-7    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    1.33 mg/mL    		 Water
    <1 mg/mL    		 Ethanol

    体内溶解度

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

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01856101 Carcinoma Transitional Cell Drug: BEZ235 Cliniques universitaires Saint-Luc- Universit茅 Catholique de Louvain|Novartis Phase 2 2013-02-01 2014-05-13
    NCT01343498 Malignant Solid Tumour Drug: BEZ235 SCRI Development Innovations, LLC|Novartis Phase 1 2011-04-01 2015-04-30
    NCT01453595 Renal Cancer Drug: BEZ235 Memorial Sloan Kettering Cancer Center|Novartis Phase 1|Phase 2 2011-10-01 2016-02-01
    NCT01290406 Endometrial Cancer Drug: BEZ235 Novartis Pharmaceuticals|Novartis Phase 2 2012-03-01 2012-06-20
    NCT01482156 Advanced Solid Tumors|Metastatic Breast Cancer|Metastatic Renal Cell Carcinoma Drug: RAD001 + BEZ235 Novartis Pharmaceuticals|Novartis Phase 1 2012-01-01 2015-11-18
    NCT01658436 Pancreatic Neuroendocrine Tumors (pNET) Drug: BEZ235 (Stage 1) Novartis Pharmaceuticals|Novartis Phase 2 2012-11-01 2016-04-19
    NCT01690871 Malignant PEComa (Perivascular Epithelioid Cell Tumors) Drug: BEZ235 Novartis Pharmaceuticals|Novartis Phase 2 2012-09-01 2013-08-01
    NCT00620594 Breast Cancer|Advanced Solid Tumors|Cowden Syndrome Drug: BEZ235 Novartis Pharmaceuticals|Novartis Phase 1 2006-12-21 2017-02-13
    NCT01495247 Inoperable Locally Advanced Breast Cancer|Metastatic Breast Cancer (MBC) Drug: BEZ235 + Paclitaxel Novartis Pharmaceuticals|Novartis Phase 1|Phase 2 2012-01-01 2014-07-22
    NCT01756118 Acute Lymphoblastic Leukemia|Leukemia, Myelocytic, Acute|Chronic Myelogenous Leukemia With Crisis of Blast Cells Drug: BEZ235 Johann Wolfgang Goethe University Hospital Phase 1 2012-06-01 2015-09-03
    NCT01717898 Castrate-resistant Prostate Cancer Patients. Drug: BEZ235|Drug: Prednisone|Drug: Abiraterone acetate Charles Ryan|Novartis Pharmaceuticals|University of California, San Francisco Phase 1|Phase 2 2013-01-01 2015-10-01
    NCT01628913 Pancreatic Neuroendocrine Tumors (pNET) Drug: BEZ235|Drug: Everolimus Novartis Pharmaceuticals|Novartis Phase 2 2012-10-01 2016-03-09
    NCT01195376 Advanced Solid Tumor Drug: BEZ235 Novartis Pharmaceuticals|Novartis Phase 1 2010-10-01 2016-04-20
    NCT01288092 Metastatic Breast Cancer Drug: BEZ235 Novartis Pharmaceuticals|Novartis Phase 2 2012-03-01 2012-06-05
    NCT01337765 Unspecified Adult Solid Tumor, Protocol Specific|Solid Tumor Drug: BEZ235 + MEK162 Array BioPharma Phase 1 2011-07-01 2016-02-11
    NCT01634061 Castration-resistant Prostate Cancer Drug: BEZ235|Drug: BKM120|Drug: BEZ235|Drug: BKM120 Novartis Pharmaceuticals|Novartis Phase 1 2012-09-01 2015-09-10
    NCT01471847 Locally Advance Breast Cancer (LABC)|Metastatic Breast Cancer (MBC) Drug: BEZ235 + Trastuzumab Phase l/Phase ll)|Drug: Lapatinib + Capecitabine (Phase II) Novartis Pharmaceuticals|Novartis Phase 1 2012-02-01 2012-11-30
    NCT01508104 Cancer Drug: BEZ235|Drug: Everolimus University of Cincinnati|Novartis Phase 1|Phase 2 2012-01-01 2012-01-06
    NCT01248494 Metastatic Breast Cancer Drug: BEZ235|Drug: BKM 120|Drug: Letrozole|Drug: BKM120 Vanderbilt-Ingram Cancer Center Phase 1 2010-11-01 2016-07-22
    NCT01285466 Metastatic or Locally Advanced Solid Tumors Drug: BEZ235 + paclitaxel|Drug: BKM120 + paclitaxel|Drug: BEZ235 + paclitaxel + trastuzumab|Drug: BKM120 + paclitaxel + trastuzumab Novartis Pharmaceuticals|Novartis Phase 1 2011-01-01 2017-02-13

    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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