Neratinib

来那替尼,HKI-272

Neratinib (HKI-272)是一种高度选择性的HER2和EGFR抑制剂,IC50分别为59 nM和92 nM;微弱抑制KDR和Src,对Akt,CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf和c-Met没有显著的抑制作用。

目录号
EY1582
EY1582
EY1582
纯度
99.13%
99.13%
99.13%
规格
5 mg
10 mg
25 mg
原价
280
500
800
售价
280
500
800
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Neratinib (synonym: HKI-272; HKI 272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met.

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% propylene glycol

  • 激酶实验

  • 细胞实验

    0.5 ng/mL-5 μg/mL

  • 动物实验

    ~80 mg/kg/day口服饲喂

  • 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] Rabindran SK, et al. Cancer Res, 2004, 64(11), 3958-3965.

    分子式
    C30H29ClN6O3
    分子量
    557.04
    CAS号
    698387-09-6
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    5 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
    NCT01128842 Advanced Malignant Solid Tumors Drug: Neratinib + Capecitabine Puma Biotechnology, Inc. Phase 1 2010-04-01 2012-05-10
    NCT00838539 Neoplasms|Malignant Carcinoma Drug: Neratinib|Drug: Temsirolimus Puma Biotechnology, Inc. Phase 1 2009-04-01 2016-11-22
    NCT02932280 Solid Tumor|Central Nervous System Tumor|Lymphoma|Leukemia Drug: Neratinib Memorial Sloan Kettering Cancer Center|Milton S. Hershey Medical Center|M.D. Anderson Cancer Center|Stanford University|Arkansas Children's Hospital Research Institute|Alberta Children's Hospital|Phoenix Children's Hospital|University of Texas Phase 1|Phase 2 2016-10-01 2017-02-15
    NCT01142063 Healthy Drug: Neratinib|Drug: Neratinib|Drug: Neratinib|Drug: Neratinib Puma Biotechnology, Inc. Phase 1 2010-06-01 2012-05-10
    NCT00958724 Advanced Malignant Solid Tumors Drug: treatment with neratinib (HKI-272) + vinorelbine Puma Biotechnology, Inc. Phase 1 2009-07-01 2012-05-10
    NCT01111825 Breast Cancer Drug: Temsirolimus|Drug: Neratinib Puma Biotechnology, Inc. Phase 1|Phase 2 2010-04-01 2016-10-05
    NCT03065387 Malignant Neoplasm of Breast|Malignant Neoplasms of Digestive Organs|Malignant Neoplasms of Female Genital Organs|Malignant Neoplasms of Ill-defined Secondary and Unspecified Sites|Malignant Neoplasms of Independent (Primary) Multiple Sites|Malignant Neoplasms of Lip Oral Cavity and Pharynx|Malignant Neoplasms of Mesothelial and Soft Tissue|Malignant Neoplasms of Respiratory and Intrathoracic Organs|Malignant Neoplasms of Thyroid and Other Endocrine Glands|Malignant Neoplasms of Urinary Tract|Neoplasms of Uncertain or Unknown Behavior Drug: Neratinib|Drug: Everolimus|Drug: Palbociclib|Drug: Trametinib M.D. Anderson Cancer Center|Pfizer|Puma Biotechnology, Inc. Phase 1 2017-04-01 2017-02-28
    NCT01960023 Colorectal Cancer Drug: Cetuximab|Drug: Neratinib NSABP Foundation Inc Phase 1|Phase 2 2013-10-01 2016-05-05
    NCT01827267 HER2-mutant Non-Small Cell Lung Cancer Drug: neratinib|Drug: temsirolimus Puma Biotechnology, Inc. Phase 2 2013-05-01 2017-03-02
    NCT02236000 Breast Cancer Drug: Neratinib|Drug: T-DM1 NSABP Foundation Inc|Puma Biotechnology, Inc. Phase 1|Phase 2 2014-08-01 2017-02-20
    NCT00781430 Hepatic Insufficiency Drug: Neratinib (HKI-272) Puma Biotechnology, Inc. Phase 1 2009-04-01 2012-05-10
    NCT01956253 Bladder Cancer Drug: Neratinib UNC Lineberger Comprehensive Cancer Center 2013-07-01 2017-03-10
    NCT01423123 Breast Cancer Drug: Paclitaxel|Biological: trastuzumab|Drug: Neratinib NSABP Foundation Inc|Pfizer Phase 1 2011-05-01 2014-07-07
    NCT00741260 Breast Cancer Drug: Neratinib|Drug: capecitabine Puma Biotechnology, Inc. Phase 1|Phase 2 2008-12-01 2016-06-22
    NCT02334501 Healthy Drug: Lansoprazole|Drug: Neratinib Puma Biotechnology, Inc. Phase 1 2014-08-01 2016-05-09
    NCT01953926 Solid Tumors Drug: Neratinib|Drug: Paclitaxel|Drug: Fulvestrant Puma Biotechnology, Inc. Phase 2 2013-09-30 2017-02-17
    NCT00864487 Healthy Subjects Drug: Neratinib Puma Biotechnology, Inc. Phase 1 2009-04-01 2012-05-10
    NCT00932464 Healthy Drug: Neratinib|Drug: Neratinib Puma Biotechnology, Inc. Phase 1 2012-08-01 2012-05-10
    NCT02673398 HER2 Positive Breast Carcinoma|Recurrent Breast Carcinoma|Stage IV Breast Cancer Other: Comprehensive Geriatric Assessment|Other: Laboratory Biomarker Analysis|Drug: Neratinib|Other: Pharmacological Study City of Hope Medical Center|National Cancer Institute (NCI)|Puma Biotechnology, Inc. Phase 2 2016-10-01 2016-11-30
    NCT01670877 Breast Neoplasms Drug: Neratinib|Drug: Fulvestrant|Drug: Trastuzumab Washington University School of Medicine Phase 2 2012-12-11 2017-02-08

    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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