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Ribociclib

LEE011

Ribociclib是一种可口服的,高度特异性CDK4/6抑制剂。

目录号
EY1032
EY1032
EY1032
EY1032
纯度
99.23%
99.23%
99.23%
99.23%
规格
2 mg
5 mg
10 mg
25 mg
原价
300
600
1000
1600
售价
300
600
1000
1600
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    LEE011 is a novel, orally available, potent and selective CDK4/6 inhibitor.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    10 μM

  • 动物实验

    ~200mg/kg 每天口服

  • 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] Rader J, et al. Clin Cancer Res. 2013, 19(22), 6173-6182.

    分子式
    C23H30N8O
    分子量
    434.54
    CAS号
    1211441-98-3
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    10 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
    NCT02754011 Breast Cancer Drug: Combination of ribociclib + capecitabine UNICANCER|Novartis Phase 1 2017-01-01 2017-02-09
    NCT02933736 Glioblastoma Multiforme|Meningioma Drug: Ribociclib St. Joseph's Hospital and Medical Center, Phoenix|Novartis Early Phase 1 2016-10-01 2017-01-04
    NCT02345824 Glioblastoma|Glioma Drug: Ribociclib University of Virginia|Novartis Pharmaceuticals Phase 1 2016-03-01 2016-10-27
    NCT02571829 Liposarcoma|Soft Tissue Sarcoma Drug: ribociclib Hadassah Medical Organization Phase 2 2016-05-01 2016-11-22
    NCT02712723 Breast Cancer Drug: Letrozole|Drug: Ribociclib|Drug: Placebo University of Kansas Medical Center|Novartis Pharmaceuticals Phase 2 2016-02-01 2017-02-17
    NCT03008408 Malignant Neoplasms of Female Genital Organs|Endometrial Carcinoma Drug: Ribociclib|Drug: Everolimus|Drug: Letrozole M.D. Anderson Cancer Center|Novartis Phase 2 2017-04-01 2017-02-14
    NCT02934568 Continued Access to Study Treatment(s)|Cancers With a Mass, Bulky Tumor, Nodule, Lump, Advanced Cancer, Advanced Solid Tumors, Advanced Solid Malignancies Drug: LEE011 Novartis Pharmaceuticals|Novartis Phase 2 2016-12-15 2017-02-27
    NCT03056833 Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Carcinoma Drug: ribociclib|Drug: Paclitaxel|Drug: Carboplatin University of Michigan Cancer Center Phase 1 2017-05-01 2017-03-16
    NCT02555189 Hormone-Resistant Prostate Cancer|Metastatic Prostate Carcinoma|Prostate Carcinoma Metastatic in the Bone|Stage IV Prostate Cancer Drug: Enzalutamide|Drug: Ribociclib Sidney Kimmel Cancer Center at Thomas Jefferson University|Novartis|Prostate Cancer Clinical Trials Consortium|Thomas Jefferson University Phase 1|Phase 2 2015-12-01 2016-12-20
    NCT03050398 Breast Cancer Drug: Ribociclib|Drug: letrozole Novartis Pharmaceuticals|Novartis Phase 3 2017-05-15 2017-03-21
    NCT03078751 Breast Cancer Drug: Ribociclib|Drug: Placebo|Drug: Adjuvant endocrine therapy Novartis Pharmaceuticals|Novartis Phase 3 2017-05-11 2017-03-08
    NCT03081234 Breast Cancer Drug: Ribociclib|Drug: Placebo|Drug: Adjuvant endocrine therapy Novartis Pharmaceuticals|Novartis Phase 3 2017-05-25 2017-03-10
    NCT03009201 Metastatic Angiosarcoma|Metastatic Epithelioid Sarcoma|Metastatic Fibrosarcoma|Metastatic Leiomyosarcoma|Metastatic Liposarcoma|Metastatic Malignant Peripheral Nerve Sheath Tumor|Metastatic Synovial Sarcoma|Metastatic Undifferentiated Pleomorphic Sarcoma|Myxofibrosarcoma|Pleomorphic Rhabdomyosarcoma|Stage III Soft Tissue Sarcoma|Stage IV Soft Tissue Sarcoma|Undifferentiated (Embryonal) Sarcoma Drug: Doxorubicin Hydrochloride|Drug: Ribociclib OHSU Knight Cancer Institute|National Cancer Institute (NCI) Phase 1 2017-01-01 2016-12-30
    NCT02414724 Lymphoma|Solid Neoplasm Drug: Gemcitabine Hydrochloride|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Ribociclib Roswell Park Cancer Institute|National Cancer Institute (NCI)|Novartis Phase 1 2015-05-01 2016-09-09
    NCT03090165 Triple Negative Breast Cancer Drug: ribociclib|Drug: ribociclib|Drug: Bicalutamide Ruth O'Regan, M.D.|Novartis|Big Ten Cancer Research Consortium Phase 1|Phase 2 2017-03-01 2017-03-23
    NCT02607124 High Grade Glioma|Diffuse Intrinsic Pontine Glioma|Bithalamic High Grade Glioma Drug: Ribociclib Children's Hospital Medical Center, Cincinnati|Novartis Phase 1|Phase 2 2016-04-01 2017-02-28
    NCT02586675 Breast Cancer|Breast Cancer - Female|Breast Cancer - Male Drug: Tamoxifen|Drug: Ribociclib|Drug: Goserelin H. Lee Moffitt Cancer Center and Research Institute|Novartis Phase 1 2016-02-01 2016-12-27
    NCT02657928 Estrogen Receptor Positive|Postmenopausal|RB1 Positive|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Recurrent Uterine Corpus Carcinoma Other: Laboratory Biomarker Analysis|Drug: Letrozole|Drug: Ribociclib Mayo Clinic|National Cancer Institute (NCI) Phase 2 2016-07-01 2017-01-26
    NCT02732119 Breast Cancer Drug: Ribociclib|Drug: Everolimus|Drug: Exemestane Novartis Pharmaceuticals|Novartis Phase 1|Phase 2 2016-06-14 2017-02-23
    NCT02632045 Metastatic Breast Cancer|Breast Carcinoma Drug: LEE-011|Drug: Fulvestrant|Drug: Placebo Kevin Kalinsky|Novartis Pharmaceuticals|Columbia University Phase 2 2016-03-01 2017-03-03
    NCT02420691 Gastrointestinal Cancer Drug: LEE011 M.D. Anderson Cancer Center|Novartis Phase 2 2015-08-01 2016-09-19

    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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