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Palbociclib HCl

帕布昔利布,帕博西尼,帕泊昔布,PD-0332991 HCl

Palbociclib (PD-0332991) HCl是一种高度选择性的CDK4/6抑制剂，无细胞试验中IC50分别为11 nM/16 nM。它对CDK1/2/5，EGFR，FGFR，PDGFR，InsR等没有抑制活性。

目录号
EY1553
EY1553
EY1553
纯度
99.18%
99.18%
99.18%
规格
5 mg
10 mg
50 mg
原价
400
600
1800
售价
400
600
1800
库存
现货
现货
现货
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  • 生物活性

    PD-0332991 is a highly specific inhibitor of CDK4/6. It is a potent anti-proliferative agent against Rb-positive tumor cells in vitro, subsequently inducing an exclusive G1 arrest. It has been reported to prevent tumor growth in disseminated human myeloma xenografts and induce G1 arrest in primary bone marrow cells. PD-0332991 is also studied in breast cancer. It causes growth inhibition of ER-positive cell lines and 10/16 HER2-amplified cell lines. 100nM PD-0332991 can inhibit the phosphorylation of Rb in three more sensitive cell lines, resulting in prevention of cell cycle progression.

  • 体外研究

  • 体内研究

    Saline

  • 激酶实验

  • 细胞实验

    0.01-1 μM

  • 动物实验

    0-150 mg/kg 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 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] Fry DW, et al. Mol Cancer Ther, 2004, 3(11), 1427-1438.
    [2] Finn, R.S. et al. 2009. Breast Cancer Res. 11(5): R77.
    [3] Katsumi, Y. et al. 2011. Biochem. Biophys. Res. Commun. 413(1): 62-68.

    分子式
    C24H30ClN7O2    		 分子量
    483.99    		 CAS号
    827022-32-2    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    3 mg/mL    		 Water
    30 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
    NCT02806648 Pancreatic Neuroendocrine Cancer Drug: Palbociclib Grupo Espanol de Tumores Neuroendocrinos Phase 2 2015-05-01 2016-06-21
    NCT02600923 Advanced Breast Cancer (Female) Drug: Palbociclib|Drug: Letrozole Pfizer Phase 3 2016-04-15 2017-03-14
    NCT03065621 Breast Cancer Female Drug: Palbociclib Jules Bordet Institute Phase 2 2017-04-01 2017-02-22
    NCT02668666 Hormone Receptor Positive Malignant Neoplasm of Breast|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Estrogen Receptor Positive Breast Cancer|Progesterone Receptor Positive Tumor|Metastatic Breast Cancer Drug: Palbociclib|Drug: Tamoxifen Oana Danciu, MD|Pfizer|Hoosier Cancer Research Network|Big Ten Cancer Research Consortium Phase 2 2016-06-01 2017-02-06
    NCT02501902 Metastatic Pancreatic Ductal Adenocarcinoma Drug: Palbociclib|Drug: Nab-Paclitaxel Pfizer|Celgene Phase 1 2015-11-23 2017-03-15
    NCT01864746 Breast Cancer|Hormonreceptor Positive|Her2-normal|Postneoadjuvant Treatment With CDK 4/6 Inhibitor|CPS-EG Score Drug: Palbociclib PD-0332991|Drug: Placebo German Breast Group|Pfizer|AGO Study Group|NSABP Foundation Inc|Breast International Group Phase 3 2013-11-01 2016-08-17
    NCT01209598 Sarcoma|Liposarcoma Drug: Palbociclib Memorial Sloan Kettering Cancer Center|Pfizer Phase 2 2010-09-23 2017-02-08
    NCT03054363 Breast Cancer Drug: Tucatinib in Combination with Palbociclib and Letrozole University of Colorado, Denver Phase 1|Phase 2 2017-03-01 2017-02-24
    NCT02022982 KRAS Mutant Non-Small Cell Lung Cancer|Solid Tumors Drug: Palbociclib|Drug: PD-0325901 Dana-Farber Cancer Institute Phase 1|Phase 2 2014-01-01 2016-12-15
    NCT02334800 Healthy, Hepatic Insufficiency Drug: Palbociclib 75 mg Capsule Pfizer Phase 1 2015-03-01 2016-11-21
    NCT02896335 Metastatic Malignant Neoplasm to Brain Drug: Palbociclib Massachusetts General Hospital|Pfizer Phase 2 2016-11-01 2017-03-03
    NCT01953731 Healthy Drug: Palbociclib|Drug: Rifampin Pfizer Phase 1 2013-10-01 2014-01-16
    NCT02738866 Metastatic Breast Cancer Drug: Palbociclib|Drug: Fulvestrant Sidney Kimmel Comprehensive Cancer Center|Pfizer Phase 2 2016-08-01 2017-02-06
    NCT02131298 Healthy Drug: Palbociclib Alone|Drug: Palbociclib plus itraconazole Pfizer Phase 1 2014-05-01 2014-06-27
    NCT02311946 Healthy Drug: Palbociclib Alone|Drug: Palbociclib + Rabeprazole Pfizer Phase 1 2015-01-01 2015-05-27
    NCT02448771 Breast Cancer Stage IV|Unresectable Locally Advanced Invasive Breast Cancer|Metastatic Invasive Breast Cancer Drug: Palbociclib|Drug: Bazedoxifene Dana-Farber Cancer Institute|Pfizer Phase 1|Phase 2 2015-07-01 2017-01-22
    NCT02499120 Squamous Cell Carcinoma of the Head and Neck (SCCHN) Drug: palbociclib|Drug: Cetuximab|Drug: Placebo Pfizer Phase 2 2015-09-10 2017-03-14
    NCT02384239 Metastatic Breast Cancer|Hormone Receptor Positive Drug: Palbociclib University of California, San Francisco Phase 2 2015-10-01 2016-12-28
    NCT02334527 Metastatic Urothelial Carcinoma (UC) Drug: Palbociclib UNC Lineberger Comprehensive Cancer Center|Pfizer Phase 2 2015-03-01 2017-03-10
    NCT02806050 Breast Cancer Drug: Palbociclib|Device: FES PET|Drug: Letrozole University Medical Center Groningen Phase 2 2016-09-01 2017-02-14
    NCT01291017 Non-small Cell Lung Cancer Drug: PD0332991 University of Florida Phase 2 2011-02-01 2016-04-08

    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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