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Palbociclib Isethionate

羟乙基磺酸帕博西丽,PD0332991 isethionate

Palbociclib (PD0332991) Isethionate是一种高度选择性的CDK4/6抑制剂，IC50为11 nM/16 nM，对CDK1/2/5， EGFR， FGFR， PDGFR， InsR等没有抑制活性。Phase 2/3。

目录号
EY1374
EY1374
EY1374
EY1374
纯度
99.33%
99.33%
99.33%
99.33%
规格
1 mg
5 mg
10 mg
50 mg
原价
235
520
780
1530
售价
235
520
780
1530
库存
现货
现货
现货
现货
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  • 生物活性

    Cyclin-dependent kinases (CDKs) are a family of protein kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. A cyclin-dependent kinase inhibitor (CKI) is a protein that interacts with a cyclin-CDK complex to block kinase activity, usually during G1 or in response to signals from the environment or from damaged DNA. Palbociclib is an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6.

  • 体外研究

  • 体内研究

    Saline

  • 激酶实验

  • 细胞实验

    2 μM

  • 动物实验

    150 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] Fry DW, et al. Mol Cancer Ther, 2004, 3(11), 1427-1438.
    [2] Michaud et al (2010) Pharmacologic inhibition of cyclin-dependent kinases 4 and 6 arrests the growth of glioblastoma multiforme intracranial xenografts. Cancer Res. 70 3228.
    [3] Toogood et al (2005) Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. J.Med.Chem. 48 2388.

    分子式
    C26H35N7O6S    		 分子量
    573.66    		 CAS号
    827022-33-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    10 mM    		 Water
    100 mM    		 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
    NCT02255461 Childhood Choroid Plexus Tumor|Childhood Ependymoblastoma|Childhood Grade III Meningioma|Childhood High-grade Cerebellar Astrocytoma|Childhood High-grade Cerebral Astrocytoma|Childhood Medulloepithelioma|Recurrent Childhood Anaplastic Astrocytoma|Recurrent Childhood Anaplastic Oligoastrocytoma|Recurrent Childhood Anaplastic Oligodendroglioma|Recurrent Childhood Brain Stem Glioma|Recurrent Childhood Cerebellar Astrocytoma|Recurrent Childhood Cerebral Astrocytoma|Recurrent Childhood Giant Cell Glioblastoma|Recurrent Childhood Glioblastoma|Recurrent Childhood Gliomatosis Cerebri|Recurrent Childhood Gliosarcoma|Recurrent Childhood Medulloblastoma|Recurrent Childhood Pineoblastoma|Recurrent Childhood Supratentorial Primitive Neuroectodermal Tumor Drug: palbociclib isethionate|Other: pharmacological study|Other: laboratory biomarker analysis Pediatric Brain Tumor Consortium|National Cancer Institute (NCI) Phase 1 2014-10-01 2016-10-19
    NCT02041273 Healthy Drug: palbociclib isethionate (phase 1 and 2 studies)|Drug: palbociclib isethionate (phase 1 and 2 studies)|Drug: palbociclib commercial free base capsule Pfizer Phase 1 2014-01-01 2014-03-14
    NCT01602887 Healthy Drug: PD-0332991|Drug: PD-0332991|Drug: PD-0332991|Drug: PD-0332991 Pfizer Phase 1 2012-05-01 2012-11-08

    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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