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Pazopanib HCl

盐酸帕唑帕尼,GW786034 HCl,Votrient,Armala

Pazopanib Hydrochloride是多靶点抑制剂,对VEGFR1,VEGFR2,VEGFR3,PDGFR,FGFR,c-Kit和c-Fms的IC50分别为10 nM,30 nM,47 nM,84 nM,74 nM,140 nM和146 nM。

目录号
EY1628
EY1628
EY1628
纯度
99.12%
99.12%
99.12%
规格
1 mg
5 mg
50 mg
原价
120
300
880
售价
120
300
880
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Pazopanib Hydrochloride (GW786034, Votrient, Armala) is a novel, multitargeted inhibitor of flt-1(VEGFR-1), Flk-1(VEGFR-2), flt-4 (VEGFR-3), PDGFR, FGFR, c-Kit and c-Fms-CSF-1R (c-fms) with IC50 values of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0 μM -10 μM

  • 动物实验

    0 mg/kg, 10 mg/kg, 30 mg/kg或100 mg/kg 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] Harris PA, et al. J Med Chem. 2008, 51(15), 4632-4640.

    分子式
    C21H24ClN7O2S
    分子量
    473.98
    CAS号
    635702-64-6
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    20 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
    NCT00929903 Childhood Central Nervous System Choriocarcinoma|Childhood Central Nervous System Embryonal Tumor|Childhood Central Nervous System Germ Cell Tumor|Childhood Central Nervous System Germinoma|Childhood Central Nervous System Mixed Germ Cell Tumor|Childhood Central Nervous System Teratoma|Childhood Central Nervous System Yolk Sac Tumor|Metastatic Childhood Soft Tissue Sarcoma|Recurrent Childhood Brain Stem Glioma|Recurrent Childhood Central Nervous System Embryonal Tumor|Recurrent Childhood Soft Tissue Sarcoma|Recurrent Childhood Visual Pathway Glioma|Unspecified Childhood Solid Tumor, Protocol Specific Drug: pazopanib hydrochloride|Other: pharmacological study National Cancer Institute (NCI) Phase 1 2009-06-01 2013-09-27
    NCT01767636 Carcinoma of the Collecting Ducts of Bellini|Chromophobe Renal Cell Carcinoma|Kidney Medullary Carcinoma|Kidney Oncocytoma|Metastatic Renal Cell Cancer|Papillary Renal Cell Carcinoma|Recurrent Renal Cell Carcinoma|Sarcomatoid Renal Cell Carcinoma|Stage IV Renal Cell Cancer Drug: Pazopanib Hydrochloride Mayo Clinic|National Cancer Institute (NCI) Phase 2 2013-05-01 2017-03-06
    NCT01247571 Recurrent Uterine Corpus Sarcoma|Uterine Carcinosarcoma Drug: Pazopanib Hydrochloride National Cancer Institute (NCI) Phase 2 2011-01-01 2016-05-06
    NCT01552356 Solid Neoplasm Other: Laboratory Biomarker Analysis|Drug: Pazopanib Hydrochloride|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1 2012-03-01 2017-01-31
    NCT00625846 Recurrent Thyroid Gland Carcinoma|Stage III Differentiated Thyroid Gland Carcinoma|Stage III Thyroid Gland Medullary Carcinoma|Stage IVA Differentiated Thyroid Gland Carcinoma|Stage IVA Thyroid Gland Medullary Carcinoma|Stage IVA Thyroid Gland Undifferentiated (Anaplastic) Carcinoma|Stage IVB Differentiated Thyroid Gland Carcinoma|Stage IVB Thyroid Gland Medullary Carcinoma|Stage IVB Thyroid Gland Undifferentiated (Anaplastic) Carcinoma|Stage IVC Differentiated Thyroid Gland Carcinoma|Stage IVC Thyroid Gland Medullary Carcinoma|Stage IVC Thyroid Gland Undifferentiated (Anaplastic) Carcinoma|Thyroid Gland Undifferentiated (Anaplastic) Carcinoma Other: Laboratory Biomarker Analysis|Drug: Pazopanib Hydrochloride National Cancer Institute (NCI) Phase 2 2008-02-01 2017-01-31
    NCT01158521 Clear Cell Renal Cell Carcinoma|Stage I Renal Cell Cancer|Stage II Renal Cell Cancer|Stage III Renal Cell Cancer Drug: pazopanib hydrochloride|Procedure: therapeutic conventional surgery Case Comprehensive Cancer Center Phase 2 2010-06-01 2016-01-08
    NCT01340794 Extra-Adrenal Paraganglioma|Metastatic Adrenal Gland Pheochromocytoma|Paraganglioma|Recurrent Adrenal Gland Pheochromocytoma Other: Laboratory Biomarker Analysis|Drug: Pazopanib Hydrochloride National Cancer Institute (NCI) Phase 2 2011-05-01 2016-06-09
    NCT01599832 Clear Cell Renal Cell Carcinoma|Recurrent Renal Cell Cancer|Stage IV Renal Cell Cancer Drug: pazopanib hydrochloride|Other: laboratory biomarker analysis|Procedure: dynamic contrast-enhanced magnetic resonance imaging|Other: pharmacogenomic studies University of Chicago|National Cancer Institute (NCI) 2012-06-01 2016-06-29
    NCT00454363 Gastrin-Producing Neuroendocrine Tumor|Lung Carcinoid Tumor|Metastatic Digestive System Neuroendocrine Tumor G1|Multiple Endocrine Neoplasia Type 1|Pancreatic Glucagonoma|Pancreatic Insulinoma|Pancreatic Polypeptide Tumor|Recurrent Digestive System Neuroendocrine Tumor G1|Recurrent Pancreatic Neuroendocrine Carcinoma|Regional Digestive System Neuroendocrine Tumor G1|Somatostatin-Producing Neuroendocrine Tumor Other: Laboratory Biomarker Analysis|Drug: Pazopanib Hydrochloride|Other: Pharmacological Study National Cancer Institute (NCI) Phase 2 2007-03-01 2015-10-15
    NCT00861913 Recurrent Melanoma|Stage IV Skin Melanoma Other: Laboratory Biomarker Analysis|Drug: Pazopanib Hydrochloride|Other: Pharmacological Study National Cancer Institute (NCI) Phase 2 2009-04-01 2017-03-03
    NCT00454142 Recurrent Lymphoepithelioma of the Nasopharynx|Recurrent Squamous Cell Carcinoma of the Nasopharynx|Stage IV Lymphoepithelioma of the Nasopharynx|Stage IV Squamous Cell Carcinoma of the Nasopharynx Drug: pazopanib hydrochloride|Other: pharmacological study|Procedure: computed tomography National Cancer Institute (NCI) Phase 2 2007-08-01 2015-11-16
    NCT01684397 Clear Cell Renal Cell Carcinoma|Stage IV Renal Cell Cancer Biological: Bevacizumab|Other: Laboratory Biomarker Analysis|Drug: Pazopanib Hydrochloride|Other: Pharmacological Study Roswell Park Cancer Institute|National Cancer Institute (NCI)|GlaxoSmithKline Phase 1|Phase 2 2012-10-05 2017-03-07
    NCT02357810 Adult Liposarcoma|Metastatic Liposarcoma|Metastatic Osteosarcoma|Recurrent Adult Soft Tissue Sarcoma|Recurrent Liposarcoma|Recurrent Osteosarcoma|Stage IV Adult Soft Tissue Sarcoma Drug: Pazopanib Hydrochloride|Drug: Oral Topotecan Hydrochloride|Other: Laboratory Biomarker Analysis Northwestern University|GlaxoSmithKline|National Cancer Institute (NCI) Phase 2 2015-02-01 2016-12-13
    NCT01532687 Adult Alveolar Soft Part Sarcoma|Adult Angiosarcoma|Adult Desmoplastic Small Round Cell Tumor|Adult Epithelioid Hemangioendothelioma|Adult Epithelioid Sarcoma|Adult Extraskeletal Myxoid Chondrosarcoma|Adult Extraskeletal Osteosarcoma|Adult Fibrosarcoma|Adult Leiomyosarcoma|Adult Liposarcoma|Adult Malignant Mesenchymoma|Adult Malignant Peripheral Nerve Sheath Tumor|Adult Rhabdomyosarcoma|Adult Synovial Sarcoma|Adult Undifferentiated Pleomorphic Sarcoma|Malignant Adult Hemangiopericytoma|Recurrent Adult Soft Tissue Sarcoma|Stage III Adult Soft Tissue Sarcoma|Stage IV Adult Soft Tissue Sarcoma Drug: Gemcitabine Hydrochloride|Other: Laboratory Biomarker Analysis|Drug: Pazopanib Hydrochloride|Other: Placebo OHSU Knight Cancer Institute|National Cancer Institute (NCI) Phase 2 2012-03-01 2016-11-14
    NCT02601209 High Grade Sarcoma|Metastatic Leiomyosarcoma|Metastatic Malignant Peripheral Nerve Sheath Tumor|Metastatic Synovial Sarcoma|Metastatic Undifferentiated Pleomorphic Sarcoma|Myxofibrosarcoma|Recurrent Leiomyosarcoma|Recurrent Malignant Peripheral Nerve Sheath Tumor|Recurrent Synovial Sarcoma|Recurrent Undifferentiated Pleomorphic Sarcoma|Uterine Corpus Leiomyosarcoma Other: Laboratory Biomarker Analysis|Drug: Pazopanib Hydrochloride|Drug: Sapanisertib National Cancer Institute (NCI) Phase 1|Phase 2 2015-11-01 2017-01-31
    NCT01713972 Unspecified Adult Solid Tumor, Protocol Specific Drug: dabrafenib|Drug: pazopanib hydrochloride|Other: Correlative studies Manisha Shah|National Comprehensive Cancer Network|Ohio State University Comprehensive Cancer Center Phase 1 2012-11-01 2016-09-12
    NCT01841736 Atypical Carcinoid Tumor|Foregut Carcinoid Tumor|Hindgut Carcinoid Tumor|Lung Carcinoid Tumor|Metastatic Carcinoid Tumor|Metastatic Digestive System Neuroendocrine Tumor G1|Midgut Carcinoid Tumor|Recurrent Digestive System Neuroendocrine Tumor G1|Regional Digestive System Neuroendocrine Tumor G1 Other: Laboratory Biomarker Analysis|Drug: Pazopanib Hydrochloride|Other: Placebo|Other: Quality-of-Life Assessment National Cancer Institute (NCI) Phase 2 2013-06-01 2016-12-28
    NCT00486642 Hormone-Resistant Prostate Cancer|Recurrent Prostate Carcinoma Drug: Bicalutamide|Other: Laboratory Biomarker Analysis|Drug: Pazopanib Hydrochloride|Other: Pharmacological Study National Cancer Institute (NCI) Phase 2 2007-09-01 2015-08-03
    NCT01413113 Recurrent Thyroid Cancer|Stage IVA Follicular Thyroid Cancer|Stage IVA Papillary Thyroid Cancer|Stage IVB Follicular Thyroid Cancer|Stage IVB Papillary Thyroid Cancer|Stage IVC Follicular Thyroid Cancer|Stage IVC Papillary Thyroid Cancer Drug: pazopanib hydrochloride|Radiation: iodine I 131 University of Washington|GlaxoSmithKline|National Cancer Institute (NCI)|National Comprehensive Cancer Network Phase 1 2011-12-01 2015-11-04
    NCT01575548 Clear Cell Renal Cell Carcinoma|Recurrent Renal Cell Carcinoma|Stage IV Renal Cell Cancer Drug: Pazopanib Hydrochloride|Other: Pharmacological Study|Other: Placebo|Other: Quality-of-Life Assessment|Other: Questionnaire Administration National Cancer Institute (NCI) Phase 3 2012-08-01 2017-03-23

    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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