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。
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.
0 μM -10 μM
0 mg/kg, 10 mg/kg, 30 mg/kg或100 mg/kg 口服
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。
[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
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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