Flavopiridol (Alvocidib)与ATP竞争性抑制CDKs,包括CDK1, CDK2, CDK4和CDK6,IC50约为40 nM。作用于CDK1, 2, 4, 6比作用于CDK7选择性强7.5倍。Flavopiridol最初被发现能抑制EGFR和PKA。
Flavopiridol (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2.
~10 μM
~7.5 mg/kg/day 腹腔注射
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] Kim KS, et al. J Med Chem, 2000, 43(22), 4126-4134.
分子式 C21H20ClNO5 |
分子量 401.84 |
CAS号 146426-40-6 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 15 mg/mL |
Water <1 mg/mL |
Ethanol 10 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00445341 | Lymphoma | Drug: Flavopiridol | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | Phase 1|Phase 2 | 2007-01-01 | 2012-10-18 |
NCT00101231 | Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Blastic Phase Chronic Myelogenous Leukemia|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Relapsing Chronic Myelogenous Leukemia | Drug: alvocidib | National Cancer Institute (NCI) | Phase 1 | 2004-10-01 | 2013-06-03 |
NCT00058240 | B-cell Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Waldenstr枚m Macroglobulinemia | Drug: alvocidib | National Cancer Institute (NCI) | Phase 1|Phase 2 | 2003-04-01 | 2014-06-06 |
NCT00112723 | Adult Lymphocyte Depletion Hodgkin Lymphoma|Adult Lymphocyte Predominant Hodgkin Lymphoma|Adult Mixed Cellularity Hodgkin Lymphoma|Adult Nodular Sclerosis Hodgkin Lymphoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Grade III Lymphomatoid Granulomatosis|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Refractory Multiple Myeloma|Splenic Marginal Zone Lymphoma|Stage I Multiple Myeloma|Stage II Multiple Myeloma|Stage III Multiple Myeloma|Waldenstr枚m Macroglobulinemia | Drug: alvocidib | National Cancer Institute (NCI) | Phase 1|Phase 2 | 2005-12-01 | 2016-06-27 |
NCT00003620 | B-cell Chronic Lymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia|Stage I Chronic Lymphocytic Leukemia|Stage II Chronic Lymphocytic Leukemia|Stage III Chronic Lymphocytic Leukemia|Stage IV Chronic Lymphocytic Leukemia | Drug: alvocidib|Other: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 2 | 1999-06-01 | 2013-01-16 |
NCT00098371 | B-cell Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia | Drug: alvocidib | National Cancer Institute (NCI) | Phase 2 | 2005-04-01 | 2016-08-31 |
NCT00047203 | Refractory Multiple Myeloma|Stage I Multiple Myeloma|Stage II Multiple Myeloma|Stage III Multiple Myeloma | Drug: alvocidib | National Cancer Institute (NCI) | Phase 2 | 2002-09-01 | 2013-01-15 |
NCT00079352 | Unspecified Adult Solid Tumor, Protocol Specific | Drug: alvocidib|Drug: gemcitabine hydrochloride|Drug: irinotecan hydrochloride | National Cancer Institute (NCI) | Phase 1 | 2004-04-01 | 2013-01-24 |
NCT00047307 | Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage II Pancreatic Cancer|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer | Drug: alvocidib|Drug: gemcitabine hydrochloride|Radiation: 3-dimensional conformal radiation therapy|Other: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 1 | 2002-08-01 | 2013-06-03 |
NCT00278330 | Blastic Phase Chronic Myelogenous Leukemia|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Refractory Anemia With Excess Blasts|Relapsing Chronic Myelogenous Leukemia|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Adult Acute Myeloid Leukemia | Drug: alvocidib|Drug: vorinostat | National Cancer Institute (NCI) | Phase 1 | 2006-01-01 | 2013-04-01 |
NCT00464633 | Leukemia, Lymphocytic, Chronic | Drug: alvocidib | Sanofi | Phase 2 | 2007-03-01 | 2013-02-08 |
NCT00012181 | Recurrent Childhood Brain Stem Glioma|Recurrent Childhood Cerebellar Astrocytoma|Recurrent Childhood Cerebral Astrocytoma|Recurrent Childhood Ependymoma|Recurrent Childhood Large Cell Lymphoma|Recurrent Childhood Liver Cancer|Recurrent Childhood Lymphoblastic Lymphoma|Recurrent Childhood Malignant Germ Cell Tumor|Recurrent Childhood Medulloblastoma|Recurrent Childhood Rhabdomyosarcoma|Recurrent Childhood Small Noncleaved Cell Lymphoma|Recurrent Childhood Soft Tissue Sarcoma|Recurrent Childhood Supratentorial Primitive Neuroectodermal Tumor|Recurrent Childhood Visual Pathway and Hypothalamic Glioma|Recurrent Childhood Visual Pathway Glioma|Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor|Recurrent Neuroblastoma|Recurrent Osteosarcoma|Recurrent Retinoblastoma|Recurrent Wilms Tumor and Other Childhood Kidney Tumors|Recurrent/Refractory Childhood Hodgkin Lymphoma|Unspecified Childhood Solid Tumor, Protocol Specific | Drug: alvocidib|Other: pharmacological study | National Cancer Institute (NCI) | Phase 1 | 2001-04-01 | 2013-07-01 |
NCT00331682 | Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage IV Pancreatic Cancer | Drug: alvocidib|Drug: docetaxel | National Cancer Institute (NCI) | Phase 2 | 2006-03-01 | 2014-05-12 |
NCT00377104 | B-cell Chronic Lymphocytic Leukemia|Contiguous Stage II Small Lymphocytic Lymphoma|Noncontiguous Stage II Small Lymphocytic Lymphoma|Stage I Chronic Lymphocytic Leukemia|Stage I Small Lymphocytic Lymphoma|Stage II Chronic Lymphocytic Leukemia|Stage III Chronic Lymphocytic Leukemia|Stage III Small Lymphocytic Lymphoma|Stage IV Chronic Lymphocytic Leukemia|Stage IV Small Lymphocytic Lymphoma | Drug: alvocidib|Other: pharmacological study|Other: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 1 | 2006-09-01 | 2013-07-01 |
NCT00083122 | Recurrent Ovarian Epithelial Cancer|Recurrent Primary Peritoneal Cavity Cancer|Stage IIIA Ovarian Epithelial Cancer|Stage IIIA Primary Peritoneal Cavity Cancer|Stage IIIB Ovarian Epithelial Cancer|Stage IIIB Primary Peritoneal Cavity Cancer|Stage IIIC Ovarian Epithelial Cancer|Stage IIIC Primary Peritoneal Cavity Cancer|Stage IV Ovarian Epithelial Cancer|Stage IV Primary Peritoneal Cavity Cancer | Drug: cisplatin|Drug: alvocidib|Drug: cisplatin/flavopiridol | National Cancer Institute (NCI) | Phase 2 | 2004-04-01 | 2014-05-06 |
NCT00098579 | Gastrointestinal Stromal Tumor|Recurrent Adult Soft Tissue Sarcoma|Stage IV Adult Soft Tissue Sarcoma | Drug: alvocidib|Drug: doxorubicin hydrochloride | National Cancer Institute (NCI) | Phase 1 | 2004-10-01 | 2013-03-18 |
NCT00324480 | Unspecified Adult Solid Tumor, Protocol Specific | Drug: alvocidib|Drug: vorinostat|Other: pharmacological study | National Cancer Institute (NCI) | Phase 1 | 2006-03-01 | 2014-02-21 |
NCT00112684 | Unspecified Adult Solid Tumor, Protocol Specific | Drug: alvocidib|Other: pharmacological study|Other: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 1 | 2006-02-01 | 2014-02-21 |
NCT00080990 | Unspecified Adult Solid Tumor, Protocol Specific | Drug: alvocidib|Drug: fluorouracil|Drug: oxaliplatin|Drug: leucovorin calcium | National Cancer Institute (NCI) | Phase 1 | 2004-02-01 | 2013-12-13 |
NCT00039455 | HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer | Biological: trastuzumab|Drug: alvocidib|Other: laboratory biomarker analysis|Other: pharmacological study | National Cancer Institute (NCI) | Phase 1 | 2002-04-01 | 2013-01-31 |
NCT00003256 | Prostate Cancer | Drug: alvocidib | National Cancer Institute (NCI) | Phase 2 | 1998-05-01 | 2013-02-08 |
NCT00735930 | Anemia|Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Thrombocytopenia | Drug: Alvocidib Hydrochloride|Drug: Lenalidomide|Other: Pharmacological Study|Other: Laboratory Biomarker Analysis | National Cancer Institute (NCI) | Phase 1 | 2008-08-01 | 2015-04-01 |
NCT00005974 | Sarcoma | Drug: alvocidib | NCIC Clinical Trials Group|Canadian Cancer Trials Group | Phase 2 | 2000-07-01 | 2011-09-27 |
NCT00003039 | Lymphoma | Drug: alvocidib | National Cancer Institute (NCI) | Phase 2 | 1997-09-01 | 2013-02-04 |
NCT00082784 | Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue|Nodal Marginal Zone Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Refractory Plasma Cell Myeloma|Splenic Marginal Zone Lymphoma|Waldenstrom Macroglobulinemia | Drug: Bortezomib|Drug: Alvocidib Hydrochloride|Other: Pharmacological Study | National Cancer Institute (NCI) | Phase 1 | 2004-03-01 | 2014-12-22 |
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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