Home > CDK & > Flavopiridol

Flavopiridol

夫拉平度,弗拉平度,NSC 649890 HCl,NSC-649890 HCl,NSC649890 HCl,Alvocidib,HMR 1275,HMR1275,HMR-1275

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。

目录号
EY1731
EY1731
EY1731
EY1731
纯度
99.26%
99.26%
99.26%
99.26%
规格
5 mg
10 mg
50 mg
100 mg
原价
480
690
2520
3490
售价
480
690
2520
3490
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    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.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~10 μM

  • 动物实验

    ~7.5 mg/kg/day 腹腔注射

  • 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] 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

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    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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