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Dasatinib Monohydrate

达沙替尼,一水达沙替尼,BMS-354825 Monohydrate

Dasatinib是一种Src/Abl抑制剂，IC50分别为0.6 nM和0.8 nM。

目录号
EY0800
EY0800
EY0800
EY0800
纯度
99.66%
99.66%
99.66%
99.66%
规格
10 mg
25 mg
50 mg
100 mg
原价
300
400
500
750
售价
300
400
500
750
库存
现货
现货
现货
现货
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  • 生物活性

    Dasatinib is a small-molecule inhibitor of both the Src and Bcr-Abl tyrosine kinases with IC50 values of 0.5 nM and 1 nM. The oncogenic tyrosine kinase Bcr-Abl, plays a critical role in the pathogenesis of CML (chronic myelogenous leukemia). In most CML patients, the kinase domain of Bcr-Abl have mutations that interfere with binding to the first Abl kinase inhibitor, but Dasatinib bind more efficiently to these Abl kinase mutations and thus more effective than imatinib in inhibiting the proliferation cells with wild-type Bcr-Abl or Bcr-Abl mutants.

  • 体外研究

  • 体内研究

    1% DMSO+30% PEG 300+1% Tween 80

  • 激酶实验

  • 细胞实验

    0 nM-32 nM

  • 动物实验

    30 mg/kg 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 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] O'Hare T, et al. Cancer Res. 2005, 65(11), 4500-4505.

    分子式
    C22H26ClN7O2S    		 分子量
    488.01    		 CAS号
    302962-49-8    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    200 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
    NCT02596828 Pineoblastoma Drug: Temozolomide|Drug: Irinotecan|Drug: Dasatinib|Drug: Rapamycin University of Regensburg Phase 2 2016-04-01 2016-12-29
    NCT01467986 Neuroblastoma Recurrent Drug: Dasatinib|Drug: Rapamycin|Drug: Irinotecan|Drug: Temozolomide|Drug: Irinotecan|Drug: Temozolomide University of Regensburg Phase 2 2013-08-01 2016-12-29
    NCT00720109 Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1|Childhood B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia Drug: Asparaginase|Drug: Cyclophosphamide|Drug: Cytarabine|Drug: Dasatinib|Drug: Daunorubicin Hydrochloride|Drug: Dexamethasone|Drug: Etoposide|Biological: Filgrastim|Drug: Hydrocortisone Sodium Succinate|Drug: Ifosfamide|Other: Laboratory Biomarker Analysis|Drug: Leucovorin Calcium|Drug: Mercaptopurine|Drug: Methotrexate|Drug: Methylprednisolone|Drug: Pegaspargase|Drug: Prednisone|Radiation: Radiation Therapy|Drug: Vincristine Sulfate National Cancer Institute (NCI) Phase 2|Phase 3 2008-07-01 2016-09-08
    NCT01256398 Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1|Untreated Adult Acute Lymphoblastic Leukemia Biological: Alemtuzumab|Procedure: Allogeneic Hematopoietic Stem Cell Transplantation|Procedure: Autologous Hematopoietic Stem Cell Transplantation|Drug: Cyclophosphamide|Drug: Cytarabine|Drug: Dasatinib|Drug: Daunorubicin Hydrochloride|Drug: Dexamethasone|Drug: Etoposide Phosphate|Biological: Filgrastim|Drug: Fludarabine Phosphate|Procedure: In Vitro-Treated Peripheral Blood Stem Cell Transplantation|Other: Laboratory Biomarker Analysis|Drug: Leucovorin Calcium|Drug: Melphalan|Drug: Mercaptopurine|Drug: Methotrexate|Biological: Pegfilgrastim|Other: Pharmacological Study|Drug: Tacrolimus|Drug: Vincristine Sulfate National Cancer Institute (NCI) Phase 2 2010-12-01 2017-01-31
    NCT02143414 B Acute Lymphoblastic Leukemia|B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1|B Acute Lymphoblastic Leukemia, Philadelphia Chromosome Negative|Philadelphia Chromosome Positive|Recurrent Adult Acute Lymphoblastic Leukemia|Refractory Adult Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia Biological: Blinatumomab|Drug: Dasatinib|Other: Laboratory Biomarker Analysis|Drug: Mercaptopurine|Drug: Methotrexate|Drug: Prednisone|Drug: Vincristine Sulfate National Cancer Institute (NCI) Phase 2 2015-01-01 2017-03-08
    NCT02883049 B Acute Lymphoblastic Leukemia|Bone Necrosis|Central Nervous System Leukemia|Cognitive Side Effects of Cancer Therapy|Neurotoxicity Syndrome|Pain|Testicular Leukemia|Therapy-Related Toxicity|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia Drug: Clofarabine|Drug: Cyclophosphamide|Drug: Cytarabine|Drug: Dasatinib|Drug: Dexamethasone|Drug: Doxorubicin Hydrochloride|Drug: Etoposide|Drug: Hydrocortisone Sodium Succinate|Other: Laboratory Biomarker Analysis|Drug: Leucovorin Calcium|Drug: Mercaptopurine|Drug: Methotrexate|Drug: Pegaspargase|Drug: Prednisone|Radiation: Radiation Therapy|Drug: Thioguanine|Drug: Vincristine Sulfate National Cancer Institute (NCI) Phase 3 2012-02-01 2017-03-20
    NCT00792948 Adult Acute Lymphoblastic Leukemia in Remission|Adult B Acute Lymphoblastic Leukemia|Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1|Adult L1 Acute Lymphoblastic Leukemia|Adult L2 Acute Lymphoblastic Leukemia|Adult T Acute Lymphoblastic Leukemia|Recurrent Adult Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia Procedure: Allogeneic Hematopoietic Stem Cell Transplantation|Drug: Cyclophosphamide|Drug: Cytarabine|Drug: Dasatinib|Drug: Dexamethasone|Drug: Doxorubicin Hydrochloride|Drug: Etoposide|Biological: Filgrastim|Other: Laboratory Biomarker Analysis|Drug: Leucovorin Calcium|Drug: Methotrexate|Drug: Methylprednisolone|Procedure: Peripheral Blood Stem Cell Transplantation|Drug: Prednisone|Drug: Sirolimus|Drug: Tacrolimus|Radiation: Total-Body Irradiation|Drug: Vincristine Sulfate National Cancer Institute (NCI) Phase 2 2009-09-01 2016-09-09
    NCT03023046 Adult Acute Lymphoblastic Leukemia|Adult Lymphoblastic Lymphoma|CD20 Positive|Philadelphia Chromosome Positive Drug: Cyclophosphamide|Drug: Dasatinib|Drug: Doxorubicin|Drug: Etoposide|Drug: Imatinib Mesylate|Other: Laboratory Biomarker Analysis|Drug: Prednisone|Biological: Rituximab|Drug: Vincristine Sulfate University of Washington|National Cancer Institute (NCI) Phase 2 2017-02-23 2017-02-28

    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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