Home > others & > (S)-crizotinib

(S)-crizotinib

crizotinib,

(S)-crizotinib是一种强效的MTH1 (NUDT1)抑制剂,其IC50为72 nM。

目录号
EY0890
EY0890
EY0890
EY0890
纯度
99.41%
99.41%
99.41%
99.41%
规格
5 mg
10 mg
25 mg
50 mg
原价
550
880
1400
2100
售价
550
880
1400
2100
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

    (S)-crizotinib, the (S)-enantiomer of crizotinib, is a potent MTH1 (NUDT1) inhibitor with IC50 of 72 nM in a cell-free assay.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~5 μM

  • 动物实验

    1% DMSO, 10% 乙醇, 10%克列莫佛, 10% 吐温80, 69% PBS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] Huber et al (2014) Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature 508 222.

    分子式
    C21H22Cl2FN5O
    分子量
    450.34
    CAS号
    1374356-45-2
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    42 mg/mL
    Water
    <1 mg/mL
    Ethanol
    23 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
    NCT02134912 Adenocarcinoma of the Lung|Large Cell Lung Cancer|Recurrent Non-small Cell Lung Cancer|Stage IV Non-small Cell Lung Cancer Drug: crizotinib|Drug: pemetrexed disodium|Other: laboratory biomarker analysis|Other: pharmacological study Southwest Oncology Group|National Cancer Institute (NCI) Phase 2 2014-08-01 2016-10-26
    NCT02761057 Recurrent Renal Cell Carcinoma|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer|Type 1 Papillary Renal Cell Carcinoma|Type 2 Papillary Renal Cell Carcinoma Drug: Cabozantinib S-malate|Drug: Crizotinib|Other: Laboratory Biomarker Analysis|Drug: Sunitinib Malate|Drug: Volitinib National Cancer Institute (NCI) Phase 2 2016-04-01 2017-03-23
    NCT02604342 Non-small Cell Lung Cancer Drug: Alectinib|Drug: Docetaxel|Drug: Pemetrexed Hoffmann-La Roche Phase 3 2015-11-03 2017-03-14
    NCT02838420 Anaplastic Lymphoma Kinase-positive Non-small Cell Lung Cancer Drug: Alectinib|Drug: Crizotinib Hoffmann-La Roche Phase 3 2016-08-01 2016-11-01
    NCT01744652 Advanced Cancers Drug: Crizotinib|Drug: Dasatinib M.D. Anderson Cancer Center|Pfizer Phase 1 2013-03-01 2016-09-26
    NCT01441128 Carcinoma, Non-Small Cell Lung|Adenocarcinoma|Carcinoma, Squamous Cell|Carcinoma, Large Cell Drug: PF-02341066/PF-00299804|Drug: PF-02341066/PF-00299804 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 1 2011-09-01 2017-01-24
    NCT01154140 Non Squamous Lung Cancer Drug: treatment|Drug: treatment Pfizer Phase 3 2011-01-01 2017-01-17
    NCT02737501 Non-small Cell Lung Cancer|Lung Cancer|Advanced Malignancies|Carcinoma Drug: Brigatinib|Drug: Xalkori (crizotinib) Ariad Pharmaceuticals Phase 3 2016-04-01 2017-03-06
    NCT03090815 Adenocarcinoma of Lung (Disorder) Genetic: Sequencing of ctDNA in plasma The University of Hong Kong|Feinstein Institute for Medical Research 2016-02-01 2017-03-20
    NCT02314364 Non-small Cell Lung Cancer Metastatic|Targetable Oncogenes (EGFR, ALK, ROS1) Radiation: SBRT with protons or photons Massachusetts General Hospital|National Cancer Institute (NCI) Phase 2 2014-12-01 2017-03-14
    NCT02767804 Non-small Cell Lung Cancer Drug: X-396 (ensartinib)|Drug: crizotinib Xcovery Holding Company, LLC Phase 3 2016-06-01 2017-03-15
    NCT02499614 Carcinoma, Non-Small-Cell Lung Drug: Crizotinib Fondazione Ricerca Traslazionale Phase 2 2014-12-01 2015-07-14
    NCT02075840 Non-Small Cell Lung Cancer Drug: Alectinib|Drug: Crizotinib Hoffmann-La Roche Phase 3 2014-08-01 2017-02-23
    NCT00932451 Carcinoma, Non-Small-Cell Lung Drug: PF-02341066 Pfizer Phase 2 2010-01-01 2016-11-17
    NCT00932893 Carcinoma, Non-Small-Cell Lung Drug: PF-02341066|Drug: Pemetrexed|Drug: Docetaxel Pfizer Phase 3 2009-09-01 2016-10-31
    NCT02465060 Advanced Malignant Neoplasm|Lymphoma|Recurrent Malignant Solid Neoplasm|Recurrent Plasma Cell Myeloma|Refractory Malignant Neoplasm|Refractory Plasma Cell Myeloma Drug: Afatinib|Drug: Akt inhibitor AZD5363|Drug: Binimetinib|Drug: Crizotinib|Other: Cytology Specimen Collection Procedure|Drug: Dabrafenib|Drug: Dasatinib|Drug: Defactinib|Drug: FGFR Inhibitor AZD4547|Other: Laboratory Biomarker Analysis|Biological: Nivolumab|Drug: Osimertinib|Drug: Palbociclib|Biological: Pertuzumab|Drug: PI3K-beta Inhibitor GSK2636771|Drug: Sapanisertib|Drug: Sunitinib Malate|Drug: Taselisib|Drug: Trametinib|Biological: Trastuzumab Emtansine|Drug: Trk Inhibitor LOXO-101|Drug: Vismodegib|Drug: WEE1 Inhibitor AZD1775 National Cancer Institute (NCI) Phase 2 2015-08-01 2017-03-23
    NCT01606878 Recurrent Childhood Anaplastic Large Cell Lymphoma|Recurrent Neuroblastoma|Unspecified Childhood Solid Tumor, Protocol Specific Drug: crizotinib|Drug: cyclophosphamide|Drug: topotecan hydrochloride|Drug: vincristine sulfate|Drug: dexrazoxane hydrochloride|Drug: doxorubicin hydrochloride|Other: pharmacological study|Other: laboratory biomarker analysis|Other: pharmacogenomic studies|Other: questionnaire administration Children's Oncology Group|National Cancer Institute (NCI) Phase 1 2013-03-01 2017-02-13
    NCT00939770 Brain and Central Nervous System Tumors|Lymphoma|Neuroblastoma|Unspecified Childhood Solid Tumor, Protocol Specific Drug: crizotinib|Other: pharmacogenomic studies|Other: pharmacological study Children's Oncology Group|National Cancer Institute (NCI) Phase 1|Phase 2 2009-09-01 2016-01-14
    NCT01979536 Anaplastic Large Cell Lymphoma, ALK-Positive|CD30-Positive Neoplastic Cells Present|Stage II Childhood Anaplastic Large Cell Lymphoma|Stage III Childhood Anaplastic Large Cell Lymphoma|Stage IV Childhood Anaplastic Large Cell Lymphoma Drug: Brentuximab Vedotin|Drug: Crizotinib|Drug: Cyclophosphamide|Drug: Cytarabine|Drug: Dexamethasone|Drug: Doxorubicin Hydrochloride|Drug: Etoposide|Drug: Ifosfamide|Other: Laboratory Biomarker Analysis|Drug: Methotrexate National Cancer Institute (NCI) Phase 2 2013-11-01 2017-03-20

    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。

  • 相关化合物库

  • 使用AMQUAR产品发表文献后请联系我们

相关推荐

X
  • 联系人 :
  • 收件地址 :
  • 电话号码 :
  • 单位名称 :
  • 产品货号 :
  • 产品规格 :
  • 发票抬头以及单位税号 :