(S)-crizotinib是一种强效的MTH1 (NUDT1)抑制剂,其IC50为72 nM。
(S)-crizotinib, the (S)-enantiomer of crizotinib, is a potent MTH1 (NUDT1) inhibitor with IC50 of 72 nM in a cell-free assay.
~5 μM
1% DMSO, 10% 乙醇, 10%克列莫佛, 10% 吐温80, 69% PBS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] 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
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。
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