VE-822是高亲和力ATR选择性抑制剂,Ki为0.2 nM,对ATM,DNA-PK和mTOR的Ki为34 nM,>4 uM和>1 uM。
VE-822 is an ATR inhibitor with IC50 of 19 nM in HT29 cells.
60 mg/kg 口服灌胃
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] Fokas E, et al. Cell Death Dis, 2012, 3, e441.
分子式 C24H25N5O3S |
分子量 463.55 |
CAS号 1232416-25-9 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 35 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
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NCT02595931 | Advanced Malignant Solid Neoplasm|Metastatic Malignant Neoplasm|Metastatic Malignant Solid Neoplasm|Refractory Malignant Neoplasm|Unresectable Malignant Neoplasm|Unresectable Solid Neoplasm | Drug: ATR Kinase Inhibitor VX-970|Drug: Irinotecan Hydrochloride|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study | National Cancer Institute (NCI) | Phase 1 | 2016-06-01 | 2017-03-13 |
NCT02567422 | Head and Neck Squamous Cell Carcinoma|Stage III Nasal Cavity and Paranasal Sinus Squamous Cell Carcinoma|Stage III Oropharyngeal Squamous Cell Carcinoma|Stage IVA Nasal Cavity and Paranasal Sinus Squamous Cell Carcinoma|Stage IVA Oropharyngeal Squamous Cell Carcinoma|Stage IVB Nasal Cavity and Paranasal Sinus Squamous Cell Carcinoma|Stage IVB Oropharyngeal Squamous Cell Carcinoma|Stage IVC Nasal Cavity and Paranasal Sinus Squamous Cell Carcinoma|Stage IVC Oropharyngeal Squamous Cell Carcinoma | Drug: ATR Kinase Inhibitor VX-970|Drug: Cisplatin|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Radiation: Radiation Therapy | National Cancer Institute (NCI) | Phase 1 | 2016-09-01 | 2017-03-13 |
NCT02589522 | Lung Carcinoma Metastatic in the Brain|Stage IV Non-Small Cell Lung Cancer | Drug: ATR Kinase Inhibitor VX-970|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Other: Quality-of-Life Assessment|Procedure: Therapeutic Conventional Surgery|Radiation: Whole-Brain Radiotherapy | National Cancer Institute (NCI) | Phase 1 | 2016-07-01 | 2017-03-23 |
NCT02595892 | Ovarian Serous Tumor|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma | Drug: ATR Kinase Inhibitor VX-970|Drug: Gemcitabine Hydrochloride|Other: Laboratory Biomarker Analysis | National Cancer Institute (NCI) | Phase 2 | 2016-08-01 | 2017-02-15 |
NCT02487095 | Carcinoma, Non-Small -Cell Lung|Ovarian Neoplasms|Small Cell Lung Carcinoma|Uterine Cervical Neoplasms|Carcinoma, Neuroendocrine | Drug: Topotecan|Drug: VX-970 | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | Phase 1|Phase 2 | 2015-06-18 | 2017-03-23 |
NCT02567409 | Metastatic Urothelial Carcinoma of the Renal Pelvis and Ureter|Stage IV Bladder Urothelial Carcinoma | Drug: ATR Kinase Inhibitor VX-970|Drug: Cisplatin|Drug: Gemcitabine Hydrochloride|Other: Laboratory Biomarker Analysis | National Cancer Institute (NCI) | Phase 2 | 2016-08-01 | 2017-03-22 |
NCT02627443 | High Grade Ovarian Serous Adenocarcinoma|Ovarian Endometrioid Tumor|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Stage IV Fallopian Tube Cancer|Stage IV Ovarian Cancer|Stage IV Primary Peritoneal Cancer | Drug: ATR Kinase Inhibitor VX-970|Drug: Carboplatin|Drug: Gemcitabine Hydrochloride|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study | National Cancer Institute (NCI) | Phase 1|Phase 2 | 2016-11-01 | 2017-03-23 |
NCT02157792 | Advanced Solid Tumor | Drug: VX-970|Drug: Gemcitabine|Drug: Cisplatin|Drug: Etoposide|Drug: Carboplatin | Vertex Pharmaceuticals Incorporated | Phase 1 | 2012-12-01 | 2016-11-15 |
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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