VE-822

VE822,VE 822

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。

目录号
EY0438
EY0438
EY0438
纯度
99.17%
99.17%
99.17%
规格
5 mg
10 mg
50 mg
原价
750
980
1800
售价
750
980
1800
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    VE-822 is an ATR inhibitor with IC50 of 19 nM in HT29 cells.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    60 mg/kg 口服灌胃

  • 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] 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

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

    NCT02723864 Neoplasms Drug: Veliparib + VX-970 + Cisplatin National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 1 2016-03-22 2017-03-21
    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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