AZ5104

AZ-5104,AZ 5104

AZ-5104是一种有效的EGFR抑制剂, 在体内外具有抗肿瘤活性。

目录号
EY0359
EY0359
EY0359
EY0359
纯度
99.43%
99.43%
99.43%
99.43%
规格
5 mg
10 mg
50 mg
100 mg
原价
480
778
2200
3300
售价
480
778
2200
3300
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

    AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 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] Cross DA, et al. Cancer Discov. 2014, 4(9), 1046-1061.
    [2] Ivana Sullivan,et al. Next-Generation EGFR Tyrosine Kinase Inhibitors for Treating EGFR-Mutant Lung Cancer beyond First Line. Front Med (Lausanne) 2016; 3: 76. Published online 2017 Jan 18. doi: 10.3389/fmed.2016.00076.

    分子式
    C27H31N7O2
    分子量
    485.58
    CAS号
    1421373-98-9
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    89 mg/mL
    Water
    <1 mg/mL
    Ethanol
    18 mg/mL

    体内溶解度

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

    NCT02529995 Carcinoma, Non-Small-Cell Lung With EGFR Mutation Positive Drug: AZD9291 40 mg|Drug: AZD9291 80 mg AstraZeneca Phase 1 2015-08-01 2017-01-13
    NCT02197247 Non Small Cell Lung Cancer Procedure: Pharmacokinetic sampling - AZD9291|Drug: Rifampicin|Drug: AZD9291 tablet dosing|Procedure: Pharmacokinetic sampling - rifampicin|Procedure: Pharmacokinetic sampling - AZ5140 and AZ7550 AstraZeneca Phase 1 2014-12-01 2017-02-03
    NCT02161770 Solid Tumours Drug: AZD9291 tablet dosing|Procedure: Pharmacokinetic sampling - AZD9291|Procedure: Pharmacokinetic sampling - AZ5140 and AZ7550 AstraZeneca Phase 1 2014-12-22 2017-03-21
    NCT02163733 Advanced Non Small Cell Lung Cancer|Advanced (Inoperable) Non Small Cell Lung Cancer Drug: AZD9291 tablets|Procedure: Pharmacokinetic sampling - AZD9291|Other: Dietary Fasted|Other: Dietary High Fat|Procedure: Pharmacokinetic sampling - AZ5140 and AZ7550 AstraZeneca Phase 1 2014-11-01 2017-02-03
    NCT02491944 Oncology Drug: AZD9291|Drug: [14C]AZD9291 AstraZeneca Phase 1 2015-07-01 2016-08-19
    NCT02224053 Healthy Volunteer Procedure: Pharmacokinetic sampling - AZD9291|Drug: AZD9291 tablet dosing|Drug: Omeprazole tablet dosing|Procedure: Pharmacokinetic sampling - AZ5140 and AZ7550 AstraZeneca Phase 1 2014-09-01 2016-05-23
    NCT02317016 Non Small Cell Lung Cancer Procedure: Pharmacokinetic sampling - AZD9291|Drug: AZD9291 tablet dosing|Drug: Rosuvastatin|Procedure: Pharmacokinetic sampling - rosuvastatin|Procedure: Pharmacokinetic sampling - AZ5140 and AZ7550 AstraZeneca Phase 1 2015-03-01 2017-02-03
    NCT02157883 Advanced Non Small Cell Lung Cancer|Advanced (Inoperable) Non Small Cell Lung Cancer Procedure: Pharmacokinetic sampling|Drug: AZD9291|Drug: Itraconazole AstraZeneca Phase 1 2014-11-01 2017-01-09
    NCT02096679 Healthy Volunteers Drug: AZD9291 AstraZeneca Phase 1 2014-05-01 2015-10-01
    NCT02923947 Solid Tumours Drug: Osimertinib; AZD9291 AstraZeneca|Quintiles, Inc. Phase 1 2017-01-01 2016-10-03
    NCT02908750 Non Small Cell Lung Cancer Drug: Fexofenadine tablet dosing|Drug: Osimertininb tablet dosing AstraZeneca|Quintiles, Inc. Phase 1 2017-01-01 2016-09-23
    NCT02511106 Stage IB-IIIA Non-small Cell Lung Carcinoma Drug: AZD9291 80 mg/40 mg|Drug: Placebo AZD9291 80 mg/40 mg AstraZeneca|Parexel Phase 3 2015-10-01 2017-02-28
    NCT02296125 Locally Advanced or Metastatic EGFR Sensitising Mutation Positive Non Small Cell Lung Cancer Drug: AZD9291 80 mg/40 mg + placebo|Drug: Placebo Erlotinib 150/100mg|Drug: Placebo Gefitinib 250 mg|Drug: Erlotinib 150/100 mg|Drug: Gefitinib 250 mg|Drug: Placebo AZD9291 80 mg/ 40 mg AstraZeneca|Parexel Phase 3 2014-12-03 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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