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AZD4547

AZD4547是一种新型选择性的FGFR抑制剂，靶向作用于FGFR1/2/3，IC50为0.2 nM/2.5 nM/1.8 nM，对FGFR4， VEGFR2(KDR)具有微弱的作用活性，但对IGFR， CDK2和p38几乎没有作用活性。

目录号
EY0881
EY0881
EY0881
EY0881
EY0881
纯度
99.28%
99.28%
99.28%
99.28%
99.28%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
320
715
910
2600
4305
售价
320
715
910
2600
4305
库存
现货
现货
现货
现货
现货
订购
订购
订购
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  • 生物活性

    AZD4547 has been demonstrated to inhibit cell proliferation and inhibit FGFRs and their downstream markers including PLCg and FRS2 phosphorylation in breast cell line Sum52-PE (expressing wild-type FGFR2), multiple myeloma line KMS11 (expressing Y373C mutated FGFR3 protein) and acute myeloid leukemia cell line KG1a (expressing wild-type FGFR1).

  • 体外研究

  • 体内研究

    4% DMSO+30% PEG 300

  • 激酶实验

  • 细胞实验

    ~1 μM

  • 动物实验

    1.5-50 mg/kg 口服饲喂，每天一次或两次

  • 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 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。

  • 参考文献

    [1] Gavine PR, et al. Cancer Res, 2012, 72(8), 2045-2056.

    分子式
    C26H33N5O3    		 分子量
    463.58    		 CAS号
    1035270-39-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    95 mg/mL     		Water
    <1 mg/mL    		 Ethanol
    <1 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
    NCT02965378 Recurrent Squamous Cell Lung Carcinoma|Stage IV Squamous Cell Lung Carcinoma Drug: FGFR Inhibitor AZD4547|Other: Laboratory Biomarker Analysis Southwest Oncology Group|National Cancer Institute (NCI) Phase 2|Phase 3 2014-06-01 2016-11-14
    NCT01824901 Recurrent Non-small Cell Lung Cancer|Squamous Cell Lung Cancer Drug: docetaxel|Drug: AZD4547 ECOG-ACRIN Cancer Research Group|National Cancer Institute (NCI)|Eastern Cooperative Oncology Group Phase 1|Phase 2 2013-09-01 2016-02-01
    NCT01791985 Breast Cancer Drug: AZD4547 / anastrozole or letrozole Imperial College London|Cancer Research UK|AstraZeneca Phase 1|Phase 2 2012-07-01 2015-06-22
    NCT01213160 Cancer|Advanced Solid Malignancies Drug: AZD4547 AstraZeneca Phase 1 2010-11-01 2016-06-28
    NCT00979134 Cancer|Advanced Solid Malignancies Drug: AZD4547|Drug: AZD4547|Drug: AZD4547 AstraZeneca Phase 1 2009-10-01 2015-06-25
    NCT02824133 Recurrent IDHwt Gliomas With FGFR3-TACC3 Fusion|Recurrent IDHwt Gliomas With FGFR1-TACC1 Fusion Drug: AZD4547 Assistance Publique - H么pitaux de Paris Phase 1|Phase 2 2015-09-01 2016-08-12
    NCT01457846 Gastro-oesophageal Junction Cancer|Gastric Cancer Drug: AZD4547|Drug: paclitaxel AstraZeneca Phase 2 2011-11-01 2017-01-16
    NCT01795768 Gastric Cancer|Oesophageal Cancer|Breast Cancer|Squamous Cell Carcinoma of the Lung Drug: AZD 4547 Royal Marsden NHS Foundation Trust|AstraZeneca Phase 2 2012-09-01 2013-03-14
    NCT01202591 FGFR Inhibition, Pharmacokinetics, Biomarkers|ER+ Breast Cancer Drug: AZD4547|Drug: Exemestane|Drug: Placebo|Drug: Fulvestrant AstraZeneca Phase 1|Phase 2 2010-12-01 2016-01-13
    NCT02546661 Muscle Invasive Bladder Cancer Drug: AZD4547|Drug: Durvalumab|Drug: Olaparib|Drug: AZD1775|Drug: Vistusertib AstraZeneca Phase 1 2016-10-01 2017-01-27
    NCT02154490 Recurrent Squamous Cell Lung Carcinoma|Stage IV Squamous Cell Lung Carcinoma Drug: Docetaxel|Biological: Durvalumab|Drug: Erlotinib Hydrochloride|Drug: FGFR Inhibitor AZD4547|Biological: Ipilimumab|Other: Laboratory Biomarker Analysis|Biological: Nivolumab|Drug: Palbociclib|Biological: Rilotumumab|Drug: Taselisib Southwest Oncology Group|National Cancer Institute (NCI) Phase 2|Phase 3 2014-06-01 2017-03-03
    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
    NCT02664935 Non-Small Cell Lung Cancer|Carcinoma, Squamous Cell|Adenocarcinoma Drug: AZD4547|Drug: AZD2014|Drug: Palbociclib|Drug: Crizotinib|Drug: Selumetinib|Drug: Docetaxel|Drug: AZD5363|Drug: AZD9291|Drug: MEDI4736 University of Birmingham|Cancer Research UK|AstraZeneca|Pfizer|Experimental Cancer Medicine Centre Network Phase 2 2015-03-01 2016-10-24
    NCT02117167 Non-small Cell Lung Cancer Metastatic Drug: AZD2014|Drug: AZD4547|Drug: AZD5363|Drug: AZD8931|Drug: Selumetinib|Drug: Vandetanib|Drug: Erlotinib|Drug: Pemetrexed|Drug: MEDI4736 UNICANCER|IFCT|Fondation ARC|AstraZeneca Phase 2 2014-04-01 2016-02-19
    NCT02299999 Metastatic Breast Cancer Drug: AZD2014|Drug: AZD4547|Drug: AZD5363|Drug: AZD8931|Drug: Selumetinib|Drug: Vandetanib|Drug: Bicalutamide|Drug: Olaparib|Drug: Anthracyclines|Drug: Taxanes|Drug: cyclophosphamide|Drug: DNA intercalators|Drug: Methotrexate|Drug: vinca alkaloids|Drug: Platinum based chemotherapies|Drug: Bevacizumab|Drug: Mitomycine C|Drug: Eribuline|Drug: MEDI4736 UNICANCER|Fondation ARC|AstraZeneca Phase 2 2014-04-01 2016-02-19

    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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