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BGJ398

NVP-BGJ398,NVP-BGJ 398,NVP-BGJ-398

BGJ398 (NVP-BGJ398)是一种选择性的FGFR抑制剂，作用于FGFR1/2/3，IC50为0.9 nM/1.4 nM/1 nM，作用于FGFR比作用于FGFR4和VEGFR2选择性高40倍以上，对Abl， Fyn， Kit， Lck， Lyn和Yes几乎没有抑制活性。

目录号
EY1367
EY1367
EY1367
EY1367
纯度
99.41%
99.41%
99.41%
99.41%
规格
5 mg
10 mg
50 mg
100 mg
原价
450
580
1100
1800
售价
450
580
1100
1800
库存
现货
现货
现货
现货
订购
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  • 生物活性

    NVP-BGJ398 is a potent, selective, and orally bioavailable inhibitor of the FGFR tyrosine kinases. NVP-BGJ398 is a small molecular with the formula of C26H31Cl2N7O3 and Molecular Weight of 560. The fibroblast growth factor receptor 1 (FGFR1), FGFR2, FGFR3, and FGFR4, encompasses the receptors for 18 different FGF ligands. These ligand–receptor combinations regulate a broad spectrum of signaling during development and in normal growth control. BGJ398 inhibits the cell proliferation and induces apoptosis in cancer cells and suppresses tumor growth in xenograft model.

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% Propylene glycol

  • 激酶实验

  • 细胞实验

    0 μM-0.1 μM

  • 动物实验

    10 mg/kg/qd和30 mg/kg/qd 口服处理

  • 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] Guagnano V, et al. J Med Chem. 2011, 54(20), 7066-7083.

    分子式
    C26H31Cl2N7O3    		 分子量
    560.48    		 CAS号
    872511-34-7    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    1 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
    NCT02160041 Solid Tumor|Hematologic Malignancies Drug: BGJ398 Novartis Pharmaceuticals|Novartis Phase 2 2014-07-01
    NCT02657486 Bladder Cancer|Non-Muscle-Invasive Urothelial Carcinoma Drug: BGJ398 Memorial Sloan Kettering Cancer Center 2016-01-01
    NCT01975701 Recurrent Glioblastoma or Other Glioma Subtypes Drug: BGJ398 Novartis Pharmaceuticals|Novartis Phase 2 2013-12-01
    NCT01697605 Tumor With Alterations of the FGF-R Drug: BGJ398 Novartis Pharmaceuticals|Novartis Phase 1 2012-10-19
    NCT01928459 Advanced Solid Tumors|Metastatic Solid Tumors Drug: BGJ398|Drug: BYL719 Novartis Pharmaceuticals|Novartis Phase 1 2013-10-01
    NCT02150967 Advanced Cholangiocarcinoma Drug: BGJ398 Novartis Pharmaceuticals|Novartis Phase 2 2014-07-14
    NCT02257541 Advanced Gastrointestinal Stromal Tumor (GIST) Drug: BGJ398|Drug: Imatinib Mesylate Memorial Sloan Kettering Cancer Center|Dana-Farber Cancer Institute|M.D. Anderson Cancer Center|University of Pittsburgh Phase 1|Phase 2 2014-10-02
    NCT02312804 Cancer of Cervix|Tumors Drug: BGJ398|Drug: Carboplatin|Drug: Paclitaxel The University of Texas Health Science Center at San Antonio Phase 1 2015-01-01
    NCT02706691 Head and Neck Squamous Cell Carcinoma Drug: BGJ398 University of Chicago Phase 2 2016-10-01
    NCT02575508 Colon Adenocarcinoma|Metastatic Pancreatic Adenocarcinoma|Pancreatic Adenocarcinoma|Pancreatic Ductal Adenocarcinoma|Rectal Adenocarcinoma|Stage III Pancreatic Cancer|Stage IIIA Colon Cancer|Stage IIIA Rectal Cancer|Stage IIIB Colon Cancer|Stage IIIB Rectal Cancer|Stage IIIC Colon Cancer|Stage IIIC Rectal Cancer|Stage IV Pancreatic Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer Drug: Fluorouracil|Drug: Irinotecan Hydrochloride|Other: Laboratory Biomarker Analysis|Drug: Oxaliplatin|Drug: pan FGFR Kinase Inhibitor BGJ398|Other: Pharmacological Study Roswell Park Cancer Institute|National Cancer Institute (NCI) Phase 1|Phase 2 null
    NCT01004224 Advanced Solid Tumors With Alterations of FGFR1, 2 and or 3|Squamous Lung Cancer With FGFR1 Amplification|Bladder Cancer With FGFR3 Mutation or Fusion|Advanced Solid Tumors With FGFR1 Amplication|Advanced Solid Tumors With FGFR2 Amplication|Advanced Solid Tumors With FGFR3 Mutation Drug: BGJ398 Novartis Pharmaceuticals|Novartis Phase 1 2009-12-11

    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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