所有图片(1)
BMS 907351, BMS-907351, BMS907351, N-(4-(6,7-Dimethoxyquinolin-4-yloxy)phenyl)-N’-(4-fluorophenyl)cyclopropane1,1-dicarboxamide, N-(4-{[6,7-bis(Methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, XL 184, XL-184, XL184
C28H24FN3O5
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生化/生理作用
Cabozantinib (XL184; BMS‐907351) is an orally active, potent inhibitor against multiple receptor tyrosine kinases, notably VEGFR2/KDR (IC50 = 35 pM), MET (IC50 = 1.3 nM/wt, 3.8 nM/Y1248H, 11.8 nM/D1246N, 14.6 nM/K1262R), KIT, RET, AXL, TIE2, and FLT3 (IC50 = 4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib inhibits MET-driven proliferation in cancer cultures (IC50 = 9.9 nM/Hs746T, 19 nM/SNU-5) and simultaneously suppressing metastasis, angiogenesis and tumor growth in vivo (3-100 mg/kg via single or daily p.o. to mice with human MDA-MB-231 xenograft, 1-60 mg/kg via single or daily p.o. to rats with C6 rat glioma).
警示用语:
Danger
危险声明
危险分类
Acute Tox. 4 Oral - Repr. 1B - STOT RE 2
靶器官
Bone marrow,Kidney,Endocrine system,Gastrointestinal tract,Liver
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Cabozantinib Enhances Anti-PD1 Activity and Elicits a Neutrophil-Based Immune Response in Hepatocellular Carcinoma
Clinical Cancer Research, 28(11), 2449-2460 (2022)
Cabozantinib: A Multitargeted Oral Tyrosine Kinase Inhibitor
Pharmacotherapy, 38(3), 357-369 (2018)
Molecular cancer therapeutics, 10(12), 2298-2308 (2011-09-20)
The signaling pathway of the receptor tyrosine kinase MET and its ligand hepatocyte growth factor (HGF) is important for cell growth, survival, and motility and is functionally linked to the signaling pathway of VEGF, which is widely recognized as a
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