SML3915
Cabozantinib malate
≥98% (HPLC)
别名:
BMS 907351 (S)-malate, BMS-907351 (S)-malate, BMS907351 (S)-malate, Cabozantinib (L)-malate, Cabozantinib (S)-malate, N-(4-(6,7-Dimethoxyquinolin-4-yloxy)phenyl)-N’-(4-fluorophenyl)cyclopropane1,1-dicarboxamide, (2S)-hydroxybutanedioate, N-(4-{[6,7-bis(Methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide (L)-malate salt, XL 184 (S)-malate, XL-184 (S)-malate, XL184 (S)-malate
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所有图片(2)
About This Item
经验公式（希尔记法）:
C28H24FN3O5·C4H6O5
CAS号:
分子量:
635.59
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77
质量水平
检测方案
≥98% (HPLC)
形式
powder
储存条件
desiccated
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
生化/生理作用
Orally active, potent receptor tyrosine kinase inhibitor against VEGFR2 (KDR), MET, KIT, RET, AXL, TIE2, and FLT3 with anti-tumor efficacy in vivo.
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).
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).
注意
Hygroscopic
警示用语：
Danger
危险分类
Eye Dam. 1 - Repr. 1B - Skin Irrit. 2 - STOT RE 2
靶器官
Bone marrow,Kidney,Endocrine system,Gastrointestinal tract,Liver
WGK
WGK 3
法规信息
新产品
Cabozantinib: A Multitargeted Oral Tyrosine Kinase Inhibitor
Pharmacotherapy, 38(3), 357-369 (2018)
Cabozantinib Enhances Anti-PD1 Activity and Elicits a Neutrophil-Based Immune Response in Hepatocellular Carcinoma
Clinical Cancer Research, 28(11), 2449-2460 (2022)
F Michael Yakes et al.
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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