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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
O=C(C1=CC2=C(OC3=CC=C(C(Cl)=C3)NC(NC4CC4)=O)C=CN=C2C=C1OC)N.O=S(O)(C)=O
InChI
1S/C21H19ClN4O4.CH4O3S/c1-29-19-10-17-13(9-14(19)20(23)27)18(6-7-24-17)30-12-4-5-16(15(22)8-12)26-21(28)25-11-2-3-11;1-5(2,3)4/h4-11H,2-3H2,1H3,(H2,23,27)(H2,25,26,28);1H3,(H,2,3,4)
InChI key
HWLFIUUAYLEFCT-UHFFFAOYSA-N
生化/生理作用
Lenvatinib (E7080)是一种针对多种受体酪氨酸激酶的口服活性抑制剂,包括VEGFR (Flt-1/KDR/Flt-4 IC50 = 22/4.0/5.2 nM)、PDGFR1/2 (IC50 = 39/51 nM)、FGFR1和KIT (IC50分别= 46和100 nM),可抑制体外血管生成(VEGF/ scf诱导HUVEC管形成IC50 = 5.1/5.2 nM)。口服Lenvatinib可导致产生scf的人小细胞肺癌H146细胞的小鼠体内肿瘤生长停滞(30 mg/kg b.i.p.o)甚至退化(100 mg/kg b.i.p.o)。
口服活性受体酪氨酸激酶抑制剂(Flt-1/KDR/Flt-4), PDGFR1/2, FGFR1和KIT具有抗血管生成的体外和体内疗效。
警示用语:
Warning
危险声明
危险分类
Repr. 2 - STOT RE 2
靶器官
Gastro-intestinal system,Kidney,Bone,Reproductive organs,Adrenal gland
储存分类代码
11 - Combustible Solids
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Journal of molecular neuroscience : MN, 70(9), 1437-1444 (2020-05-10)
The therapeutic effect of deferoxamine (DFO) for spinal cord injury (SCI) has been demonstrated in previous studies; however, the exact mechanism of action is still unclear. Here, we hypothesized that DFO ameliorates spinal cord compression by promoting neovascularization. Using an
International journal of molecular sciences, 21(9) (2020-05-14)
Multiple kinase inhibitors are available for patients with advanced hepatocellular carcinoma (HCC). It is largely unknown whether regorafenib or lenvatinib modulates innate immunity including Toll-like receptor (TLR)-signaling pathways in HCC. We performed real-time RT-PCR to investigate 84 TLR-associated gene expression
Oncology reports, 44(4), 1709-1716 (2020-09-19)
Anaplastic thyroid carcinoma (ATC) is a rare type of thyroid carcinoma with a poor prognosis. Thus, suitable preclinical tumor models are required for the development of new ATC therapies. In the present study, orthotopic tumor xenograft models were established using
Liver cancer, 9(3), 338-357 (2020-07-11)
Combining anti-angiogenic therapy with immune checkpoint blockade with anti-programmed cell death-1 (PD-1) antibodies is a promising treatment for hepatocellular carcinoma (HCC). Tyrosine kinase inhibitors are well-known anti-angiogenic agents and offer potential for combination with anti-PD-1 antibodies. This study investigated the
International journal of cancer, 122(3), 664-671 (2007-10-19)
E7080 is an orally active inhibitor of multiple receptor tyrosine kinases including VEGF, FGF and SCF receptors. In this study, we show the inhibitory activity of E7080 against SCF-induced angiogenesis in vitro and tumor growth of SCF-producing human small cell
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