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Merck
CN

SML3017

Sigma-Aldrich

甲磺酸乐伐替尼

≥98% (HPLC)

别名:

4-[3-氯-4-(N’-环丙基脲)苯氧基]-7-甲氧喹啉-6-甲酰胺甲磺酸盐, 4-[3-氯-4-[(环丙基羰基)氨基]苯氧基]-7-甲氧基-6-喹啉甲酰胺甲磺酸盐, 4-[3-氯-4-[[(环丙胺)羰基]氨基]苯氧基]-7-甲氧基-6-喹啉甲酰胺甲基磺酸盐(1:1), E 7080甲磺酸盐, E-7080甲磺酸盐, E7080甲磺酸盐, ER-203492-00甲磺酸盐, 乐伐替尼甲基磺酸盐

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About This Item

经验公式(希尔记法):
C21H19ClN4O4 · CH4O3S
分子量:
522.96
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77

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。

象形图

Health hazard

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:

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International journal of molecular sciences, 21(9) (2020-05-14)
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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
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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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