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Lenvatinib mesylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lenvatinib mesylate图片
CAS NO:857890-39-2
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
仑伐替尼甲酸盐
E7080 mesylate
产品介绍
Lenvatinib mesylate (E7080 mesylate),一种口服,多靶点酪氨酸激酶抑制剂,抑制血管内皮生长因子受体(VEGFR1-3),成纤维细胞生长因子受体(FGFR1-4),血小板衍生生长因子受体(PDGFR),干细胞因子受体(KIT),转染期间重排(RET),显示有效抗癌的活性。
生物活性

Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibitsVEGFR1-3,FGFR1-4,PDGFR,KIT, andRET, shows potent antitumor activities[1][2].

IC50& Target[1][2][3]

VEGFR1

22 nM (IC50)

VEGFR2

4 nM (IC50)

VEGFR3

5.2 nM (IC50)

FGFR1

46 nM (IC50)

FGFR2

 

FGFR3

 

FGFR4

 

PDGFRα

51 nM (IC50)

PDGFRβ

39 nM (IC50)

c-Kit

100 nM (IC50)

RET

 

体外研究
(In Vitro)

Lenvatinib mesylate (E7080 mesylate) has IC50s of 4, 5.2, 22 nM for VEGFR2(KDR), VEGFR3(Flt-4), and VEGFR1/Flt-1, respectively. Lenvatinib inhibits PDGFRα, PDGFRβ, FGFR1, and KIT with IC50s of 51, 39, 46, 100 nM, respectively[3].

体内研究
(In Vivo)

Lenvatinib mesylate (E7080 mesylate) (100 mg/kg, p.o.) is administeredand bevacizumab significantly inhibits local tumor growth at the m.f.p., and at the end of treatment, Lenvatinib mesylate also significantly inhibits metastasis to both regional lymph nodes and distant lung[3].
Lenvatinib mesylate (E7080 mesylate) inhibits the growth of H146 tumor at 30 and 100 mg/kg (BID, QDx21) in a dose-dependent manner and causes tumor regression at 100 mg/kg in H146 xenograft model. IHC analysis with anti-CD31 antibody shows that lenvatinib at 100 mg/kg decreases microvessel density more than anti-VEGF antibody and imatinib treatment[4].

Clinical Trial
分子量

522.96

性状

Solid

Formula

C22H23ClN4O7S

CAS 号

857890-39-2

中文名称

乐伐替尼甲酸盐;仑伐替尼甲酸盐;乐法替尼甲酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 7.35 mg/mL(14.05 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9122 mL9.5610 mL19.1219 mL
5 mM0.3824 mL1.9122 mL3.8244 mL
10 mM0.1912 mL0.9561 mL1.9122 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。