Lenvatinib mesylate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

甲磺酸乐伐替尼 (E7080 甲磺酸盐) 是一种口服多靶点酪氨酸激酶抑制剂，可抑制 VEGFR1-3、FGFR1-4、PDGFR、KIT 和 RET，具有有效的抗肿瘤活性。

Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.

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.

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.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.

E7080 mesylate

Angiogenesis

VEGFR

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857890-39-2

522.96

C??H??ClN?O?S

>98% (HPLC)

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

O=C(C1=C(OC)C=C2N=CC=C(OC3=CC=C(NC(NC4CC4)=O)C(Cl)=C3)C2=C1)N.OS(=O)(C)=O

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(-20℃)

With Ice Pack

≥ 2 years