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Lenvatinib mesylate

Time:2016-10-30

Lenvatinib_mesylate

CAS#: 417716-92-8 (mesylate)

Description: Lenvatinib, also known as E7080, is a synthetic, orally available inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR/FLK-1) tyrosine kinase with potential antineoplastic activity. E7080 blocks VEGFR2 activation by VEGF, resulting in inhibition of the VEGF receptor signal transduction pathway, decreased vascular endothelial cell migration and proliferation, and vascular endothelial cell apoptosis.

Synonym: E7080; E-7080; E 7080; Lenvatinib; Lenvatinib mesylate; trade name Lenvima.

IUPAC/Chemical Name: 4-(3-chloro-4-(3-cyclopropylureido)phenoxy)-7-methoxyquinoline-6-carboxamide mesylate

THEORETICAL ANALYSIS

Name: Lenvatinib mesylate
CAS#: 417716-92-8 (mesylate)
Chemical Formula: C22H23ClN4O7S
Exact Mass:
Molecular Weight: 522.96
Elemental Analysis: C, 50.53; H, 4.43; Cl, 6.78; N, 10.71; O, 21.42; S, 6.13

TECHNICAL DATA

Appearance:
White to off-white solid powder
Purity:
>98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition:
Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility:
Soluble in DMSO, not in water
Shelf Life:
>5 years if stored properly
Drug Formulation:
This drug may be formulated in DMSO
Stock Solution Storage:
0 – 4 C for short term (days to weeks), or -20 C for long term (months).

REFERENCES

1: Ikuta K, Yano S, Trung VT, Hanibuchi M, Goto H, Li Q, Wang W, Yamada T, Ogino H, Kakiuchi S, Uehara H, Sekido Y, Uenaka T, Nishioka Y, Sone S. E7080, a multi-tyrosine kinase inhibitor, suppresses the progression of malignant pleural mesothelioma with different proangiogenic cytokine production profiles. Clin Cancer Res. 2009 Dec 1;15(23):7229-37. Epub 2009 Nov 24. PubMed PMID: 19934291.

2: Okamoto N, Chantangsi C, Horák A, Leander BS, Keeling PJ. Molecular phylogeny and description of the novel katablepharid Roombia truncata gen. et sp. nov., and establishment of the Hacrobia taxon nov. PLoS One. 2009 Sep 17;4(9):e7080. PubMed PMID: 19759916; PubMed Central PMCID: PMC2741603.

3: Matsui J, Funahashi Y, Uenaka T, Watanabe T, Tsuruoka A, Asada M. Multi-kinase inhibitor E7080 suppresses lymph node and lung metastases of human mammary breast tumor MDA-MB-231 via inhibition of vascular endothelial growth factor-receptor (VEGF-R) 2 and VEGF-R3 kinase. Clin Cancer Res. 2008 Sep 1;14(17):5459-65. PubMed PMID: 18765537.

4: Koyama N, Magario N, Yamamoto Y, Matsui J, Tsuruoka A. [Anti-tumor effect of E7080, a novel angiogenesis inhibitor]. Nippon Yakurigaku Zasshi. 2008 Aug;132(2):100-4. Review. Japanese. PubMed PMID: 18689959.

5: Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M. E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008 Feb 1;122(3):664-71. PubMed PMID: 17943726.