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lenvatinib Mesylate

lenvatinib Mesylate
lenvatinib Mesylate structure
CAS No.
857890-39-2
Chemical Name:
lenvatinib Mesylate
Synonyms
CAT#A863437;E7080 Mesylate;envatinib MesyL;E7080;E-7080;E 7080;lenvatinib Mesylate;lenvatinib Mesylater;lenvatinib Methanesulfonate;lenvatinib Mesylate (E7080);Lenvatinib Mesylate fandachem;lenvatinib Mesylate USP/EP/BP
CBNumber:
CB42651170
Molecular Formula:
C22H23ClN4O7S
Formula Weight:
522.95862
MOL File:
857890-39-2.mol

lenvatinib Mesylate Properties

FDA UNII
3J78384F61
NCI Dictionary of Cancer Terms
lenvatinib mesylate
NCI Drug Dictionary
lenvatinib mesylate

lenvatinib Mesylate price More Price(3)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 29832 Lenvatinib (mesylate) 857890-39-2 500mg $69 2021-03-22 Buy
Cayman Chemical 29832 Lenvatinib (mesylate) 857890-39-2 5g $345 2021-03-22 Buy
Cayman Chemical 29832 Lenvatinib (mesylate) 857890-39-2 1g $110 2021-03-22 Buy

lenvatinib Mesylate Chemical Properties,Uses,Production

Description

Developed by Eisai Inc., lenvatinib mesylate is a vascular endothelial growth factor receptor (VEGF) inhibitor which has activity against VEGF subtypes 1, 2, and 3 and was approved by the FDA in 2015 for the treatment of differentiated thyroid cancer that is either locally recurrent, metastatic, or progressive and did not respond to radioactive iodine treatment. In May 2016, the FDA approved the drug as a combination therapy with everolimus for the treatment of advanced renal cell carcinoma. Because VEGF (and fibroblast growth factor receptors, known as FGFRs) are thought to play a role in cardiovascular signaling pathways, VEGF2R and FGFR inhibition are thought to be the mechanisms behind the primary side effect of lenvatinib mesylate, which is hypertension.

Uses

E7080 (Lenvatinib) is a multi-target inhibitor of VEGFR2 and VEGFR3 with IC50 of 4 nM and 5.2 nM, respectively.

Definition

ChEBI: A methanesulfonate salt obtained by reaction of lenvatinib with one molar equivalent of methanesulfonic acid. A multi-kinase inhibitor and orphan drug used (as its mesylate salt) for the treatment of various types of thyroid cancer that do not respond to r dioiodine.

Chemical Synthesis

Starting from commercial aniline 193, a substitution reaction under neutral conditions in warm isopropyl alcohol with a commercial vinyl methoxy derivative of Meldrum’s acid (194) produced enamine 195 in good yield. Next, subjection of 195 to DOWTHERM A at 190 °C affected an intramolecular cyclizative substitution reaction, followed by loss of acetone, and a decarboxylation reaction to furnish quinolone 196. This cyclization reaction, which is a variant of the Conrad-Limpach reaction, is particularly noteworthy given the temperature and pH at which it takes place. Conrad- Limpach cyclizations typically proceed under basic conditions at temperatures well above 240 °C. However, a process was developed by Zeneca in 2004 which involved subjecting 195 to the DOWTHERM heat transfer fluid (commercially available from Dow and Sigma-Aldrich, consisting of a eutectic mixture of biphenyl and diphenyl oxide) allowed the team to lower the temperature required for the reaction, clearly observe bubbling of gas indicating the progress of the reaction, and simple cooling and treatment with ether to facilitated precipitate formation. The resulting solid could be collected by filtration and required no additional purification on scale in 80% yield. Quinoline 196 was then converted to the corresponding chloride using thionyl chloride in refluxing DMF, and the resulting ester 197 was converted to the corresponding amide through the use of 28% aqueous ammonia in warm ethanol, which ultimately produced the key chloroquinoline lenvatinib subunit 198 in 80% yield from 197.
       
Commercial aminophenol 199 was converted to the corresponding carbamate through the use of phenyl chloroformate in essentially quantitative yield prior to subjection to cyclopropylamine in chilled DMF, which ultimately furnished urea 201 in 77% overall yield from 200. Next, exposure of phenol 201 to chloroquinoline 198 in the presence of potassium t-butoxide followed by treatment with methanesulfonic acid and acetic acid resulted in clean formation of lenvatinib mesylate (XXV) in 96% yield across the two-step sequence.
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lenvatinib Mesylate Preparation Products And Raw materials

Raw materials

Preparation Products


lenvatinib Mesylate Suppliers

Global( 222)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Jinan Ande Pharmaceutical Co.,Ltd.
+8613256107535
andepharm@163.com CHINA 208 58
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
+86-755-23284190 sales@tianpharm.com CHINA 305 58
Henan DaKen Chemical CO.,LTD.
+86-371-66670886
info@dakenchem.com China 20918 58
Jinan Xinke Pharmaceutical Sci.&Tech. Co.,Ltd.
+8618660188356 +86-531-88259693
maguanglei@xinkeyiyao.com;Tracy.li@xinkeyiyao.com CHINA 29 58
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com CHINA 8909 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26751 60
Anqing Chico Pharmaceutical Co., Ltd.
15380796838
chloewu@chicopharm.cn CHINA 341 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29954 58

View Lastest Price from lenvatinib Mesylate manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-11-29 Lenvatinib Mesylate
857890-39-2
US $1.00 / KG 1KG 99% 50kg Jinan Ande Pharmaceutical Co.,Ltd.
2021-11-27 Lenvatinib Mesylate
857890-39-2
US $0.00-0.00 / Kg/Drum 1KG >99% by HPLC 10kg/month Jinan Xinke Pharmaceutical Sci.&Tech. Co.,Ltd.
2021-11-09 Lenvatinib
857890-39-2
US $0.00 / Kg/Bag 2Kg/Bag 99% up /EP 20 tons Sinoway Industrial co., ltd.

857890-39-2(lenvatinib Mesylate)Related Search:


  • lenvatinib Methanesulfonate
  • E7080 Mesylate
  • 4-[3-Chloro-4-[[(cyclopropylamino)carbonyl]amino]phenoxy]-7-methoxy-6-quinolinecarboxamide monomethanesulfonate
  • 4-[3chloro-4-(N'-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide methanesulfonate
  • CAT#A863437
  • Lenvatinib Mesylate,Amadis Chemical offer CAS#857890-39-2
  • lenvatinib Mesylate
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  • maltitol E:candyli(at)speedgainpharma(dot)com
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  • 4-[3-chloro-4-(N'-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide mesylate
  • lenvatinib Mesylate (E7080)
  • 6-Quinolinecarboxamide,4-[3-chloro-4-[[(cyclopropylamino)carbonyl]amino]phenoxy]-7-methoxy-,monomethanesulfonate
  • envatinib MesyL
  • Lenvatinib Mesylate fandachem
  • lenvatinib Mesylate USP/EP/BP
  • lenvatinib Mesylater
  • 857890-39-2
  • C21H19ClN4O4CH4O3S
  • C22H23ClN4O7S
  • FGF receptor antagonist
  • API
  • API
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