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カボザンチニブリンゴ酸塩

カボザンチニブリンゴ酸塩 化学構造式
1140909-48-3
CAS番号.
1140909-48-3
化学名:
カボザンチニブリンゴ酸塩
别名:
カボザンチニブリンゴ酸塩;カボザンチニブs-リンゴ酸塩;カボザンチニブリンゴ酸塩 (JAN)
英語化学名:
Cabozantinib Malate
英語别名:
Smalate;XL184(S)-malate;XL-184 (Malate);Cabozantnib Malate;CABOZANTINIB MALATE;Carbozanitinb Malate;Cabozantinib L-Malate;Cabozantinib (S)-malate;Cabozantinib L-Malate Salt;XL184(Cabozantinib malate)
CBNumber:
CB22554284
化学式:
C32H30FN3O10
分子量:
635.6
MOL File:
1140909-48-3.mol

カボザンチニブリンゴ酸塩 物理性質

貯蔵温度 :
Sealed in dry,Room Temperature
CAS データベース:
1140909-48-3

安全性情報

カボザンチニブリンゴ酸塩 価格

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入

カボザンチニブリンゴ酸塩 化学特性,用途語,生産方法

効能

抗悪性腫瘍薬, チロシンキナーゼ阻害薬

化学的特性

Off-White Solid

使用

Cabozantinib is a small molecule C-Met modulator. Cabozantinib acts as a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2, Met, FLT3, Tie2 and Kit, respectively. Cabozantinib shows dose-dependent inhibition of tumor growth and tumor regression, associated with disruption of the tumor vasculature and extensive tumor cell a poptosis.

使用

XL184 (Cabozantinib, BMS-907351) is a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2, Met, FLT3, Tie2 and Kit, respectively.

使用

Cabozantinib malate is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.

定義

ChEBI: A malate salt that is the mono-(S)-malate salt of cabozantinib. A multi-tyrosine kinase inhibitor, used for the treatment of progressive, metastatic, medullary thyroid cancer.

臨床応用

Cabozantinib (S)-malate (Cometriq®), which was discovered and developed by Exelixis, gained approval by the U.S. FDA in November 2012. The drug’s indication is for the treatment of medullary thyroid cancer (MTC), and is the second drug for this disease after AstraZeneca’s vandetanib (Caprelsa®). The drug was successfully launched on January 24, 2013. Cabozantinib inhibits multiple receptor tyrosine kinases including RET, MET, VEGFR-1, -2 and -3, KIT, TRKB, FLT-3, AXL, and TIE-2. It is currently also undergoing clinical trials for the treatment of prostate, ovarian, brain, melanoma, breast, non-small cell lung, pancreatic, hepatocellular and kidney cancers.

Chemical Synthesis

Of the three syntheses of cabozantinib reported, the kilo-gram scale process route is described in the scheme.


The preparation began with 6,7-dimethoxy-quinoline-4-ol (46) which upon treatment with POCl3 provided chloride 47 in 70% yield. Exposure of 47 to 4-aminophenol under basic conditions using t- BuONa furnished diaryl ether 48 in 72% yield. This aniline was then coupled with amidoacid chloride 51 (which arose from the activation of commercial diacid 49 to the corresponding monochloride and coupling with p-fluoroaniline and subsequent exposure to oxalyl chloride to furnish the transient acid chloride) to construct cabozantinib as the free base 52 in 95% yield. Salt formation of cabozantinib 52 was carried out with (S)-malic acid, which ultimately delivered the final product of cabozantinib (S)- malate (VIII) in 75% yield.

カボザンチニブリンゴ酸塩 上流と下流の製品情報

原材料

準備製品


カボザンチニブリンゴ酸塩 生産企業

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1140909-48-3(カボザンチニブリンゴ酸塩)キーワード:


  • 1140909-48-3
  • 1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide,(2S)-2-hydroxybutanedioic acid
  • Smalate
  • XL184(S)-malate
  • N-(2-{[(3R)-1-(4-CHLOROBENZYL)-3-PYRROLIDINYL]AMINO}-2-OXOETHYL)-3-(TRIFLUOROMETHYL)BENZAMIDE HYDROCHLORIDE (1:1)
  • Cabozantinib (XL184) S-malate
  • Cabozantinib malate, 98%, a potent VEGFR2 inhibitor
  • Carbozanitinb Malate
  • (2S)-2-Hydroxybutanedioic acid compd. with N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide (1:1)
  • Cabozantinib (S)-malate
  • Cabozantinib L-Malate Salt
  • N-[4-[(6,7-DiMethoxy-4-quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxaMide (2S)-
  • Cabozantinib (S)-Malate(XL-184)
  • CABOZANTINIB MALATE
  • XL184(Cabozantinib malate)
  • Cabozantinib (S)-malate (2S)-2-Hydroxybutanedioic acid compd. with N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide (1:1)
  • Cabozantinib malate, >=99%
  • Cabozantinib L-Malate
  • Cabozantinib Malate (XL184)
  • XL-184 (Malate)
  • XL184;XL-184;CABOZANTINIB;XL 184
  • Cabozantnib Malate
  • Cabozantinib S-malate (XL184 S-malate)
  • Butanedioic acid, 2-hydroxy-, (2S)-, compd. with N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide (1:1)
  • CabozantiCabozantinib Malatenib Malate
  • Cabozantinib (S)-Malate Salt
  • Cabozantinib Malate fandachem
  • quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide
  • N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide 2-hydroxysuccinate
  • Cabozantinib Malate USP/EP/BP
  • カボザンチニブリンゴ酸塩
  • カボザンチニブs-リンゴ酸塩
  • カボザンチニブリンゴ酸塩 (JAN)
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