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656247-18-6生产厂家

656247-18-6价格

656247-18-6

656247-18-6结构式
656247-18-6结构式

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中文名 (3Z)-2,3-二氢-3-[[[4-[甲基[2-(4-甲基-1-哌嗪基)乙酰]氨基]苯基]氨基]苯亚甲基]-2-氧代-1H-吲哚-6-甲酸甲酯乙磺酸盐
英文名 nintedanib esylate
中文别名 尼达尼布乙基磺酸盐
乙磺酸尼达尼布
尼达尼布乙磺酸盐
英文别名 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone monoethanesulfonate salt
3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-ethylene]-6-methoxycarbonyl-2-indolinone monoethanesulfonate
UNII:42F62RTZ4G
methyl (3S,5R)-3,5-di[(tert-butyldimethylsilyl)oxy]-1-hydroxy-cyclohexanecarboxylate
nintedanib ethanesulfonate salt
Ethanesulfonic acid - methyl (3Z)-3-{[(4-{methyl[(4-methyl-1-pipe razinyl)acetyl]amino}phenyl)amino](phenyl)methylene}-2-oxo-6-indo linecarboxylate (1:1)
Nintedanib ethanesulfonate
(3S,5S)-3,5-Bis[[(1,1-dimethylethyl)dimethylsilyl]oxy]-1-hydroxy-cyclohexanecarboxylic Acid Methyl Ester
1H-Indole-6-carboxylic acid, 2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-, methyl ester, (3Z)-, compd. with ethanesulfonic acid (1:1)
methyl (3S,5S)-3,5-bis[tert-butyl(dimethyl)silyloxy]-1-hydroxy-cyclohexanecarboxylate
3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone monoethanesulfonate
Ethanesulfonic acid - methyl (3Z)-3-{[(4-{methyl[(4-methyl-1-piperazinyl)acetyl]amino}phenyl)amino](phenyl)methylene}-2-oxo-6-indolinecarboxylate (1:1)
Vargatef
3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone monoethanesulphonate
Methyl (3Z)-3-[({4-[N-methyl-2-(4-methylpiperazin-1-yl)acetamido]phenyl}amino)(phenyl)methylidene]-2-oxo-2,3-dihydro-1H-indole-6-carboxylate ethanesulfonate
methyl (3Z)-3-[({4-[N-methyl-2-(4-methylpiperazin-1-yl)acetamido]phenyl}amino)(phenyl)methylidene]-2-oxo-2,3-dihydro-1H-indole-6-carboxylate ethanesulfonate salt
BIBF 1120 esylate
BIBF 1120 (esylate)
描述 Nintedanib esylate (BIBF 1120 esylate) 是一种有效的 VEGFR1/2/3,FGFR1/2/3 和 PDGFRα/β 三重抑制剂,IC50 值分别为 34 nM/13 nM/13 nM,69 nM/37 nM/108 nM 和 59 nM/65 nM。
相关类别
靶点

VEGFR1:34 nM (IC50)

VEGFR2:13 nM (IC50)

VEGFR3:13 nM (IC50)

FGFR1:69 nM (IC50)

FGFR2:37 nM (IC50)

FGFR3:108 nM (IC50)

PDGFRα:59 nM (IC50)

PDGFRβ:65 nM (IC50)

体外研究 Nintedanib(BIBF 1120)与激酶结构域的氨基和羧基末端裂片之间的裂缝中的ATP结合位点结合。 Nintedanib(BIBF 1120)在细胞试验中抑制PDGF-BB刺激的BRP的增殖,EC50为79nM。在用5%血清加PDGF-BB刺激后,Nintedanib(BIBF 1120)(100nM)阻断MAPK的活化。 Nintedanib(BIBF 1120)可阻止PDGF-BB刺激增殖,在人血管平滑肌细胞(HUASMC)培养物中EC50为69 nM [1]。
体内研究 Nintedanib(BIBF 1120)(25-100mg/kg每日口服)在所有肿瘤模型中具有高活性,包括在裸鼠中生长的人肿瘤异种移植物和同系大鼠肿瘤模型。这在3天后肿瘤灌注的磁共振成像中显而易见,5天后血管密度和血管完整性降低,并且生长受到严重抑制[1]。 Nintedanib(BIBF 1120)可口服,在体内肿瘤模型中显示出令人鼓舞的功效,同时耐受性良好[2]。
动物实验 使用5周龄至6周龄的无胸腺NMRI-nu / nu雌性小鼠(21-31g)进行测定。适应环境后,将小鼠用1至5×106(100μL)FaDu,Caki-1,SKOV-3,H460,HT-29或PAC-120细胞接种到动物的右侧腹部。适应环境后,将F344 Fischer大鼠用5×106(100μL)GS-9L细胞皮下注射到动物的右侧腹部。对于药代动力学分析,在小鼠眶后丛的指定时间点分离血液,并使用高效液相色谱 - 质谱法[1]分析血浆。
参考文献

[1]. Hilberg F, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res, 2008, 68(12), 4774-4782.

[2]. Roth GJ, et al. Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). J Med Chem, 2009, 52(14), 4466-4480.

[3]. Suzuki N, et al. Effect of a novel oral chemotherapeutic agent containing a combination of trifluridine, tipiracil and the novel triple angiokinase inhibitor nintedanib, on human colorectal cancer xenografts. Oncol Rep. 2016 Dec;36(6):3123-3130.

分子式 C33H39N5O7S
分子量 649.757
精确质量 649.257019
PSA 160.46000
LogP 4.62470
外观性状 粉末
储存条件 -20℃

~96%

656247-18-6结构式

656247-18-6

文献:BOEHRINGER INGELHEIM INTERNATIONAL GMBH Patent: WO2009/71523 A1, 2009 ; Location in patent: Page/Page column 4; 25-27 ;
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