Nintedanib esylate|656247-18-6|(乙磺酸尼达尼布; BIBF 1120 esylate)-陌孚医药/Medlife

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Nintedanib esylate (Synonyms: 乙磺酸尼达尼布; BIBF 1120 esylate)

目录号: PL09004 纯度: ≥99%

CAS No. :656247-18-6

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中文名称	Nintedanib esylate
中文别名	(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;尼达尼布乙磺酸盐;乙磺酸尼达尼布;尼达尼布单乙基磺酸盐;INTEDANIB尼达尼布乙烷磺酸盐;尼达尼布乙基磺酸盐;BIBF1120 乙磺酸酯盐;乙烷磺酸尼达尼布;尼达尼布乙磺酸(Intedanib乙磺酸)
英文名称	Nintedanib esylate
英文别名	BIBF 1120 esylate;(3Z)-2,3-DIHYDRO-3-[[[4-[METHYL[2-(4-METHYL-1-PIPERAZINYL)ACETYL]AMINO]PHENYL]AMINO]PHENYLMETHYLENE]-2-OXO-1H-INDOLE-6-...;(3Z)-2,3-Dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-1H-indole-6-carboxylic acid methyl ester ethanesulfonate;(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate;BIBF 1120 ethanesulfonate salt;BIBF1120;BIBF-1120 esylate;Intedanib ethanesulfonate;Nintedanib Esylate;Nintedanib Ethanesulfonate Salt;Nintedanib, Ethanesulfonate Salt (BIBF1120 Esylate, Intedanib Esylate, Vargatef®);Nintedanib ethanesulfonate;Trinidad Neeb esylate;(3Z)-2,3-Dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-1H-indole-6-carboxylic acid methyl ester ethanesulfonate;Nintedanib ethanesulfonate;BIBF 1120 esylate;BIBF-1120 esylate;Nintedanib esylate;Nintedanib ethanesulfonate salt;BIBF1120/nintedanib ethanesulfonate salt;Trinidad Neeb esylate;OFEV;BIBF 1120 (esylate);42F62RTZ4G;Nintedanib Esilate;BCP09963;NSC753000;Nintedanib esylate
Cas No.	656247-18-6
分子式	C₃₃H₃₉N₅O₇S
分子量	649.76
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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。

生物活性

Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC 50 s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

性状

Solid

IC50 & Target[1][2]

VEGFR1 34 nM (IC50) VEGFR2 13 nM (IC5

体外研究(In Vitro)

Nintedanib (BIBF 1120) binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. Nintedanib (BIBF 1120) inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. Nintedanib (BIBF 1120) (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. Nintedanib (BIBF 1120) prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Nintedanib (BIBF 1120) (25-100 mg/kg daily p.o.) is highly active in all tumor models, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model. This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and profound growth inhibition. Nintedanib (BIBF 1120) is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

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]. 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.

溶解度数据	In Vitro: DMSO : 66.67 mg/mL (102.61 mM; Need ultrasonic)H₂O : 16.67 mg/mL (25.66 mM; Need ultrasonic)Ethanol : 3.08 mg/mL (4.74 mM; Need ultrasonic)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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