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抑制剂/激活剂

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凋亡与自噬

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Nintedanib 尼达尼布; BIBF 1120

Nintedanib (BIBF 1120) 是一种有效的三重血管激酶抑制剂，抑制 VEGFR1/2/3，FGFR1/2/3 和 PDGFRα/β 的 IC50 值分别为 34 nM/13 nM/13 nM，69 nM/37 nM/108 nM 和 59 nM/65 nM。

货号：
TK0549
规格：

1mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	656247-17-5
生物活性	Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
分子式	C31H33N5O4
分子量	539.62
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 11.5 mg/mL (21.31 mM; Need ultrasonic)
体内研究	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.
体外研究	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).
文献	•Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •Br J Cancer. 2020 Mar;122(7):986-994. •Free Radic Biol Med. 2021 May 11;S0891-5849(21)00291-4. •Am J Respir Cell Mol Biol. 2021 Mar 24. •Am J Respir Cell Mol Biol. 2020 Feb;62(2):178-190. •Am J Respir Cell Mol Biol. 2019 Apr;60(4):478-487. •Am J Respir Cell Mol Biol. 2019 Jul;61(1):74-85. •Stem Cell Res Ther. 2020 Nov 25;11(1):496. •Acta Pharmacol Sin. 2021 Mar 2. •J Cell Biochem. 2020 Mar;121(3):2343-2353. •J Photochem Photobiol B. 2016 Feb 5;157:70-76. •Sci Rep. 2018 Jun 22;8(1):9540. •J Pharmacol Exp Ther. 2019 Jun;369(3):511-522. •Oncol Rep. 2016 Dec;36(6):3123-3130. •J Nat Prod. 2019 May 24;82(5):1331-1337. •PLoS One. 2019 Aug 6;14(8):e0218632. •Fundam Clin Pharmacol. 2021 Feb 1. •Journal of Molecular Structure. 2016 Jul 5; 1115:171-179. •Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11. •Nature Machine Intelligence. 2020 Jun. •Harvard Medical School LINCS LIBRARY
纯度及产品资料	98%

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