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Nintedanib esylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nintedanib esylate图片
CAS NO:656247-18-6
规格:98%
分子量:649.76
包装与价格:
包装价格(元)
1g电议
5g电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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。
CAS:656247-18-6
分子式:C33H39N5O7S
分子量:649.76
纯度:98%
存储:Store at -20°C

Background:

Nintedanib esylate (BIBF 1120 esylate) 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. 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)


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)[1].


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[1]. Nintedanib (BIBF 1120) is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated[2].


[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.