CAS NO: | 656247-18-6 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
1 g | 电议 |
5 g | 电议 |
生物活性 | Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor forVEGFR1/2/3,FGFR1/2/3andPDGFRα/βwithIC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively. | ||||||||||||||||
IC50& Target[1] |
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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 EC50of 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 EC50of 69 nM in cultures of human vascular smooth muscle cells (HUASMC)[1]. | ||||||||||||||||
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[1]. Nintedanib (BIBF 1120) is orally available and displays encouraging efficacy inin vivotumor models while being well tolerated[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 649.76 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C33H39N5O7S | ||||||||||||||||
CAS 号 | 656247-18-6 | ||||||||||||||||
中文名称 | 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 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | 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) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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