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My CartCAS：656247-17-5
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 656247-17-5 |
| Name | Nintedanib |
| Molecular Formula | C31H33N5O4 |
| Molecular Weight | 539.63 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 1592732-453-0 |
| MDL | MFCD11974012 |
| SMILES | O=C1NC2=CC(C(OC)=O)=CC=C2/C1=C(NC3=CC=C(N(C(CN4CCN(C)CC4)=O)C)C=C3)\C5=CC=CC=C5 |
| Target Point | PDGFR;VEGFR1/2/3;FGFR1/2/3 |
| Passage | Angiogenesis; Protein Tyrosine Kinase/RTK |
| Background | Nintedanib is a potent triple angiokinase inhibitor that inhibits VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β. |
| Biological Activity | 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[1-3]。 |
| In Vitro | Nintedanib结合激酶结构域的氨基和羧基末端裂片之间的裂口中的ATP结合位点。 Nintedanib在细胞测定中抑制PDGF-BB刺激的BRP的增殖，EC50为79nM。用5％血清加PDGF-BB刺激后，Nintedanib(100nM)阻断MAPK的活化。 Nintedanib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]。 |
| In Vivo | Nintedanib(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]。 |
| Animal Experiment | 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 - 质谱法分析血浆。 |
| Kinase Experiment | 在存在或不存在在25％DMSO中进行的Nintedanib的连续稀释的情况下测定酶活性。每个微量滴定板含有内部对照，例如空白，最大反应和历史参考化合物。所有孵育均在室温下在旋转振荡器上进行。将10μL每种Nintedanib稀释液加入10μL稀释的激酶(0.8μg/ mL VEGFR2，10mM Tris pH 7.5，2mM EDTA和2mg/mL BSA)中并预孵育1小时。通过加入30μL含有62.4mM Tris pH 7.5，2.7mM DTT，5.3mM MnCl 2，13.3mM Mg-乙酸盐，0.42mM ATP，0.83mg/mL Poly-Glu-Tyr(4：1)的底物混合物开始反应。)和1.7μg/ mL聚-Glu-Tyr(4：1)- 生物素并孵育1小时。加入50μL250mMEDTA，20mM HEPES，pH7.4终止反应。将90μL反应混合物转移至链霉抗生物素蛋白板并孵育1-2小时。用PBS洗涤三次后，加入EU标记的抗体PY20(推荐在DELFIA测定缓冲液中稀释1：2000的0.5mg/mL标记抗体)。通过三次DELFIA洗涤缓冲液除去过量的检测抗体。然后在多标记读数器上测量前10分钟，将每个孔与100μLDELFIA增强溶液一起温育。 |
| Data Literature Source | [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. |
| Unit | Bottle |
| Specification | 5mg 10mg 50mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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