{{cart_num}}
My CartCAS：212141-51-0
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
Qty：
Size：
| CAS | 212141-51-0 |
| Name | Vatalanib dihydrochloride |
| Molecular Formula | C20H15ClN4·2HCl |
| Molecular Weight | 419.73 |
| Solubility | Soluble in Water/DMSO |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD08458964 |
| SMILES | ClC1=CC=C(C=C1)NC2=NN=C(C3=C2C=CC=C3)CC4=CC=NC=C4.[H]Cl.[H]Cl |
| Target Point | VEGFR |
| Passage | Angiogenesis;Protein Tyrosine Kinase/RTK |
| Background | It is an inhibitor of VEGFR2/KDR. |
| Biological Activity | Vatalanib是VEGFR2/KDR的抑制剂，其IC50值为37nM。Vatalanib还抑制Flk，c-Kit和PDGFRβ，IC50分别为270 nM，730 nM和580 nM。[1-3] |
| In Vitro | Vatalanib通过抑制HUVECs中VEGF诱导的胸苷掺入和IC50为7.1 nM来显示抗增殖作用，并且在相同剂量范围内剂量依赖性地抑制VEGF诱导的内皮细胞存活和迁移，而对细胞没有细胞毒性或抗增殖作用。[1]。最近的一项研究表明，Vatalanib显著抑制肝细胞癌细胞的生长，并通过增加Bax蛋白水平和降低Bcl-xL和Bcl-2来增强IFN/5-FU诱导的细胞凋亡[2]。 |
| In Vivo | 在每日一次口服给药(25-100mg/kg)后，Vatalanib在生长因子植入物模型和肿瘤细胞驱动的血管生成模型中诱导对VEGF和PDGF的血管生成应答的剂量依赖性抑制。在相同剂量范围内，Vatalanib还抑制裸鼠中几种人类癌症的生长和转移，而对循环血细胞或骨髓白细胞没有显著影响[1]。 |
| Cell Experiment | 将HUVEC接种到涂有1.5％明胶的96孔板中。 24小时后，在存在或不存在Vatalanib的情况下，将生长培养基替换为含有1.5％FCS和恒定浓度的VEGF(50ng/mL)，bFGF(0.5ng/mL)或FCS(5％)的基础培养基。 。作为对照，还包括没有生长因子的孔。孵育24小时后，加入BrdUrd标记溶液，并在固定，封闭和添加过氧化物酶标记的抗BrdUrd抗体之前将细胞再孵育24小时。然后使用3，3'5，5'-四甲基联苯胺底物[1]检测结合的抗体。 |
| Animal Experiment | 在植入腔室前1天开始用Vatalanib(12.5，25或50mg/kg二盐酸盐，每天一次)或载体(水)处理小鼠，并在之后持续5天。在治疗结束时，杀死小鼠，并移除室。小心地移除在腔室周围生长的血管化组织并称重，并通过测量组织的血红蛋白含量来评估血液含量[1]。 |
| Kinase Experiment | 每种GST融合的激酶在优化的缓冲条件下孵育。在环境温度下，在存在或不存在测试物质(Vatalanib)的情况下，ATP的总体积为30μL。加入10μL250mMEDTA [1]终止反应。 |
| Data Literature Source | [1]. Wood JM，et al. PTK787/ZK 222584，a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases，impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 2000，60(8 [2]. Murakami M，et al. Tyrosine kinase inhibitor PTK/ZK enhances the antitumor effects of interferon-α/5-fluorouracil therapy for hepatocellular carcinoma cells. Ann Surg Oncol. 2011，18(2)，589-596. [3]. Wan J，et al. Local recurrence of small cell lung cancer following radiofrequency ablation is induced by HIF-1α expression in the transition zone. Oncol Rep. 2016 Mar;35(3):1297-308. |
| Unit | Bottle |
| Specification | 10mg 20mg 50mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
Sorry, there is no more information.
Manual Download
