Tivozanib (AV-951)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Tivozanib是一种酪氨酸激酶抑制剂，对VEGFR-2的IC50值为160 pM[1]。
Tivozanib是一种喹啉-尿素衍生物。作为第2代TKI，其具有皮摩尔级别的对VEGFR-1、-2和-3的效力，及最小的c-kit抑制。Tivozanib对VEGFR-2具有比sunitinib、sorafenib或pazopanib高2个数量级的效价，并有相对较低的脱靶抑制[1]。细胞实验中，Tivozanib也可在纳摩尔级别抑制激酶PDGFR和C-KIT的磷酸化[2]。
除了几个其他实体瘤模型外，Tivozanib在RCC异种移植模型中显示出抗肿瘤活性，使其可用于临床实验评估。多个I期和II起临床试验都证明了Tivozanib的安全和高效。为了比较其在一线与tivozanib和sorafenib效用的差异，III期随机试验也有报道[2]。
参考文献：
[1] M. N. Fishman, S. Srinivas, R.J. Hauke, R.J. Amato, B. Esteves, M.M. Cotreau, A.L. Strahs, W.J. Slichenmyer, P. Bhargava, F.F. Kabbinavar. Phase Ib study of tivozanib (AV-951) in combination with temsirolimus in patients with renal cell carcinoma. European Journal of Cancer. 2013(49):2841-2850.
[2] Viktor Grunwald, Axel Stuart Merseburger. The progression free survival-plateau with vascular endothelial growth factor receptor inhibitors – Is there more to come European Journal of Cancer. 2013(49):2504-2511.
[3] C Lance Cowey. Profile of tivozanib and its potential for the treatment of advanced renal cell carcinoma. Drug Design, Development and Therapy. 2013 (7): 519-527.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 454.86 |
| Cas No. | 475108-18-0 |
| Formula | C22H19ClN4O5 |
| Solubility | ≥22.75 mg/mL in DMSO; insoluble in H2O; ≥2.68 mg/mL in EtOH with gentle warming |
| Chemical Name | 1-[2-chloro-4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(5-methyl-1,2-oxazol-3-yl)urea |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC(=NO1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
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细胞系 |
人卵巢癌细胞系，包括A2780CP, OVCAR3和SKOV3 |
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溶解方法 |
在DMSO中的溶解度>22.8mg/mL。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月 |
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反应时间 |
10μm, 48h |
|
应用 |
Tivozanib和EGFR定向治疗的结合表现出细胞生长抑制和诱导凋亡的协同活性，该现象表明抗VEGFR的靶向途径对EGFR定向治疗有敏化作用。 |
| 临床实验[2]: | |
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疾病模型 |
RCC（肾细胞癌）病人 |
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剂量 |
每日1.5 mg ，3周，口服 |
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应用 |
Tivozanib表现出对VEGFR家族成员的高敏感性抑制。接受tivozanib治疗的病人有着12.7个月的PFS（无进展生存期），这是在mRCC三期临床中报道的最好的PFS。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
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References: [1]. Momeny M1, Sabourinejad Z2,3, et al, Anti-tumour activity of tivozanib, a pan-inhibitor of VEGF receptors, in therapy-resistant ovarian carcinoma cells. Sci Rep. 2017 Apr 6;7:45954. doi: 10.1038/srep45954. [2]. Grünwald V1, Merseburger AS2. The progression free survival-plateau with vascular endothelial growth factor receptor inhibitors – Is there more to come Eur J Cancer. 2013 Jul;49(11):2504-11. doi: 10.1016/j.ejca.2013.03.022. Epub 2013 Apr 16. |
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| Description | Tivozanib是一种酪氨酸激酶抑制剂，对VEGFR-2的IC50值为160 pM。 | |||||
| 靶点 | VEGFR-2 | |||||
| IC50 | 160 pM | |||||
质量控制和MSDS
- 批次:
化学结构
