Cabozantinib malate (XL184)
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Cabozantinib malate是一种有效的MET和VEGF受体2抑制剂,其IC50值分别为1.3 nM和0.035 nM[1].
Cabozantinib是一种pan-酪氨酸激酶抑制剂,被研发作为一种口服抗癌药,包括甲状腺髓样癌\胶质母细胞瘤\非小细胞肺癌\胰腺癌\乳腺癌以及结肠癌.Cabozantinib的靶点包括MET\VEGFR2\RET\FLT3\KIT\AXL和TEK.在细胞试验中,Cabozantinib抑制MET\VEGFR2\KIT\FLT3以及AXL磷酸化,其IC50值分别为7.8 μM\1.9 μM\5.0 μM\7.5 μM和42 μM[1,2].
Cabozantinib作为一种pan-酪氨酸激酶抑制剂,可以影响多种生物学过程.Cabozantinib抑制HMVEC细胞的管形成,其IC50值为6.7 nM.在B16F10细胞中,Cabozantinib抑制肝细胞生长因子诱导的癌细胞迁移与侵袭,其IC50值分别为31 nM和9 nM.此外,Cabozantinib对多种肿瘤显示出抗增殖作用,如SNU-5\HS746T\MDA-MB-231和U87MG.据报道,Cabozantinib和Gefitinib联合用药可以有效地抑制耐Gefitinib的HCC827GR6细胞系[1,2].
参考文献:
[1] Yakes F M, Chen J, Tan J, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Molecular cancer therapeutics, 2011, 10(12): 2298-2308.
[2] Zhang Y, Guessous F, Kofman A, et al. XL-184, a MET, VEGFR-2 and RET kinase inhibitor for the treatment of thyroid cancer, glioblastoma multiforme and NSCLC. IDrugs, 2010, 13(2): 112.
Storage | Store at -20°C |
M.Wt | 635.59 |
Cas No. | 1140909-48-3 |
Formula | C32H30FN3O10 |
Solubility | ≥31.8 mg/mL in DMSO; insoluble in H2O; ≥2.5 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;(2S)-2-hydroxybutanedioic acid |
SDF | Download SDF |
Canonical SMILES | COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C=C3)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F.C(C(C(=O)O)O)C(=O)O |
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]: | |
细胞系 |
TT细胞 |
溶解方法 |
在DMSO中的溶解度>31.8mg/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 |
反应时间 |
13.7, 41, 123, 370, 1111, 3333nmol/L 作用1h |
应用 |
Cabozantinib抑制了多种形式的致癌RET激酶活性,包括M918T 和Y791F突变体。并且它抑制了包含RET C634W激活突变的TT肿瘤细胞的增殖,该突变在MEN2A(多发性内分泌瘤2A)和家族性MTC(甲状腺髓样癌)中最常出现。 |
动物实验[2]: | |
动物模型 |
携带H441细胞移植瘤的雌性nu/nu小鼠 |
剂量 |
一次性100 mg/kg,口服 |
应用 |
在小鼠模型中,cabozantinib显著的改变了肿瘤的病理学表现,导致了肿瘤和内皮细胞增殖的降低,增加细胞凋亡,在乳房,肺,胶质瘤模型中剂量依赖性的抑制肿瘤生长。重要的是,在肿瘤转移的模型中,cabozantinib没有增加肺部肿瘤负荷。 |
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。 |
References: [1]. Yakes F M, Chen J, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Molecular cancer therapeutics, 2011, 10(12): 2298-2308. [2]. Zhang Y, Guessous F, et al. XL-184, a MET, VEGFR-2 and RET kinase inhibitor for the treatment of thyroid cancer, glioblastoma multiforme and NSCLC. IDrugs, 2010, 13(2): 112. |
质量控制和MSDS
- 批次:
化学结构
![Cabozantinib malate (XL184)](http://www.apexbt.com//media/diy/images/struct/B1401.png)
相关生物数据
![Cabozantinib malate (XL184) Cabozantinib malate (XL184)](http://www.apexbt.com/media/diy/images/wb/B1401_1.jpg)
相关生物数据
![Cabozantinib malate (XL184) Cabozantinib malate (XL184)](http://www.apexbt.com/media/diy/images/wb/B1401_2.jpg)
相关生物数据
![Cabozantinib malate (XL184) Cabozantinib malate (XL184)](http://www.apexbt.com/media/diy/images/wb/B1401_3.jpg)