Cabozantinib malate (XL184)
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.
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
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