Tasquinimod
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.
Tasquinimod是一种口服的喹啉-3-甲酰胺,具有有效的抗血管生成和抗肿瘤生长的能力,有希望用于治疗晚期前列腺癌[1]。
Tasquinimod可以显著上调TSP-1的表达,下调VEGF和HIF-1α的表达。Tasquinimod的抗血管生成活性是由于其在MDSCs(骨髓来源的抑制性细胞)中对S100A9/TLR4的双重抑制以及在内皮细胞和肿瘤细胞中对HIF1-α和HDAC4/N-CoR/HDACs去乙酰化的抑制,从而抑制缺氧诱导的血管生成。
培养的人内皮和前列腺癌细胞以及人前列腺癌异种移植阉割雄性裸鼠用于评估放疗和放疗与tasquinimod联合使用的效应。由于tasquinimod可以有效减少内皮细胞、癌细胞、TAMs(肿瘤相关巨噬细胞)和MDSCs(骨髓来源的抑制性细胞)中的低氧反应,因而tasquinimod可以抑制肿瘤血管生成,同时保留已形成的血管。体外和体内的数据表明,tasquinimod作为单药治疗具有有效的抗癌活性,而与docetaxel、雄激素剥夺治疗或放疗联合使用可以显著提高其抗癌活性[1,3]。
在临床应用相关的药物水平,tasquinimod显著增强分次放疗的抗癌效果。I期和II期临床研究表明,在有轻微CRPC(去势抵抗性前列腺癌)症状的患者中,tasquinimod耐受性良好,可以显著提高4.3个月的的存活率,抑制肿瘤转移。结果表明,tasquinimod作为一个极有前途和急需的治疗手段可用于治疗CRPC[1,2]。
参考文献:
[1]. Williamson SC, Hartley AE, Heer R. A review of tasquinimod in the treatment of advanced prostate cancer. Drug Design Development And Therapy, 2013, 7: 167-174.
[2]. Olsson A, Bjork A, Vallon-Christersson J, et al. Tasquinimod (ABR-215050), a quinoline-3-carboxamide anti-angiogenic agent, modulates the expression of thrombospondin-1 in human prostate tumors. Molecular Cancer, 2010, 9: 107.
[3]. Dalrymple SL, Becker RE, Zhou HM, et al. Tasquinimod prevents the angiogenic rebound induced by fractionated radiation resulting in an enhanced therapeutic response of prostate cancer xenografts. Prostate, 2012, 72(6): 638-648.
- 1. Shunan Liu, Yanyan Song, et al. "RAGE Inhibitors as Alternatives to Dexamethasone for Managing Cerebral Edema Following Brain Tumor Surgery." Neurotherapeutics. 2022 Mar;19(2):635-648. PMID:35226341
- 2. Inna I. Paramonova, Natalia A. Vilchinskaya, et al. "HDAC4 Is Indispensable for Reduced Slow Myosin Expression at the Early Stage of Hindlimb Unloading in Rat Soleus Muscle." Pharmaceuticals (Basel). 2021 Nov 16;14(11):1167. PMID:34832949
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 406.36 |
Cas No. | 254964-60-8 |
Formula | C20H17F3N2O4 |
Synonyms | ABR-215050;ABR215050;ABR 215050 |
Solubility | insoluble in H2O; ≥20.32 mg/mL in DMSO; ≥4.75 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[4-(trifluoromethyl)phenyl]quinoline-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | CN1C2=C(C(=CC=C2)OC)C(=C(C1=O)C(=O)N(C)C3=CC=C(C=C3)C(F)(F)F)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 |
LNCaP细胞 |
溶解方法 |
在DMSO中的溶解度>10 mM。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。 |
反应条件 |
24 h;50 μM |
应用 |
基于四个独立的生物学重复而产生微阵列数据表明,在LNCaP细胞中,50μM tasquinimod处理24小时后对基因表达的药物诱导效应。RT-PCR获得的表达数据与微阵列分析数据一致,tasquinimod显著上调THBS1、GDF15和CYP1A1的表达,而CXCR4和AGER1的表达没有显著变化。 |
动物实验[2]: | |
动物模型 |
雄性无胸腺BALB / c裸鼠(8周龄) |
剂量 |
10 mg/kg/day;口服给药 |
应用 |
除了以前报道的tasquinimod对肿瘤生长的效应,为了研究tasquinimod早期治疗是否能抑制肿瘤的建立,在LNCaP细胞皮下接种时即开始治疗,并与接种一周后肿瘤生长已建立时再开始治疗进行比较。将对照组中肿瘤成瘤率设为100%,tasquinimod(10 mg/kg/day)在接种时治疗可将肿瘤成瘤率减少到12.5 %,而接种后1周治疗时肿瘤成瘤率仅减少到87.5%(P<0.01)。此外,当从第七天开始治疗时,tasquinimod减少已建立肿瘤的大小。 |
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] Olsson A, Bj?rk A, Vallon-Christersson J, et al. Research Tasquinimod (ABR-215050), a quinoline-3-carboxamide anti-angiogenic agent, modulates the expression of thrombospondin-1 in human prostate tumors[J]. 2010. [2] Jennbacken K, Welen K, Olsson A, et al. Inhibition of metastasis in a castration resistant prostate cancer model by the quinoline‐3‐carboxamide tasquinimod (ABR‐215050)[J]. The Prostate, 2012, 72(8): 913-924. |
描述 | Tasquinimod是一种口服的抗癌药。 | |||||
靶点 | tumor microenvironment | |||||
IC50 |
质量控制和MSDS
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