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Tasquinimod

现货
Catalog No.
A3860
抗血管生成和抗肿瘤剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,500.00
现货
5mg
¥ 1,400.00
现货
10mg
¥ 2,000.00
现货
50mg
¥ 6,000.00
现货
200mg
¥ 14,000.00
现货

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Background

Tasquinimod is an orally administered quinoline-3-carboxamide with potent antiangiogenic and antitumorigenic ability that has shown promise in the treatment of advanced prostate cancers [1].
Treatment with tasquinimod leads to a remarkable up-regulation in the expression of TSP-1 and down-regulation of VEGF and HIF-1α. The antiangiogenic activities of tasquinimod are therefore due to the dual inhibition of S100A9/TLR4 in MDSCs and the inhibition of HDAC4/N-CoR/HDACs deacetylation of HIF1-α in both endothelial and tumor cells, inhibiting hypoxia induced angiogenesis.
Human endothelial and prostate cancer cells in culture and human prostate cancer xenografts growing in castrated male nude mice were evaluated for their response to radiation alone and in combination with tasquinimod. Due to its potent reduction of the hypoxic response in endothelial cells, cancer cells, TAMs and MDSCs, tasquinimod inhibits tumor angiogenesis while sparing already formed vasculature. The data obtained in vivo and in vitro highlights a potent anticancer effect as a monotherapy in addition to greatly improving the response to combination therapies with docetaxel, androgen deprivation therapy or radiotherapy [1, 3].
At clinically relevant drug levels, tasquinimod significantly enhances anti-cancer efficacy of fractionated radiation with optimal timing for initiating daily tasquinimod treatment being after completion of the fractionated radiation. Phase I and II studies of tasquinimod have demonstrated tasquinimod to be well-tolerated and lead to significant improvements in progression-free survival from metastasis, by a period of 4.3 months, in patients with minimally symptomatic CRPC. The result highlights tasquinimod as an extremely promising and much needed therapeutic tool for use in CRPC [1, 2].
References:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt406.36
Cas No.254964-60-8
FormulaC20H17F3N2O4
SynonymsABR-215050;ABR215050;ABR 215050
Solubility≥20.318 mg/mL in DMSO, ≥4.75 mg/mL in EtOH with ultrasonic and warming, <2.47 mg/mL in H2O
Chemical Name4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[4-(trifluoromethyl)phenyl]quinoline-3-carboxamide
SDFDownload SDF
Canonical SMILESCN1C2=C(C(=CC=C2)OC)C(=C(C1=O)C(=O)N(C)C3=CC=C(C=C3)C(F)(F)F)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

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.

生物活性

描述 Tasquinimod是一种口服的抗癌药。
靶点 tumor microenvironment          
IC50            

质量控制

化学结构

Tasquinimod