产品说明书

Tasquinimod

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Chemical Structure| 254964-60-8 同义名 : ABR-215050
CAS号 : 254964-60-8
货号 : A337216
分子式 : C20H17F3N2O4
纯度 : 99%+
分子量 : 406.355
MDL号 : MFCD18251454
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(98.44 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

5% DMSO+30% PEG 300+water 8 mg/mL

生物活性
靶点

  • HDAC4
描述 Tasquinimod is a novel inhibitor of tumor angiogenesis that enhances the therapeutic anticancer response when combine with other standard-of-care modalities (radiation, androgen ablation, and/or taxan-based chemotherapies) in experimental animal models[3]. Tasquinimod has been documented to have a robust and consistent anti-angiogenic activity in vitro at dose between 10-50μM and in vivo at 1-10mg/kg/day resulting in a potent anti-tumor effect in rodent and human prostate cancer xenografts tested in the same dose range[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.61mL

4.92mL

2.46mL
参考文献

[1]Isaacs JT, Antony L, et al. Tasquinimod Is an Allosteric Modulator of HDAC4 survival signaling within the compromised cancer microenvironment. Cancer Res. 2013 Feb 15;73(4):1386-99.

[2]Isaacs JT, Pili R, et al. Identification of ABR-215050 as lead second generation quinoline-3-carboxamide anti-angiogenic agent for the treatment of prostate cancer. Prostate. 2006 Dec 1;66(16):1768-78.

[3]Isaacs JT. The long and winding road for the development of tasquinimod as an oral second-generation quinoline-3-carboxamide antiangiogenic drug for the treatment of prostate cancer. Expert Opin Investig Drugs. 2010;19(10):1235-1243.

[4]Olsson A, Björk A, Vallon-Christersson J, Isaacs JT, Leanderson T. Tasquinimod (ABR-215050), a quinoline-3-carboxamide anti-angiogenic agent, modulates the expression of thrombospondin-1 in human prostate tumors. Mol Cancer. 2010;9:107.