Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tasquinimod (ABR-215050) 是一种口服抗血管生成剂,有潜在的抗肿瘤活性。它也是 S100A9抑制剂,与 HDAC4Zn2+结合结构域结合的 Kd 值在10到30 nM 之间。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 340 | 现货 | ||
2 mg | ¥ 467 | 现货 | ||
5 mg | ¥ 670 | 现货 | ||
10 mg | ¥ 960 | 现货 | ||
25 mg | ¥ 1,590 | 现货 | ||
50 mg | ¥ 2,380 | 现货 | ||
100 mg | ¥ 3,620 | 现货 | ||
500 mg | ¥ 8,120 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 787 | 现货 |
产品描述 | Tasquinimod (ABR-215050) is a quinoline-3-carboxamide linomide analog with antiangiogenic and potential antineoplastic activities. Tasquinimod has been shown to decrease blood vessel density but the exact mechanism of action is not known. This agent has also been shown to augment the antineoplastic effects of docetaxel and androgen ablation in a murine model of prostate cancer involving human prostate cancer xenografts. |
靶点活性 | HDAC4:10-30 nM (Kd) |
体外活性 | Tasquinimod inhibits tumor angiogenesis by allosteric inhibition of HDAC4/N-CoR/HDAC3 dependent deacetylation of HIF-1α. [1] Tasquinimod also targets infiltrating myeloid cells, and modulates local tumour immunity by blocking the interaction between S100A9 and its ligands receptor of advanced glycation end products and Toll-like receptor 4. [3] |
体内活性 | Tasquinimod (30 mg/kg/d p.o.) shows anti-angiogenic activity and thus causes tumor growth inhibition in mice bearing human and rodent prostate cancer models. [2] |
细胞实验 | Tasquinimod is dissolved in DMSO and stored, and then diluted with appropriate media before use[3]. Two human prostate cancer cell lines, CWR-22RH and LNCaP (ATCC) are both androgen independent, but remain sensitive to androgen stimulation of growth, express PSA and a mutated androgen receptor. The hormone independent cell lines LNCaP19 and DU145 are also tested for TSP1 induction after in vitro exposure to Tasquinimod (0.1-100 μM). CWR-22RH, LNCaP and DU145 are grown in RPMI Medium 1640 containing 10% FCS and L-Glutamine mixture, while LNCAP19 is cultured in RPMI-medium with 10% hormone free (RDCC) FCS[3]. |
别名 | 他喹莫德, ABR-215050 |
分子量 | 406.36 |
分子式 | C20H17F3N2O4 |
CAS No. | 254964-60-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 9 mg/mL (22.1 mM)
DMSO: 75 mg/mL (184.6 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.4609 mL | 12.3044 mL | 24.6087 mL | 61.5218 mL |
5 mM | 0.4922 mL | 2.4609 mL | 4.9217 mL | 12.3044 mL | |
10 mM | 0.2461 mL | 1.2304 mL | 2.4609 mL | 6.1522 mL | |
20 mM | 0.123 mL | 0.6152 mL | 1.2304 mL | 3.0761 mL | |
DMSO | 50 mM | 0.0492 mL | 0.2461 mL | 0.4922 mL | 1.2304 mL |
100 mM | 0.0246 mL | 0.123 mL | 0.2461 mL | 0.6152 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Tasquinimod 254964-60-8 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC ABR 215050 他喹莫德 ABR-215050 Inhibitor inhibit Histone deacetylases ABR215050 inhibitor