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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。
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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 | 库存 | 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 x 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 | ABR-215050, 他喹莫德 |
分子量 | 406.36 |
分子式 | C20H17F3N2O4 |
CAS No. | 254964-60-8 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 9 mg/mL (22.1 mM) DMSO: 65 mg/mL (159.96 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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