Tasquinimod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。

Tasquinimod 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.

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]

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]

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].

254964-60-8

C20H17F3N2O4

406.36

ABR-215050;他喹莫德

Ethanol:9 mg/mL (22.1 mM)
H2O:<1 mgml
DMSO:75 mg/mL (184.6 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years