product name Tasquinimod
Description: Tasquinimod, also known as ABR215050, is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling.Tasquinimod is a quinoline-3-carboxamide linomide analogue with also 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. It is currently in Phase 3 study.
References: Cancer Res. 2013 Feb 15;73(4):1386-99; Prostate. 2006 Dec 1;66(16):1768-78; Cancer Chemother Pharmacol. 2014 Jan;73(1):1-8.
406.36
Formula
C20H17F3N2O
CAS No.
254964-60-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 81 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: 11 mg/mL warmed (27.1 mM)
Solubility (In vivo)
5% DMSO+30% PEG 300+ddH2O: 8 mg/mL
Synonyms
ABR215050
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19424772/
| In Vitro |
In vitro activity: Tasquinimod inhibits tumor angiogenesis by allosteric inhibition of HDAC4/N-CoR/HDAC3 dependent deacetylation of HIF-1α. 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. Kinase Assay: Cell Assay: Generated microarray data based on four separate biological replicates showed a drug-induced effect of 50μM tasquinimod on gene expression in LNCaP cells when cultured in vitro for 24 h. The expression data achieved by RT-PCR were consistent with the microarray analysis data with a significant up-regulation of THBS1, GDF15 and CYP1A1 whereas CXCR4 and AGER1 did not change expression significantly. |
|---|---|
| In Vivo | 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. |
| Animal model | Mice bearing PC-82 , CWR-22Rv1, LAPC-4, or LNCaP prostate cancer xenografts. |
| Formulation & Dosage | Dissovled in water; 30 mg/kg/d; oral administration. |
| References | Cancer Res. 2013 Feb 15;73(4):1386-99; Prostate. 2006 Dec 1;66(16):1768-78; Cancer Chemother Pharmacol. 2014 Jan;73(1):1-8. |
