| CAS NO: | 254964-60-8 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 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 | ABR-215050; ABR215050; ABR 215050; 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-((4-trifluoromethyl)phenyl)-1,2-dihydroquinoline-3-carboxamide InChi Key: ONDYALNGTUAJDX-UHFFFAOYSA-N InChi Code: InChI=1S/C20H17F3N2O4/c1-24(12-9-7-11(8-10-12)20(21,22)23)18(27)16-17(26)15-13(25(2)19(16)28)5-4-6-14(15)29-3/h4-10,26H,1-3H3 SMILES Code: O=C(C1=C(O)C2=C(N(C)C1=O)C=CC=C2OC)N(C)C3=CC=C(C(F)(F)F)C=C3 |
| 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: Tasquinimod binds to the regulatory Zn2+ binding domain of HDAC4 with Kd of 10-30 nM. 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. |
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