Tasquinimod is an oral antiangiogenic and S100A9 inhibitor. Tasquinimod allosteric binding at 10-30 nM Kd in the zinc-regulated domain of HDAC4 inhibits co-localization of N-Cor /HDAC3, thereby inhibiting deacetylation of histones and HDAC4-client transcription factors such as HIF-1α. TAMs secretes angiogenic factors such as VEGF, FGF, TNF- α and TGF-β when bone marrow is derived to inhibit cell differentiation. Tasquinimod inhibits tumor angiogenesis by inhibiting tumor invasion of S100A9/ TLR4-dependent MDSCs and/or by inhibiting HIF-1α deacetylation of HDAC4/ N-COR/HDAC3-dependent MDSCs to TAMs. Tasquinimod is an orally active quinoline-3-carboxylamide that binds with high affinity to HDAC4 and S100A9 in cancer and infiltrates host cells in the impaired tumor microenvironment, inhibiting an adaptive survival pathway required for angiogenic responses.
| Molecular Weight | 406.36 |
| Formula | C20H17F3N2O4 |
| CAS Number | 254964-60-8 |
| Solubility (25°C) | DMSO ≥ 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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