Tasquinimod is an oral antiangiogenic agent, it is also a S100A9 inhibitor. Tasquinimod binds allosterically within the regulatory Zinc domain of HDAC4 with a Kd of 10-30 nM, which results in inhibition of co-localization of N-CoR/HDAC3, thereby inhibiting deacetylation of histones and HDAC4 client transcription factors, such as HIF-1α. TAMs secrete angiogenic factors like VEGF, FGF, TNF- α, and TGF-β when myeloid-derived suppressor cells differentiate. Tasquinimod can suppress tumor angiogenesis due to inhibition of S100A9/TLR4 dependent MDSCs tumor infiltration and/or to inhibition of HDAC4/N-CoR/HDAC3 dependent deacetylation of HIF-1α by MDSCs suppressing their differentiation into TAMs. Tasquinimod, an orally active quinoline-3-carboxamide, binds with high affinity to HDAC4 and S100A9 in cancer and infiltrating host cells within compromised tumor microenvironment inhibiting adaptive survival pathways needed for an angiogenic response.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥ 40 mg/mL|
Quinoline-3-carboxamides such as tasquinimod are not specific inhibitors of S100A9
Martin Pelletier, et al. Blood Adv. 2018 May 22;2(10):1170-1171. PMID: 29789315.
Anti-cancer potency of tasquinimod is enhanced via albumin-binding facilitating increased uptake in the tumor microenvironment
John T Isaacs, et al. Oncotarget. 2014 Sep 30;5(18):8093-106. PMID: 25193858.
Tasquinimod Is an Allosteric Modulator of HDAC4 survival signaling within the compromised cancer microenvironment
John T Isaacs, et al. Cancer Res. 2013 Feb 15;73(4):1386-99. PMID: 23149916.
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