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Tasquinimod

Cat. No. M9633
Tasquinimod Structure
Synonym:

ABR-215050

Size Price Availability
5mg USD 150  USD150 4-7 Days
10mg USD 220  USD220 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 406.36
Formula C20H17F3N2O4
CAS Number 254964-60-8
Purity >99%
Solubility DMSO ≥ 40 mg/mL
Storage at -20°C
References

[1] Martin Pelletier, et al. Blood Adv. Quinoline-3-carboxamides such as tasquinimod are not specific inhibitors of S100A9

[2] John T Isaacs, et al. Oncotarget. Anti-cancer potency of tasquinimod is enhanced via albumin-binding facilitating increased uptake in the tumor microenvironment

[3] John T Isaacs, et al. Cancer Res. Tasquinimod Is an Allosteric Modulator of HDAC4 survival signaling within the compromised cancer microenvironment

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Tasquinimod, ABR-215050 supplier, HDAC, inhibitors

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