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Tasquinimod

Cat. No. M9633

All AbMole products are for research use only, cannot be used for human consumption.

Tasquinimod Structure
Synonym:

ABR-215050

Size Price Availability Quantity
1mg USD 60  USD60 In stock
5mg USD 120  USD120 In stock
10mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
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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Keywords: Tasquinimod, ABR-215050 supplier, HDAC, inhibitors, activators

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