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Tasquinimod

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Purity:100%

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COA LCMS HNMR

Tasquinimod

Catalog No. T6695Cas No. 254964-60-8

Tasquinimod (ABR-215050) is a quinoline-3-carboxamide linomide analog with antiangiogenic and potential antineoplastic activities. Tasquinimod has been shown to decrease blood vessel density but the exact mechanism of action is not known. This agent has also been shown to augment the antineoplastic effects of docetaxel and androgen ablation in a murine model of prostate cancer involving human prostate cancer xenografts.

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Pack Size	Price	Availability
1 mg	$45	In Stock
2 mg	$64	In Stock
5 mg	$96	In Stock
10 mg	$137	In Stock
25 mg	$230	In Stock
50 mg	$340	In Stock
100 mg	$520	In Stock
500 mg	$1,160	In Stock
1 mL x 10 mM (in DMSO)	$115	In Stock

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Product Introduction

Bioactivity

Description	Tasquinimod (ABR-215050) is a quinoline-3-carboxamide linomide analog with antiangiogenic and potential antineoplastic activities. Tasquinimod has been shown to decrease blood vessel density but the exact mechanism of action is not known. This agent has also been shown to augment the antineoplastic effects of docetaxel and androgen ablation in a murine model of prostate cancer involving human prostate cancer xenografts.
Targets&IC50	HDAC4:10-30 nM (Kd)
In vitro	Tasquinimod inhibits tumor angiogenesis by allosteric inhibition of HDAC4/N-CoR/HDAC3 dependent deacetylation of HIF-1α. [1] 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. [3]
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. [2]
Cell Research	Tasquinimod is dissolved in DMSO and stored, and then diluted with appropriate media before use[3]. Two human prostate cancer cell lines, CWR-22RH and LNCaP (ATCC) are both androgen independent, but remain sensitive to androgen stimulation of growth, express PSA and a mutated androgen receptor. The hormone independent cell lines LNCaP19 and DU145 are also tested for TSP1 induction after in vitro exposure to Tasquinimod (0.1-100 μM). CWR-22RH, LNCaP and DU145 are grown in RPMI Medium 1640 containing 10% FCS and L-Glutamine mixture, while LNCAP19 is cultured in RPMI-medium with 10% hormone free (RDCC) FCS[3].
Alias	ABR-215050

Chemical Properties

Molecular Weight	406.36
Formula	C20H17F3N2O4
Cas No.	254964-60-8

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

Ethanol: 9 mg/mL (22.1 mM)

DMSO: 65 mg/mL (159.96 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4609 mL	12.3044 mL	24.6087 mL	123.0436 mL
5 mM	0.4922 mL	2.4609 mL	4.9217 mL	24.6087 mL
10 mM	0.2461 mL	1.2304 mL	2.4609 mL	12.3044 mL
20 mM	0.1230 mL	0.6152 mL	1.2304 mL	6.1522 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0492 mL	0.2461 mL	0.4922 mL	2.4609 mL
100 mM	0.0246 mL	0.1230 mL	0.2461 mL	1.2304 mL

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