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Size | Price | Stock |
---|---|---|
250mg | $1400 | Check With Us |
500mg | $2020 | Check With Us |
1g | $3030 | Check With Us |
Cat #: V0268 CAS #: 254964-60-8 Purity ≥ 98%
Description: Tasquinimod (also known as ABR215050), a quinoline-3-carboxamide linomide analogue and an investigational drug, is a novel, and orally bioactive anti-angiogenic agent which potently inhibits HDAC4 allosterically with with potential anticancer activity.
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Molecular Weight (MW) | 406.36 |
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Molecular Formula | C20H17F3N2O |
CAS No. | 254964-60-8 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 81 mg/mL (199.3 mM)r |
Water: <1 mg/mLr | |
Ethanol: 11 mg/mL warmed (27.1 mM) | |
Solubility In Vivo | 5% DMSO+30% PEG 300+ddH2O: 8 mg/mL |
Synonyms | ABR-215050; ABR215050; ABR 215050; 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-((4-trifluoromethyl)phenyl)-1,2-dihydroquinoline-3-carboxamide InChi Key: ONDYALNGTUAJDX-UHFFFAOYSA-N InChi Code: InChI=1S/C20H17F3N2O4/c1-24(12-9-7-11(8-10-12)20(21,22)23)18(27)16-17(26)15-13(25(2)19(16)28)5-4-6-14(15)29-3/h4-10,26H,1-3H3 SMILES Code: O=C(C1=C(O)C2=C(N(C)C1=O)C=CC=C2OC)N(C)C3=CC=C(C(F)(F)F)C=C3 |
Protocol | In Vitro | Tasquinimod suppresses hypoxia induced decrease in histone acetylation without lowering HDAC expression or directly inhibiting HDAC activity. 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 |
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Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.4609 mL | 12.3044 mL | 24.6087 mL | 49.2174 mL |
5mM | 0.4922 mL | 2.4609 mL | 4.9217 mL | 9.8435 mL |
10mM | 0.2461 mL | 1.2304 mL | 2.4609 mL | 4.9217 mL |
20mM | 0.1230 mL | 0.6152 mL | 1.2304 mL | 2.4609 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.