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| 2mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
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. For the treatment of castration-resistant prostate cancer, Tasquinimod is presently being investigated in Phase 3 clinical trials.
| Targets |
HDAC4 ( Kd = 10-30 nM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
Tasquinimod has a Kd of 10–30 nM for binding to the regulatory Zn2+ binding domain of HDAC4.
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| Cell Assay |
CWR-22RH and LNCaP (ATCC) are two human prostate cancer cell lines that express PSA and have a mutated androgen receptor. Despite being androgen independent, they both show sensitivity to androgen stimulation of growth. The in vitro exposure of hormone-independent cell lines LNCaP19 and DU145 to Tasquinimod (0.1-100 μM) is followed by an assessment of TSP1 induction. While LNCAP19 is cultivated in RPMI-medium with 10% hormone free (RDCC) FCS, CWR-22RH, LNCaP, and DU145 are grown in RPMI Medium 1640 containing 10% FCS and L-Glutamine mixture.
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| Animal Protocol |
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| References |
| Molecular Formula |
C20H17F3N2O
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| Molecular Weight |
406.36
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| Exact Mass |
406.11
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| Elemental Analysis |
C, 59.11; H, 4.22; F, 14.03; N, 6.89; O, 15.75.
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| CAS # |
254964-60-8
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CN1C2=C(C(=CC=C2)OC)C(=C(C1=O)C(=O)N(C)C3=CC=C(C=C3)C(F)(F)F)O
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| InChi Key |
ONDYALNGTUAJDX-UHFFFAOYSA-N
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| 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
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| Chemical Name |
4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[4-(trifluoromethyl)phenyl]quinoline-3-carboxamide
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| Synonyms |
ABR-215050; ABR215050; ABR 215050
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: 5% DMSO+30% PEG 300+ddH2O: 8mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4609 mL | 12.3044 mL | 24.6087 mL | |
| 5 mM | 0.4922 mL | 2.4609 mL | 4.9217 mL | |
| 10 mM | 0.2461 mL | 1.2304 mL | 2.4609 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04405167 | Recruiting | Drug: Tasquinimod Drug: IRd chemotherapy |
Multiple Myeloma | University of Pennsylvania | July 10, 2020 | Phase 1 |
| NCT01234311 | Completed | Drug: tasquinimod Drug: Placebo |
Prostate Cancer | Active Biotech AB | March 2011 | Phase 3 |
| NCT01048203 | Completed | Drug: ABR-215050 | Healthy | Active Biotech AB | January 2009 | Phase 1 |
| NCT01513733 | Completed | Drug: tasquinimod | Prostate Cancer | Andrew J. Armstrong, MD | January 2012 | Phase 1 |
| NCT02159950 | Completed | Drug: Tasquinimod Biological: Sipuleucel-T |
Metastatic Prostate Carcinoma Stage IV Prostate Cancer |
Roswell Park Cancer Institute | January 2015 | Phase 2 |
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