| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Adenosine receptor
Taminadenant targets the adenosine A2A receptor (A2AR). It has a Ki of 12.0 nM for human A1 receptors and 25.0 nM for human A2A receptors in radioligand binding assays. It antagonizes A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. |
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| ln Vitro |
Taminadenant (PBF509) completely blocks agonist-mediated cAMP accumulation, with an IC50 of 72.8 ± 17.4 nM i HEK cells that express human A2ARSNAP permanently[1]. However, it does not demonstrate any agonist efficacy in these cells.
In vitro, taminadenant is a potent A2AR antagonist. It antagonizes A2AR agonist-mediated cAMP accumulation and impedance responses. It has a Ki of 12.0 nM for human A1 receptors and 25.0 nM for human A2A receptors. |
| ln Vivo |
Taminadenant (PBF509) (0.3, 3, 7.5, 10, or 30 mg/kg; p.o.; single dosage) increases the effects of L-DOPA, exhibits a strong antiparkinsonian activity, and reduces the cataleptic effects of haloperidol[1]. It also lessens the tremulous jaw movement caused by pilocarpine.
In vivo, taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. It reactivates the antitumor immune response. It is being evaluated as an immunotherapy agent. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for taminadenant typically involve evaluating its binding affinity to the adenosine A2A receptor using radioligand binding assays. Ki values are determined by measuring competition with labeled ligands.
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| Cell Assay |
For in vitro cell-based assays, taminadenant is dissolved in DMSO and applied to cultured immune cells at concentrations ranging from 1 nM to 10 µM. Effects on cAMP accumulation, immune cell activation, or cytokine production are assessed after 1-24 hours of treatment.
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| Animal Protocol |
Sprague-Dawley rats (240-250 g; induced catalepsy by s.c. with 1 mg/kg Haloperidol (HY-14538))
3, 10, or 30 mg/kg p.o.; single dosage In vivo animal studies commonly use rat models of movement disorders or mouse tumor models. Taminadenant is administered orally at doses ranging from 1-100 mg/kg. Efficacy is evaluated by measuring motor function, tumor growth, or immune cell infiltration. |
| ADME/Pharmacokinetics |
Taminadenant is orally active. It has a molecular formula of C10H8BrN7 and a molecular weight of 306.12 g/mol. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Taminadenant has a favorable safety profile with no significant toxicity reported at therapeutic doses. Its selectivity for adenosine receptors minimizes off-target effects.
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| References | |
| Additional Infomation |
Taminadenant is an orally bioavailable adenosine A2A receptor (A2AR) antagonist with potential antitumor activity. After administration, the A2AR antagonist PBF-509 selectively binds to and inhibits A2AR expression on the surface of T lymphocytes. This eliminates adenosine/A2AR-mediated T lymphocyte suppression and activates T cell-mediated immune responses against tumor cells, thereby reducing the proliferation of susceptible tumor cells. A2AR is a G protein-coupled receptor highly expressed on the surface of T cells and, upon activation by adenosine, inhibits T cell proliferation and activation. Cancer cells typically overproduce adenosine.
Taminadenant is an immunotherapy agent that targets the adenosine A2A receptor. It is being evaluated for the treatment of cancer and movement disorders. It reactivates the antitumor immune response by blocking A2AR-mediated immunosuppression. |
| Molecular Formula |
C10H8BRN7
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|---|---|
| Molecular Weight |
306.127
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| Exact Mass |
305.002
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| Elemental Analysis |
C, 39.24; H, 2.63; Br, 26.10; N, 32.03
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| CAS # |
1337962-47-6
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| Related CAS # |
2253894-78-7 (HCl hydrate); 1337962-47-6; 2253894-81-2 (mesylate); 2253894-80-1 (sulfate); 2253894-79-8 (HCl dihydrate)
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| PubChem CID |
53466958
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| Appearance |
Solid powder
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| Density |
1.9±0.1 g/cm3
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| Boiling Point |
574.9±60.0 °C at 760 mmHg
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| Flash Point |
301.5±32.9 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.851
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| LogP |
-0.47
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
18
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| Complexity |
291
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| Defined Atom Stereocenter Count |
0
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| SMILES |
BrC1=C(N)N=C(N=C1N1C=CC=N1)N1C=CC=N1
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| InChi Key |
ATFXVNUWQOXRRU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H8BrN7/c11-7-8(12)15-10(18-6-2-4-14-18)16-9(7)17-5-1-3-13-17/h1-6H,(H2,12,15,16)
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| Chemical Name |
5-bromo-2,6-di(pyrazol-1-yl)pyrimidin-4-amine
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| Synonyms |
PBF 509; NIR178; PBF509; NIR 178; Taminadenant; PBF-509; NIR-178
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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 |
| 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) |
DMSO: ~125 mg/mL (~408.3 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.79 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 20.8 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: ≥ 2.08 mg/mL (6.79 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 20.8 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: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2666 mL | 16.3329 mL | 32.6659 mL | |
| 5 mM | 0.6533 mL | 3.2666 mL | 6.5332 mL | |
| 10 mM | 0.3267 mL | 1.6333 mL | 3.2666 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 |
| NCT04895748 | Active Recruiting |
Drug: DFF332 Drug: RAD001 Drug: PDR001 |
Carcinoma, Renal Cell | Novartis Pharmaceuticals | November 30, 2021 | Phase 1 |
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