OP-5244 sodium
Based on 1 Customer Validation
OP-5244 sodium is a potent and orally active inhibitor of CD73, with an IC50 of 0.25 nM. OP-5244 sodium reverses immunosuppression through blocking of adenosine production, and has the potential for the cancer research.
For research use only. We do not sell to patients.
- Purity: 99.87%
- Formula: C19H28ClN5NaO9P
- Molecular Weight:559.87
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Biological Activity
IC50: 0.25 nM (CD73)[1]
OP-5244 inhibits the production of adenosine (ADO), with an EC50 of 0.79±0.38 nM in H1568 (NSCLC) cells[1].
OP-5244 inhibits AMP hydrolysis to ADO in peripheral blood derived CD8+ T cells with an EC50 of 0.22 nM[1].
OP-5244 (4.1-1000 nM; 96 h) rescues AMP-suppressed CD8+ T cells proliferation and cytokine production[1].
OP-5244 (0.01 nM-10 μM) inhibits ADO production completely in human and murine cancer cell lines (H1568 and EMT6, respectively)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
OP-5244 (150 mg/kg; p.o. twice daily for 16 d) increases CD8+ T cells infiltration and reverses immunosuppression in mice[1].
OP-5244 (0.2 mg/kg; i.v.) exhibits terminal elimination half-lives (rat 8.5, dog 0.82, cyno 4.6 h) due to moderate plasma clearance (rat 0.18, dog 1.22, cyno 0.05 L/kg/h) and low steady-state volume of distribution (rat 0.22, dog 0.29, cyno 0.10 L/kg/h)[1].
OP-5244 (10 mg/kg; p.o.) exhibits Cmax (rat 0.82, dog 1.25, cyno 1.72 μM) and AUC (rat 1.96, dog 1.75, cyno 14.2 µM•h) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice with breast cancer[1]
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Dosage:15 mg/kg/day
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Administration:S.c. for 13 days
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Result:Inhibited tumor growth.
Showed a 95% lower ADO/AMP ratio compared to that of the vehicle group.
Chemical Information
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Appearance Solid
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Molecular Weight 559.87
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Formula C19H28ClN5NaO9P
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Color White to off-white
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SMILES
O[C@H]1[C@@H](O)[C@H](N2N=CC3=C(NC4CCCC4)N=C(Cl)N=C32)O[C@@H]1CO[C@]([P](O)(O[Na])=O)(COC)CO
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 33.33 mg/mL (59.53 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7861 mL | 8.9306 mL | 17.8613 mL | 44.6532 mL |
| 5 mM | 0.3572 mL | 1.7861 mL | 3.5723 mL | 8.9306 mL | |
| 10 mM | 0.1786 mL | 0.8931 mL | 1.7861 mL | 4.4653 mL | |
| 15 mM | 0.1191 mL | 0.5954 mL | 1.1908 mL | 2.9769 mL | |
| 20 mM | 0.0893 mL | 0.4465 mL | 0.8931 mL | 2.2327 mL | |
| 25 mM | 0.0714 mL | 0.3572 mL | 0.7145 mL | 1.7861 mL | |
| 30 mM | 0.0595 mL | 0.2977 mL | 0.5954 mL | 1.4884 mL | |
| 40 mM | 0.0447 mL | 0.2233 mL | 0.4465 mL | 1.1163 mL | |
| 50 mM | 0.0357 mL | 0.1786 mL | 0.3572 mL | 0.8931 mL |