2381268-71-7
2381268-71-7 structure
- Name: OP-5244
- Chemical Name: OP-5244
- CAS Number: 2381268-71-7
- Molecular Formula: C19H29ClN5O9P
- Molecular Weight: 537.89
- Catalog: Research Areas Inflammation/Immunology
- Create Date: 2021-01-12 18:18:18
- Modify Date: 2024-07-22 16:32:00
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OP-5244 is a potent and orally bioavailable inhibitor of CD73, with an IC50 of 0.25 nM. OP-5244 reverses immunosuppression through blocking of adenosine production, and has the potential for the cancer research[1].
| Name | OP-5244 |
|---|
| Description | OP-5244 is a potent and orally bioavailable inhibitor of CD73, with an IC50 of 0.25 nM. OP-5244 reverses immunosuppression through blocking of adenosine production, and has the potential for the cancer research[1]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 0.25 nM (CD73)[1] |
| In Vitro | 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]. |
| In Vivo | OP-5244 (15 mg/kg/day; s.c. for 13 d) exhibits anti-tumor effects as a single agent as shown by the tumor growth inhibition in mice[1]. 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]. Animal Model: BALB/c mice with breast cancer[1] Dosage: 15 mg/kg/day Administration: S.c. for 13 days Result: Inhibited tumor growth. Showed a 95% lower ADO/AMP ratio compared to that of the vehicle group. |
| References |
| Molecular Formula | C19H29ClN5O9P |
|---|---|
| Molecular Weight | 537.89 |