[CAS NO. 2381268-71-7] OP-5244
PRODUCTS SPECIFICATIONS [2381268-71-7]
DESCRIPTION [2381268-71-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 537.89 |
| Molecular Formula | C19H29ClN5O9P |
| 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)=O)(COC)CO |
Summary
IC50 & Target
IC50: 0.25 nM (CD73) [1]
In Vitro
OP-5244 inhibits the production of adenosine (ADO), with an EC
50
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 EC
50
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 C
max
(rat 0.82, dog 1.25, cyno 1.72 μM) and AUC (rat 1.96, dog 1.75, cyno 14.2 µM•h)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
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 : 250 mg/mL ( 464.78 mM ; Need ultrasonic)
H 2 O : 100 mg/mL ( 185.91 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8591 mL | 9.2956 mL | 18.5912 mL |
| 5 mM | 0.3718 mL | 1.8591 mL | 3.7182 mL |
| 10 mM | 0.1859 mL | 0.9296 mL | 1.8591 mL |
