OP-5244 sodium is a potent and orally active inhibitor ofCD73, with anIC₅₀of 0.25 nM. OP-5244 sodium reverses immunosuppression through blocking of adenosine production, and has the potential for thecancerresearch^[1].

IC50: 0.25 nM (CD73)^[1]

OP-5244 inhibits the production of adenosine (ADO), with an EC₅₀of 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 EC₅₀of 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].

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 μMoh)^[1].

559.87

Solid

C₁₉H₂₈ClN₅NaO₉P

Room temperature in continental US; may vary elsewhere.

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)

DMSO : 33.33 mg/mL(59.53 mM;ultrasonic and warming and heat to 60℃)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。