OP-5244 是一种有效和具有口服活性的 CD73 抑制剂，IC₅₀ 值为 0.25 nM。OP-5244 通过阻断腺苷的产生来逆转免疫抑制作用，具有进行癌症研究的潜力。

OP-5244 is a potent and orally active inhibitor of CD73, with an IC 50 of 0.25 nM. OP-5244 reverses immunosuppression through blocking of adenosine production, and has the potential for the cancer research.

Solid

IC50: 0.25 nM (CD73)

OP-5244 inhibits the production of adenosine (ADO), with an EC50 of 0.79±0.38 nM in H1568 (NSCLC) cells.
OP-5244 inhibits AMP hydrolysis to ADO in peripheral blood derived CD8 T cells with an EC50 of 0.22 nM.
OP-5244 (4.1-1000 nM; 96 h) rescues AMP-suppressed CD8 T cells proliferation and cytokine production.
OP-5244 (0.01 nM-10 μM) inhibits ADO production completely in human and murine cancer cell lines (H1568 and EMT6, respectively). has not independently confirmed the accuracy of these methods. They are for reference only.

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.
OP-5244 (150 mg/kg; p.o. twice daily for 16 d) increases CD8 T cells infiltration and reverses immunosuppression in mice.
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).
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) . has not independently confirmed the accuracy of these methods. They are for reference only.

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)

[1]. Du X, et, al. Orally Bioavailable Small Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression Through Blockade of Adenosine Production. J Med Chem. 2020 Aug 31.

In Vitro: DMSO : 250 mg/mL (464.78 mM; Need ultrasonic)H₂O : 100 mg/mL (185.91 mM; Need ultrasonic)配制储备液