OP-5244 is a potent and orally active 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].

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].

上海金畔生物科技有限公司 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^[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

537.89

C₁₉H₂₉ClN₅O₉P

2381268-71-7

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)

In Vitro: 

DMSO : 250 mg/mL (464.78 mM; Need ultrasonic)

*

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 6.5 mg/mL (12.08 mM); Clear solution

  此方案可获得 ≥ 6.5 mg/mL (12.08 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 65.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 6.5 mg/mL (12.08 mM); Clear solution

  此方案可获得 ≥ 6.5 mg/mL (12.08 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 65.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 6.5 mg/mL (12.08 mM); Clear solution

  此方案可获得 ≥ 6.5 mg/mL (12.08 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 65.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.