OP-5244
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。
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包装价格促销价数量
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5mg￥9175.007340.00- +
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10mg￥14962.0011970.00- +
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25mg￥31525.0025220.00- +
- 货号: ajcx34232
- CAS: 2381268-71-7
- 别名:
- 分子式: C19H29ClN5O9P
- 分子量: 537.89
- 纯度: ＞98%
- 溶解度: DMSO : 250 mg/mL (464.78 mM; Need ultrasonic)
- 储存: 4°C, away from moisture and light
- 库存: 现货
Background
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].
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].
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].
[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.
