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。
生物活性 | OP-5244 is a potent and orally active inhibitor ofCD73, with anIC50of 0.25 nM. OP-5244 reverses immunosuppression through blocking of adenosine production, and has the potential for thecancerresearch[1]. |
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体外研究 (In Vitro) | 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].
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体内研究 (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 Cmax(rat 0.82, dog 1.25, cyno 1.72 μM) and AUC (rat 1.96, dog 1.75, cyno 14.2 μMoh)[1].
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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 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) |
溶解性数据 | 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 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 |
*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。 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 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。 *以上所有助溶剂都可在本网站选购。
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