OP-5244

COA

级别和纯度:

≥99%

CAS编号: 2381268-71-7
分子式: C₁₉H₂₉ClN₅O₉P
分子量: 537.89

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货号 (SKU)	包装规格	是否现货
O650904-5mg	5mg	期货
O650904-10mg	10mg	期货
O650904-25mg	25mg	期货

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CD73 (25) Immunology/Inflammation (1938)

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基本描述

规格或纯度	≥99%
英文名称	OP-5244
生化机理	OP-5244 是一种强效的 CD73 口服活性抑制剂，IC50 为 0.25 nM。OP-5244 可通过阻断腺苷的产生来逆转免疫抑制，有望用于癌症研究。
储存温度	2-8°C储存,避光,干燥
运输条件	冰袋运输
作用类型	抑制剂
产品介绍	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 In Vitro OP-5244 inhibits the production of adenosine (ADO), with an EC 50 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 EC 50 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c mice with breast cancer 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. Form:Solid IC50& Target:IC50: 0.25 nM (CD73)
纯度	≥99%

化学和物理性质

溶解性	DMSO : 250 mg/mL (464.78 mM; Need ultrasonic) H2O : 100 mg/mL (185.91 mM; Need ultrasonic)

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化学和物理性质

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