1. Immunology/Inflammation
  2. CD73
  3. OP-5244

OP-5244 

目录号: HY-136978
产品使用指南

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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OP-5244 Chemical Structure

OP-5244 Chemical Structure

CAS No. : 2381268-71-7

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Description

OP-5244 is a potent and orally bioavailable 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 & Target

IC50: 0.25 nM (CD73)[1]

In Vitro

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].

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 µM•h) [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.
Molecular Weight

537.89

Formula

C₁₉H₂₉ClN₅O₉P

CAS No.

2381268-71-7

SMILES

O[C@@H]1[C@@H](CO[C@]([P](O)(O)=O)(COC)CO)O[C@@H](N2N=CC3=C(NC4CCCC4)N=C(Cl)N=C32)[C@@H]1O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

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Keywords:

OP-5244OP5244OP 5244CD73ecto-5′-nucleotidase, NT5EimmunosuppressionadenosinecancerInhibitorinhibitorinhibit

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