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

OP-5244 

Cat. No.: HY-136978 Purity: 99.63%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

OP-5244 Chemical Structure

OP-5244 Chemical Structure

CAS No. : 2381268-71-7

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5 mg USD 850 In-stock
10 mg USD 1400 In-stock
25 mg USD 2950 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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 & 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].

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Appearance

Solid

Formula

C19H29ClN5O9P
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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)
Solvent & Solubility
In Vitro: 

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

H2O : 100 mg/mL (185.91 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

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

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.63%

COA (258 KB) HNMR (524 KB) RP-HPLC (296 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

OP-52442381268-71-7OP5244OP 5244CD73ecto-5′-nucleotidase, NT5EimmunosuppressionadenosinecancerInhibitorinhibitorinhibit

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