OP-5244 sodium is a potent and orally bioavailable inhibitor of CD73, with an IC50 of 0.25 nM. OP-5244 sodium reverses immunosuppression through blocking of adenosine production, and has the potential for the cancer research.

Product information

Molecular Weight: 559.87

Formula: C19H28ClN5NaO9P

Chemical Name: sodium hydrogen ((R)-2-(((2R, 3S, 4R, 5R)-5-(2-chloro-6-(cyclopentylamino)-9H-purin-9-yl)-3, 4-dihydroxytetrahydrofuran-2-yl)methoxy)-1-hydroxy-3-methoxypropan-2-yl)phosphonate

Smiles: COC[C@](CO)(OC[C@H]1O[C@H]([C@H](O)[C@@H]1O)N1C=NC2=C1N=C(Cl)N=C2NC1CCCC1)P(O)(=O)O[Na]

InChiKey: NTPVIBWTUJFXAW-XLBLCPJHSA-M

InChi: InChI=1S/C19H29ClN5O9P.Na/c1-32-8-19(7-26,35(29,30)31)33-6-11-13(27)14(28)17(34-11)25-9-21-12-15(22-10-4-2-3-5-10)23-18(20)24-16(12)25;/h9-11,13-14,17,26-28H,2-8H2,1H3,(H,22,23,24)(H2,29,30,31);/q;+1/p-1/t11-,13-,14-,17-,19-;/m1./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

OP-5244 inhibits the production of adenosine (ADO), with an EC50 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 EC50 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).

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 Cmax (rat 0.82, dog 1.25, cyno 1.72 μM) and AUC (rat 1.96, dog 1.75, cyno 14.2 µM•h) .

Products are for research use only. Not for human use.