OP-5244 - ≥99% , CAS No.2381268-71-7

CAS: 2381268-71-7 Cat. No.: O650904 분자식: C₁₉H₂₉ClN₅O₉P 분자량: 537.89

GRADE & PURITY ≥99%

Storage

Store at 2-8°C,Protected from light,Desiccated

Shipped In

Wet ice

개요

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)

Specifications

사양 및 순도

≥99%

생화학 및 생리적 메커니즘

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.

보관 조건

Store at 2-8°C,Protected from light,Desiccated

배송

Wet ice

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작업 유형

INHIBITOR

순수함

≥99%

이름과 식별자

• 분자량: 537.89

화학 및 물리적 특성

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