OP-5244 - ≥99% , CAS No.2381268-71-7

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

등급 & 순도 ≥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)

사양

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)

자주 묻는 질문

How should this product be stored?

Store at 2–8 °C, protected from light, desiccated. Keep the container tightly closed with desiccant — the material is moisture-sensitive.

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How is this product shipped?

This product ships chilled on wet ice. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2381268-71-7, the molecular formula is C19H29ClN5O9P, and the molecular weight is 537.89 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.