MEDS700
MEDS700 is a blood-brain barrier permeable inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 1.5 nM. MEDS700 induces apoptosis and differentiation, and inhibits proliferation of cancer cells. MEDS700 can be used in research on acute myeloid leukemia and other conditions.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2770979-81-0
- 分子式: C23H15F6N3O3
- 分子量:495.37
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
MEDS700 (0.001-10 μM; 3 days) induces differentiation and apoptosis in THP1 and U937 acute myeloid leukemia (AML) cell lines, with an EC50 value ranging from 19 nM to 64 nM[1].
MEDS700 (0.1-1 μM; 3 days) induces apoptosis in MV4-11 acute myeloid leukemia (AML) cells at concentrations of 0.1 μM and 1 μM[1].
MEDS700 exhibits potent antiproliferative activity against a panel of solid tumor cell lines at nanomolar concentrations, with the strongest activity observed in neuroblastoma, Ewing sarcoma, bladder cancer and fibrosarcoma cells[1].
MEDS700 potently inhibits the proliferation of SF7761 and SU-DIPG-XIII DMG cell lines, with EC50 values of 9.3 nM and 32.9 nM, respectively, and exhibits activity in SF8628 cells with extended exposure time[1].
MEDS700 (72 h) exerts antiproliferative and cytotoxic effects on SH-SY5Y neuroblastoma cells via pyrimidine depletion, induces S-phase cell cycle arrest, caspase-dependent apoptosis, and irreversible loss of colony-forming ability, with an EC50 of 13 nM[1].
MEDS700 (1-100 μM; 72 h) exhibits only extremely low toxicity in mixed neural cell cultures derived from human induced pluripotent stem cells (hiPSCs), with an EC30 of 199 μM, indicating that this compound has a favorable safety window relative to its anti-tumor activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 AML cells
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Concentration:0.1 μM, 1 μM
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Incubation Time:3 days
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Result:Induced ~40% apoptosis at both 0.1 μM and 1 μM.
Co-treatment with 5 μM uridine reduced apoptosis.
Co-treatment with dipyridamole (1.0 μM) increased apoptosis to ~100% at both concentrations, even in the presence of 5 μM or 100 μM uridine.
Parmacokinetics
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (male, 8 weeks old)[1]
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Dosage:5 mg/kg (i.v.); 20 mg/kg (p.o.)
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Administration:i.v.; single dose; p.o.; single dose
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Result:Exhibited oral bioavailability of 37.8%.
Showed a half-life of over 12 hours after oral administration and 8.1 hours after intravenous administration.
Reached an intracerebral Cmax of 0.67 μg/mL.
Maintained a therapeutically relevant brain concentration of approximately 160 nM for up to 24 hours after oral administration.
化学情報
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CAS 番号 2770979-81-0
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分子量 495.37
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分子式 C23H15F6N3O3
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SMILES
FC1=C(F)C(NC(C2=C3C=CC=CN3N=C2O)=O)=C(F)C(F)=C1C4=CC(OCC(F)(F)C)=CC=C4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)