LCI40
LCI40 is an orally active dual PI3K/BRD4 inhibitor (PI3Kα IC50 = 0.071 μM, PI3Kβ IC50 = 0.17 μM, PI3Kγ IC50 = 0.66 μM, PI3Kδ IC50 = 0.072 μM, BRD4 BD1 IC50 = 0.19 μM, and BRD4 BD2 IC50 = 1.88 μM. LCI40 inhibits phosphorylation of pAKT (S473) and suppresses c-MYC levels in mantle cell lymphoma cells. LCI40 displays immunomodulatory capacity with minimal toxicity to normal mouse immune cells. LCI40 can be used for the research of mantle cell lymphoma.
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。
- 分子式: C23H20N2O4
- 分子量:388.42
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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BRD4 (BD2) 1.88 μM (IC50) |
BRD4 (BD1) 0.19 μM (IC50) |
PI3Kγ 0.66 μM (IC50) |
PI3Kα 0.071 μM (IC50) |
PI3Kβ 0.17 μM (IC50) |
LCI40 (1.0 μM) is highly selective for PI3K family enzymes and PIK3CA mutants[1].
LCI40 (1.0 μM) is highly selective for BET family bromodomains, particularly the BD1 domains of BRD4, BRD3, BRD2, and BRDT[1].
LCI40 (48 h) potently reduces cell viability in human Mino (IC50 = 357 nM) and JeKo-1 (IC50 = 519 nM) mantle cell lymphoma cell lines[1].
LCI40 (0.1-1 μM; 2 h) dose-dependently inhibits PI3K/AKT signaling (pAKTS473) and reduces c-MYC protein expression in IgM-stimulated human Mino mantle cell lymphoma cells[1].
LCI40 (0.5 μM; 48 h) interferes with IL-4-mediated alternative macrophage activation in mouse BMDMs by suppressing M2 marker expression and metabolic reprogramming[1].
LCI40 (0.1-5 μM; 1 h pretreatment) dose-dependently restrains CD3/CD28-mediated mouse pan-T cell activation and proliferation, reduces activation marker and effector gene expression, and has micromolar cytotoxicity to resting T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:IgM-stimulated human Mino mantle cell lymphoma cells
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Concentration:0.1; 0.5; 1 μM
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Incubation Time:2 h
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Result:Dose-dependently inhibited phosphorylation of AKT at S473.
Reduced c-MYC protein levels.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-last | AUC0-∞ | Vz/F | CL/F |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 20 mg/kg | p.o. | 2.5 h | 0.3 h | 336.5 ng/mL | 153.7 ng·h/mL | 159.2 ng·h/mL | 472.6 L/kg | 128.1 L/h/kg |
化学情報
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分子量 388.42
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分子式 C23H20N2O4
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SMILES
O=C1C=C(N2CCOCC2)OC3=C1C=CC=C3C4=CC(C(OC)=CC=N5)=C5C=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)
LCI40 関連分類
HY-183770 関連分類
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