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.
For research use only. We do not sell to patients.
- Formula: C23H20N2O4
- Molecular Weight:388.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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 |
Chemical Information
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Molecular Weight 388.42
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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