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.
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- 화학식: C23H20N2O4
- 분자량:388.42
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보관:
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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Biological Activity
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Chemical Information
- 순도&문서
- 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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분자량 388.42
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LCI40 Related Classifications
HY-183770 Related Classifications
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