LASSBio-2337
LASSBio-2337 is a dual pan-PI3K/mTOR inhibitor with an mTOR IC50 of 5.8 μM.LASSBio-2337 functionally modulates mTOR and all PI3K isoforms.LASSBio-2337 acts as a cytotoxic agent in leukemia cells, including multidrug-resistant populations.LASSBio-2337 spares nontumor human peripheral blood mononuclear cells.LASSBio-2337 displays moderate PAMPA-GIT permeability.LASSBio-2337 shows low metabolic stability in rat liver microsomes.LASSBio-2337 is aqueous insoluble.LASSBio-2337 can be used for the research of acute lymphoblastic leukemia, chronic myelogenous leukemia, breast cancer.
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- Fòrmula: C18H24N6O2
- Peso molecular:356.42
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Almacenamiento:
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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Actividad biológica
Descripciòn
In Vitro
LASSBio-2337 (4 h; 24 h) is insoluble in aqueous buffer at pH 7.4, with solubility below 1 μM after 4 h and 24 h of incubation[1].
LASSBio-2337 (0.003-100 μM; 72 h) is cytotoxic to CCRF-CEM acute lymphoblastic leukemia cells, with a CC50 of 4.37 μM after 72 h of incubation[1].
LASSBio-2337 (8 h) has moderate gastrointestinal tract permeability, with a 48.40% predicted absorbed fraction and a permeability coefficient of 1.74 × 10-6 cm/s in the PAMPA-GIT assay[1].
LASSBio-2337 (10 μM; 0, 15, 30, 45, 60 min) has low metabolic stability in rat liver microsomes, with a half-life of 34.3 min in the presence of an NADPH-regenerating system, indicating clearance via oxidative metabolism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CCRF-CEM acute lymphoblastic leukemia cells (PTEN-mutated), MOLT-4 acute lymphoblastic leukemia cells (PTEN and PIK3R1-mutated), MCF7 breast carcinoma cells (PIK3CA-mutated)
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Concentration:0.003-100 μM
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Incubation Time:72 h
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Result:Demonstrated a CC50 of 4.37 (3.45-5.53) μM against CCRF-CEM cells, with a maximum cytotoxic effect (Emax) of 91.1%.
Demonstrated a CC50 of 8.05 (3.80-17.06) μM against MOLT-4 cells, with a maximum cytotoxic effect (Emax) of 99.1%.
Demonstrated a CC50 of 39.69 (24.72-63.71) μM against MCF7 cells, with a maximum cytotoxic effect (Emax) of 62.8%.
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Cell Line:K562 chronic myelogenous leukemia cells (P53/CDKN2A-mutated), Lucena multidrug-resistant chronic myelogenous leukemia cells (P-glycoprotein-expressing MDR phenotype), Human peripheral blood mononuclear cells (hPBMCs, nontumor cells)
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Concentration:0.003-100 μM
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Incubation Time:72 h
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Result:Demonstrated a CC50 of 9.44 (5.02-17.75) μM, with a maximum cytotoxic effect (Emax) of 93.6%.
Demonstrated a CC50 of 9.33 (5.48-15.90) μM against Lucena multidrug-resistant chronic myelogenous leukemia cells, with a maximum cytotoxic effect (Emax) of 93.5%.
Reduced hPBMC viability by only 33% at the highest tested concentration (50 μM), and did not decrease viability by ≥50% at any tested concentration.
Chemical Information
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Peso molecular 356.42
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Fòrmula C18H24N6O2
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SMILES
OC1=CC=CC(C2=NC(N3CCNCCC3)=NC(N4CCOCC4)=N2)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LASSBio-2337 Related Classifications
HY-181710 Related Classifications
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