2. PI3K/Akt/mTOR
  3. mTOR PI3K
  4. 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.

For research use only. We do not sell to patients.

LASSBio-2337

LASSBio-2337 Chemical Structure

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LASSBio-2337 Related Antibodies

Top Publications Citing Use of Products

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mTOR mTORC1 mTORC2

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Description

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[1].

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.

LASSBio-2337 Related Antibodies

Cell Cytotoxicity Assay[1]

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)
Concentration: 0.003-100 μM
Incubation Time: 72 h
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%.

Cell Cytotoxicity Assay[1]

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)
Concentration: 0.003-100 μM
Incubation Time: 72 h
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.
Molecular Weight

356.42

Formula

C18H24N6O2
SMILES

OC1=CC=CC(C2=NC(N3CCNCCC3)=NC(N4CCOCC4)=N2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LASSBio-2337 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LASSBio-2337LASSBio2337LASSBio 2337mTORPI3KMammalian target of RapamycinPhosphoinositide 3-kinaserat liver microsomesCCRF-CEM cellshuman peripheral blood mononuclear cellsleukemia cellschronic myelogenous leukemiaMOLT-4 cellsPI3K isoformsbreast canceracute lymphoblastic leukemiaInhibitorinhibitorinhibit

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