LAF389
LAF389, a prodrug of LAF153 (HY-183876), is a methionine aminopeptidase (MetAps) inhibitor with an IC50 of 800 nM against MetAp2, and exhibits a maximum inhibition rate of 20% against MetAp1 at 300 nM. LAF389 possesses antiproliferative, antiangiogenic and cytotoxic activities. LAF389 can be used in research related to cancers such as advanced solid tumors.
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- CAS No.: 270902-51-7
- Formule: C25H42N2O8
- Masse moléculaire:498.61
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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MetAp2 800 nM (IC50) |
MetAp1 |
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
13 nM
Compound: LAF389
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Antiproliferative activity against human A549 cells after 96 hrs
Antiproliferative activity against human A549 cells after 96 hrs
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[PMID: 28185457] |
| HCT-116 | IC50 |
23 nM
Compound: LAF389
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Antiproliferative activity against human HCT116 cells after 96 hrs
Antiproliferative activity against human HCT116 cells after 96 hrs
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[PMID: 28185457] |
| MDA-MB-435 | IC50 |
40 nM
Compound: LAF389
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Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability after 72 hrs by MTS assay
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[PMID: 28185457] |
LAF389 potently inhibits monolayer proliferation of human cancer cell lines, including those unresponsive to standard cytotoxics or with drug resistance, and is more unaffected by P-glycoprotein overexpression than paclitaxel[1].
LAF389 (0.0001-10 μM; 72 h) inhibits proliferation of HUVEC (IC50 = 20 nM) and A549 human non-small cell lung carcinoma cells, with greater potency against endothelial cells and cytotoxic activity against A549 cells at micromolar concentrations[2].
LAF389 (3-300 nM; 8-48 h) induces a pH-shifted, unprocessed form of 14-3-3γ in H1299, U2OS, MDA-MB-435, and A549 cells, with detection starting at 3 nM after 24 h and accumulation over 48 h[2].
LAF389 (0.1-1000 nM; 18 h) inhibits processing of 14-3-3γ in HUVEC, inducing the unprocessed form with maximal response at 1 μM after 18 h of incubation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 human non-small cell lung carcinoma cells, human umbilical vein endothelial cells (HUVEC)
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Concentration:0.0001, 0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:72 h
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Result:Potently inhibited HUVEC proliferation with an IC50 of 20 nM.
Inhibited A549 cell proliferation with roughly 10-fold lower potency.
Caused substantial cell death of A549 cells at micromolar concentrations.
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Cell Line:H1299 human small cell lung carcinoma cells, U2OS, MDA-MB-435, A549 human non-small cell lung carcinoma cells
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Concentration:3-300 nM (24 h incubation); 200 nM (8 h, 24 h, 48 h incubation)
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Incubation Time:8 h, 24 h, 48 h
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Result:Shifted the isoelectric point of the 14-3-3γ isoform to a more basic pH in H1299 cells.
Caused the shifted band to be detectable after 8 h of incubation and accumulate up to 48 h.
Induced effects starting at 3 nM LAF389 at 24 h, increasing up to 300 nM.
Confirmed the shifted band as the unprocessed form of 14-3-3γ, retaining its N-terminal methionine.
Induced the same effect in U2OS, MDA-MB-435, and A549 cells.
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Cell Line:human umbilical vein endothelial cells (HUVEC)
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Concentration:0.1, 0.3, 1, 3, 10 and 30 nM (18 h incubation); 1, 10, 100 and 1000 nM (18 h incubation)
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Incubation Time:18 h
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Result:Inhibited MetAp processing of 14-3-3γ, leading to detection of the unprocessed form via both isoform-specific polyclonal antibodies and the unprocessed-form-specific monoclonal antibody.
Caused maximal detection of the unprocessed form at 1 μM LAF389.
LAF389 (intravenous injection; repeated bolus administration; repeated cycle 3 times with a 7-day interval after 3 consecutive days of administration) exhibits significant, frequency-dependent tumor growth inhibition in a panel of human solid tumor xenograft models in immunocompromised mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 270902-51-7
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Masse moléculaire 498.61
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Formule C25H42N2O8
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SMILES
CC(C)(C)/C=C/[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC)C(N[C@H]1CC[C@H](CNC1=O)OC(C2CCCCC2)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LAF389 Related Classifications
HY-118953 Related Classifications
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