MEAP
MEAP (2-(4-Morpholinoanilino-6-[(2-exo-norbornyl) amino)-purine) is a NEDD9-STAT3 modulator. MEAP disrupts NEDD9-STAT3 interaction, driving STAT3 Y705 dephosphorylation. MEAP induces G2/M phase arrest. MEAP can be used for the research of anaplastic thyroid cancer.
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- Formule: C25H33N7O
- Masse moléculaire:447.58
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
STAT3 |
In Vitro
MEAP potently inhibits AURKA, AURKB, AURKC, and FAK kinases in a cell-free biochemical assay[1].
MEAP potently induces centrosome-mediated microtubule nucleation in THJ-16T anaplastic thyroid cancer cells[1].
MEAP (1-5 μM) increases pericentriolar material accumulation at less active centrosomes during interphase and early mitosis in THJ-16T anaplastic thyroid cancer cells with normal centrosome numbers[1].
MEAP significantly increases pericentriolar material recruitment to supernumerary centrosomes in interphase THJ-11T and THJ-16T anaplastic thyroid cancer cells[1].
MEAP (300 nM; 48 h) preferentially induces spindle multipolarity by activating inactive supernumerary centrosomes in ALDH+ THJ-11T and THJ-16T anaplastic thyroid cancer cells, without changing centrosome amplification or fragmentation rates[1].
MEAP (300 nM; 48 h) induces selective G2/M phase arrest in ALDH+ THJ-16T anaplastic thyroid cancer cells, without selective apoptosis or senescence relative to ALDH− cells[1].
MEAP (300 nM; 96 h) reduces the ALDH+ anaplastic thyroid cancer cell population by over 80% in THJ-11T, THJ-16T, and 8505c cells via selective growth inhibition, with a dose-dependent response in THJ-16T cells[1].
MEAP (0.1-1 μM) pretreatment dose-dependently suppresses tumorsphere formation in THJ-11T, THJ-16T, and 8505c anaplastic thyroid cancer cells, attenuating stemness[1].
MEAP (100 nM; 5-60 min) selectively induces rapid dephosphorylation of STAT3Y705 in ALDH+ THJ-16T anaplastic thyroid cancer cells, while nonselectively reducing phosphorylated Aurora-A levels[1].
MEAP (100 nM; 10 min) disrupts the NEDD9-STAT3 protein interaction in ALDH+ THJ-16T anaplastic thyroid cancer cells within 10 minutes[1].
MEAP (100 nM; 15 min) reduces colocalization of NEDD9 and phosphorylated STAT3Y705 in ALDH+ THJ-16T anaplastic thyroid cancer cells, altering their intracellular localization[1].
MEAP (100 nM; 24 h) induces centrosome microtubule nucleation and γ-tubulin accumulation in ALDH+ THJ-16T anaplastic thyroid cancer cells in a NEDD9-STAT3-dependent manner[1].
MEAP reduces chromosome missegregation in ALDH+ THJ-16T anaplastic thyroid cancer cells in a NEDD9-STAT3-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Sorted ALDH+ and ALDH- THJ-11T and THJ-16T anaplastic thyroid cancer cells
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Concentration:300 nM
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Incubation Time:48 h
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Result:Reduced the percentage of inactive mitotic centrosomes in ALDH+ THJ-11T and THJ-16T cells.
Increased spindle multipolarity (32% in ALDH+ cells vs. 8% in ALDH- cells) and decreased pseudobipolar spindles in ALDH+ cells.
Did not alter the frequency of centrosome amplification or centrosome fragmentation.
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Cell Line:Sorted ALDH+ and ALDH- THJ-16T anaplastic thyroid cancer cells
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Concentration:300 nM
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Incubation Time:1 h; 24 h; 48 h
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Result:Induced G2/M phase accumulation in ALDH+ cells (reaching 15% of cells in G2/M by 48 hours) but not in ALDH- cells.
Did not cause selective apoptosis or senescence in ALDH+ cells relative to ALDH- cells.
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Cell Line:Sorted ALDH+ and ALDH- THJ-16T anaplastic thyroid cancer cells
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Concentration:100 nM
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Incubation Time:5 min; 15 min; 30 min; 45 min; 60 min
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Result:Rapidly depleted pSTAT3-Y705 levels in ALDH+ cells within 5 minutes, with no change in ALDH- cells.
Reduced phosphorylated Aurora-A levels nonselectively in both ALDH+ and ALDH- cells.
Did not alter total STAT3, total Aurora-A, or NEDD9 protein levels.
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Cell Line:ALDH+ THJ-16T anaplastic thyroid cancer cells
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Concentration:100 nM
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Incubation Time:15 min
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Result:Reduced colocalization of NEDD9 and pSTAT3-Y705, with Pearson's R value decreasing from 0.83 (DMSO) to 0.33.
Decreased cytoplasmic pSTAT3-Y705 staining and redistributed NEDD9 from the perinuclear region.
In Vivo
MEAP (30 mg/kg; i.p.; triweekly; 4 weeks) drives a robust antitumor response with ~4-fold tumor volume reduction relative to controls and no apparent host toxicity in a subcutaneous ATC mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID (female, 6- to 8-week-old, orthotopic model with 5 × 105 8505c ATC cells injected into right thyroid gland)[1]
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Dosage:30 mg/kg
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Administration:i.p.; 3 total doses on day 15, 17, and 20
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Result:Eliminated detectable ALDH1-positive cell clusters in tumors.
Increased the γ-tubulin weak/strong centrosome symmetry ratio from 0.29 to 0.74.
Increased the percentage of mitotic cells with multipolar spindles to ~15%.
Reduced the percentage of mitotic cells with missegregated chromosomes to ~40%.
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Animal Model:NOD-SCID (female, 6- to 8-week-old, subcutaneous model with 8505c ATC cells implanted subcutaneously, treatment initiated when tumors reached 40-80 mm3)[1]
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Dosage:30 mg/kg
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Administration:i.p.; triweekly for 4 weeks
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Result:Resulted in a ~4-fold reduction in tumor volume compared with vehicle controls.
Outperformed Taxol in suppressing ATC tumor growth.
Caused no detectable toxicity or body weight loss.
Chemical Information
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Masse moléculaire 447.58
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Formule C25H33N7O
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SMILES
C[C@@H]1[C@H](C[C@H]2C[C@@H]1C2(C)C)NC3=C4N=CNC4=NC(NC5=CC=C(C=C5)N6CCOCC6)=N3
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Synonyms
2-(4-Morpholinoanilino-6-[(2-exo-norbornyl) amino)-purine
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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)
MEAP Related Classifications
HY-183628 Related Classifications
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Keywords
- MEAP
- 2-(4-Morpholinoanilino-6-[(2-exo-norbornyl) amino)-purine
- STAT
- anaplastic thyroid cancer
- NEDD9-STAT3 interaction
- pericentriolar accumulation
- STAT3 Y705
- spindle multipolarity
- G2/M phase arrest
- centrosome microtubule nucleation
- NEDD9-STAT3 signaling axis
- supernumerary centrosomes
- THJ-16T
- Inhibitor
- inhibitor
- inhibit