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Art. -Nr.: HY-183628

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MEAP

(Synonyms: 2-(4-Morpholinoanilino-6-[(2-exo-norbornyl) amino)-purine)

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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Formel: C₂₅H₃₃N₇O
Molecular Weight:447.58

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

MEAP Chemical Structure

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
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Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

STAT3

Alle STAT Isoform-spezifische Produkte anzeigen :

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 STAT3^Y705 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 STAT3^Y705 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.

Immunofluorescence^[1]

Cell Line:

Sorted ALDH+ and ALDH- THJ-11T and THJ-16T anaplastic thyroid cancer cells
Concentration:

300 nM
Incubation Time:

48 h
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.

Cell Cycle Analysis^[1]

Cell Line:

Sorted ALDH+ and ALDH- THJ-16T anaplastic thyroid cancer cells
Concentration:

300 nM
Incubation Time:

1 h; 24 h; 48 h
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.

Western Blot Analysis^[1]

Cell Line:

Sorted ALDH+ and ALDH- THJ-16T anaplastic thyroid cancer cells
Concentration:

100 nM
Incubation Time:

5 min; 15 min; 30 min; 45 min; 60 min
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.

Immunofluorescence^[1]

Cell Line:

ALDH+ THJ-16T anaplastic thyroid cancer cells
Concentration:

100 nM
Incubation Time:

15 min
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.; 3 total doses on days 15, 17, and 20) selectively eliminates ALDH⁺ ATC cell clusters, increases centrosome symmetry, induces spindle multipolarity, and reduces chromosomal instability in an orthotopic mouse model^[1].
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.

Animal Model:

NOD-SCID (female, 6- to 8-week-old, orthotopic model with 5 × 10⁵ 8505c ATC cells injected into right thyroid gland)^[1]
Dosage:

30 mg/kg
Administration:

i.p.; 3 total doses on day 15, 17, and 20
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%.

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]
Dosage:

30 mg/kg
Administration:

i.p.; triweekly for 4 weeks
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

Molecular Weight 447.58
Formel C₂₅H₃₃N₇O
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
Synonyms

2-(4-Morpholinoanilino-6-[(2-exo-norbornyl) amino)-purine
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Yu HG, et al. ALDH+ Anaplastic Thyroid Cancer Cells Show Vulnerability to a Pharmacologic Inducer of Centrosome Declustering. Cancer Res Commun. 2026;6(5):1151-1167. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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MEAP

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

MEAP Related Classifications

HY-183628 Related Classifications