M9101
M9101 is a selective Aurora A PROTAC degrader with a DC50 of 2.3 nM. M9101 induces G2/M arrest in triple-negative breast cancer cells and potently inhibits the proliferation of multiple tumor cell lines. M9101 can be used in the research of various cancers including triple-negative breast cancer.
(Pink: Aurora A Target protein ligand; Blue: Cereblon ligand (HY-W248665); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C38H38ClN9O6S
- Peso molecular:784.28
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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
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Chemical Information
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Ver todos los productos específicos de isoformas PROTACs
MoreVer todos los productos específicos de isoformas Aurora Kinase
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Actividad biológica
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Aurora A 2.3 nM (DC50) |
Aurora B > 1 μM (DC50) |
Cereblon |
M9101 (0.01-1000 nM; 4 h) induces selective, dose-dependent degradation of Aurora A in BT549 and BT20 triple-negative breast cancer cells[1].
M9101 (10-100 nM; 4 h) exhibits high selectivity for Aurora A in MDA-MB-231 cells, with significant degradation of only Aurora A observed in a global proteomic analysis of 4680 proteins, and no degradation of known TP0903 off-target kinases[1].
M9101 (graded concentrations; 72 h) potently inhibits the proliferation of multiple cancer cell lines, with IC50 values ranging from 11.7 nM to 80.1 nM across tested models including triple-negative breast cancer, non-small cell lung cancer, prostate cancer, melanoma, multiple myeloma, bladder cancer, lymphoma, and rhabdomyosarcoma[1].
M9101 (indicated concentrations; 12 h) induces dose-dependent G2/M phase accumulation in MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BT549 and BT20 triple-negative breast cancer cells
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Concentration:0.01, 0.1, 0.3, 1, 3, 10, 30, 100, 300 and 1000 nM
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Incubation Time:4 h
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Result:Induced selective, dose-dependent degradation of Aurora A in both BT549 and BT20 cells.
Caused no significant degradation of Aurora B across the tested concentrations.
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Cell Line:MDA-MB-231 triple-negative breast cancer cells
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Concentration:10 and 100 nM
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Incubation Time:12 h
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Result:Induced dose-dependent accumulation of cells in the G2/M phase, a phenotype more pronounced than that caused by the catalytic inhibitor alisertib.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17/SCID (female, 6 to 8 weeks old, subcutaneous xenograft model)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; daily; 5 consecutive days
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Result:Induced 86.9% maximum degradation of Aurora A and 59.8% maximum degradation of Aurora B in tumor tissue at 10 mg/kg.
Induced 94.2% maximum degradation of Aurora A and 62.1% maximum degradation of Aurora B in tumor tissue at 20 mg/kg.
Caused no obvious changes in body weight with either dose.
Chemical Information
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Peso molecular 784.28
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Fòrmula C38H38ClN9O6S
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SMILES
O=C1NC(CCC1N2C(C3=CC4=C(C=C3C2=O)CN(C4)C5CCN(CC5)C6=CC=C(NC7=NC=C(Cl)C(NC8=CC=CC=C8S(N(C)C)(=O)=O)=N7)C=C6)=O)=O
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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)
M9101 Related Classifications
HY-184193 Related Classifications
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