1. PROTAC Epigenetics Cell Cycle/DNA Damage
  2. PROTACs Aurora Kinase
  3. 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).

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

M9101

M9101 Chemical Structure

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Description

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[1]. (Pink: Aurora A Target protein ligand; Blue: Cereblon ligand (HY-W248665); Black: linker).

IC50 & Target[1]

Aurora A

2.3 nM (DC50)

Aurora B

> 1 μM (DC50)

Cereblon

 

In Vitro

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.

Western Blot Analysis[1]

Cell Line: BT549 and BT20 triple-negative breast cancer cells
Concentration: 0.01, 0.1, 0.3, 1, 3, 10, 30, 100, 300 and 1000 nM
Incubation Time: 4 h
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.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 triple-negative breast cancer cells
Concentration: 10 and 100 nM
Incubation Time: 12 h
Result: Induced dose-dependent accumulation of cells in the G2/M phase, a phenotype more pronounced than that caused by the catalytic inhibitor alisertib.
In Vivo

M9101 (10-20 mg/kg; i.p.; daily; 5 days) selectively degrades Aurora A in MDA-MB-231 xenograft tumors, achieving 86.9% and 94.2% maximum degradation at 10 mg/kg and 20 mg/kg, respectively, with minimal Aurora B degradation and no detectable body weight changes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CB17/SCID (female, 6 to 8 weeks old, subcutaneous xenograft model)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; daily; 5 consecutive days
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.
Molecular Weight

784.28

Formula

C38H38ClN9O6S

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

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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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.

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Product Name:
M9101
Cat. No.:
HY-184193
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