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DBPR728

Chemical Structure : DBPR728

CAS No.: 2702965-64-6

DBPR728 (DBPR-728)

Catalog No.: PC-22141Not For Human Use, Lab Use Only.

DBPR728 is an oral bioavailable acyl-based prodrug of 6K465, which is a potent selective Aurora A (AURKA) inhibitor, effectively inhibits cancer cells overexpressing c-MYC- and/or N-MYC.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

DBPR728 is an oral bioavailable acyl-based prodrug of 6K465, which is a potent selective Aurora A (AURKA) inhibitor, effectively inhibits cancer cells overexpressing c-MYC- and/or N-MYC.
DBPR728 induced durable tumor regression of c-MYC- and/or N-MYC- overexpressing xenografts including SCLC, triple-negative breast cancer (TNBC), hepatocellular carcinoma and medulloblastoma.
DBPR728 at 300 mg/kg induced c-MYC reduction and cell apoptosis in the tumor xenografts for more than 7 days.
DBPR728 also synergized with the mTOR inhibitor everolimus to suppress c-MYC- or N-MYC- driven SCLC.

Physicochemical Properties

M.Wt 598.12
Formula C29H37ClFN9O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(5-((2-((1-(3-chloro-2-fluorobenzoyl)piperidin-4-yl)amino)-6-(4-ethylpiperazin-1-yl)pyrimidin-4-yl)amino)-3-methyl-1H-pyrazol-1-yl)propan-1-one

References

1. Chang CP, et al. Mol Cancer Ther. 2024 Apr 9. doi: 10.1158/1535-7163.MCT-23-0602.

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