1307864-98-7

Basic information

• Product Name: C₂₄H₂₈N₄O₄
• Synonyms: C₂₄H₂₈N₄O₄
• CAS NO: 1307864-98-7
• Molecular Weight: 436.511
• Mol File: 1307864-98-7.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: C₂₄H₂₈N₄O₄(CAS DataBase Reference)
• NIST Chemistry Reference: C₂₄H₂₈N₄O₄(1307864-98-7)
• EPA Substance Registry System: C₂₄H₂₈N₄O₄(1307864-98-7)

Safety Data

• Hazardous Substances Data: 1307864-98-7(Hazardous Substances Data)

Upstream product

• 351002-16-9 TGX₀₆₆ 
• 663619-90-7 9-bromo-2-hydroxy-7-methyl-4H-pyrido[1,2-a]pyrimidin-4-one 
• 663619-89-4 7-methyl-2-(4-morpholinyl)-9-[1-(phenylamino)ethyl]-4H-pyrido[1,2-a]pyrimidin-4-one 
• 96-32-2 bromoacetic acid methyl ester 

Downstream Products

• 1308384-65-7 TGX-D₁ 
• 1307864-99-8 C₂₉H₃₉N₅O₄ 
• 1307865-00-4 NH₂-SL-TGX 

Relevant articles and documents

Development of a peptide-drug conjugate for prostate cancer therapy

TGX-221 is a highly potent phosphoinositide 3-kinase β (PI3Kβ) inhibitor that holds great promise as a novel chemotherapeutic agent to treat prostate cancer. However, poor solubility and lack of targetability limit its therapeutic applications. The objective of this present study is to develop a peptide-drug conjugate to specifically deliver TGX-221 to HER2 overexpressing prostate cancer cells. Four TGX-221 derivatives with added hydroxyl groups were synthesized for peptide conjugation. Among them, TGX-D1 exhibited a similar bioactivity to TGX-221, and it was selected for conjugation with a peptide promoiety containing a HER2-targeting ligand and a prostate specific antigen (PSA) substrate linkage. From this selection, the peptide-drug conjugate was proven to be gradually cleaved by PSA to release TGX-D1. Cellular uptake of the peptide-drug conjugate was significantly higher in prostate cancer cells compared to the parent drug. Moreover, both the peptide-drug conjugate and its cleaved products demonstrated comparable activities as the parent drug TGX-D1. Our results suggest that this peptide-drug conjugate may provide a promising chemotherapy for prostate cancer patients.