Anselmi, Michele; Borbely, Adina; Figueras, Eduard; Michalek, Carmela; Kemker, Isabell; Gentilucci, Luca; Sewald, Norbert published an article in 2021. The article was titled 《Linker hydrophilicity modulates the anticancer activity of RGD-cryptophycin conjugates》, and you may find the article in Chemistry – A European Journal.SDS of cas: 21085-72-3 The information in the text is summarized as follows:
Most anticancer agents are hydrophobic and can easily penetrate the tumor cell membrane by passive diffusion. This may impede the development of highly effective and tumor-selective treatment options. A hydrophilic β-glucuronidase-cleavable linker was used to connect the highly potent antimitotic agent cryptophycin-55 glycinate with the αvβ3 integrin ligand c(RGDfK). Incorporation of the self-immolative linker containing glucuronic acid results in lower cytotoxicity than that of the free payload, suggesting that hydrophilic sugar linkers can preclude passive cellular uptake. In vitro drug-release studies and cytotoxicity assays demonstrated the potential of this small mol.-drug conjugate, providing guidance for the development of therapeutics containing hydrophobic anticancer drugs. The experimental part of the paper was very detailed, including the reaction process of (2R,3R,4S,5S,6S)-2-Bromo-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate(cas: 21085-72-3SDS of cas: 21085-72-3)
(2R,3R,4S,5S,6S)-2-Bromo-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate(cas: 21085-72-3) may be used for the synthesis of HMR1098-S-Glucuronide Methyl Ester, a new K-ATP-blocking agent being developed as a drug for prevention of sudden cardiac death.SDS of cas: 21085-72-3
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary