Description
MAC glucuronide linker is a vital tool used in the biomedical industry for drug discovery and targeted therapy. It enables the conjugation of drugs with glucuronide, facilitating their delivery and activation in specific organs or tissues. This linker plays a significant role in treating various diseases, including cancer, inflammation, and metabolic disorders.
IUPAC Name
methyl (2S,3S,4S,5R,6S)-3,4,5-triacetyloxy-6-[4-[[bromomethyl(2-methylsulfonylethyl)carbamoyl]oxymethyl]-2-[[2-[9H-fluoren-9-ylmethoxycarbonyl(methyl)amino]acetyl]amino]phenoxy]oxane-2-carboxylate
Canonical SMILES
CC(=O)OC1C(C(OC(C1OC(=O)C)OC2=C(C=C(C=C2)COC(=O)N(CCS(=O)(=O)C)CBr)NC(=O)CN(C)C(=O)OCC3C4=CC=CC=C4C5=CC=CC=C35)C(=O)OC)OC(=O)C
InChI
InChI=1S/C43H48BrN3O17S/c1-24(48)60-36-37(61-25(2)49)39(62-26(3)50)41(64-38(36)40(52)57-5)63-34-16-15-27(21-58-43(54)47(23-44)17-18-65(6,55)56)19-33(34)45-35(51)20-46(4)42(53)59-22-32-30-13-9-7-11-28(30)29-12-8-10-14-31(29)32/h7-16,19,32,36-39,41H,17-18,20-23H2,1-6H3,(H,45,51)/t36-,37-,38-,39+,41+/m0/s1
In Vitro
A series of MAC β-glucuronide model constructs were prepared to evaluate stability and enzymatic release, and the results demonstrated high stability at physiological pH in a substitution-dependent manner. All the MAC model compounds efficiently released alcohol drug surrogates under the action of β-glucuronidase. To assess the MAC technology for ADCs, the potent microtubule-disrupting agent auristatin E (AE) was incorporated through the norephedrine alcohol. Conjugation of the MAC β-glucuronide AE drug linker to the anti-CD30 antibody cAC10, and an IgG control antibody, gave potent and immunologically specific activities in vitro and in vivo.
Shipping
Room temperature