MAC glucuronide linker - CAS 2260960-07-2

MAC glucuronide linker - CAS 2260960-07-2 Catalog number: BADC-00672

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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.

Category
ADCs Linker
Product Name
MAC glucuronide linker
CAS
2260960-07-2
Catalog Number
BADC-00672
Molecular Formula
C43H48BrN3O17S
Molecular Weight
990.82
MAC glucuronide linker

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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.
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Room temperature
The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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