GNE-987 GSH linker-2
GNE-987 GSH linker-2 (compound 9a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 GSH linker-2 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.23 nM and 0.38 nM, respectively[1].
Product Specifications
UNSPSC
12352203
Target
Epigenetic Reader Domain; PROTAC-Linker Conjugates for PAC
Type
ADC Related
Related Pathways
Antibody-drug Conjugate/ADC Related; Epigenetics; PROTAC
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/protac-brd4-degrader-11.html
Purity
99.48
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@H](CN3C([C@@H](NC(CCCCCCCCCCNC(C4=CC(N(C5=NC=C(F)C=C5F)CC6=CNC7=C6C8=CN(C)C7=O)=C8C=C4CS(=O)(C)=O)=O)=O)C(C)(C)C)=O)OC(OC[C@@H](C)SS(C)(=O)=O)=O)=O)C=C2
Molecular Formula
C61H75F2N9O12S4
Molecular Weight
1292.56
References & Citations
[1]Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64 (5) :2576-2607.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, sealed storage, away from moisture and light)
Scientific Category
ADC Related
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
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