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(R)-NX-2127 (compound 28) is an orally bioavailable Bruton’s Tyrosine Kinase (Btk) degrader. (R)-NX-2127 mediates the degradation of transcription factors IKZF1 and IKZF3 through molecular glue interactions with the cereblon E3 ubiquitin ligase complex. NX-2127 degrades common BTK resistance mutants, including BTKC481S. NX-2127 can bind and proteasomally degrade each mutant BTK proteoform, resulting in potent blockade of BCR signaling. NX-2127 exhibited rapid association and dissociation rates, with Kd values of 18 nM (for WT BTK), 45 nM (BTK C481S), 18 nM (BTK T474I), 44 nM (BTK M437R), 97 nM (BTK V416L), and 88 nM (BTK L528W).
| Cell Experiment | |
|---|---|
| Cell lines | knock-in BTK WT, C481S, V416L, T474I, or L528W TMD8 cells |
| Preparation method | Calcium flux Intracellular calcium levels in knock-in BTK WT, C481S, V416L, T474I, or L528W TMD8 cells were either treated with vehicle [dimethyl sulfoxide (DMSO)] or 1 mM of NX-2127 for 24 hours before staining using Indo-1 on an LSR-Fortessa-HTS flow cytometer. Indo-1 Violet and Indo-1 Blue levels were measured for two minutes immediately followed by stimulation with 10 μg/ml of anti-human IgM and then measured continuously for 10 min. BTK WT or L528W mutant cells expressing shHCK or shILK were treated with doxycycline for 48 hours before being stained using Indo-1 and measured as described above. |
| Concentrations | 1 mM |
| Incubation time | 24 hours |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 719.83 |
| Formula | C39H45N9O5 |
| CAS Number | 3024312-52-2 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related BTK Products |
|---|
| PCI-32765
PCI-32765 (Ibrutinib) is a potent, selective and orally bioavailable irreversible inhibitor of BTK with IC50 value of 0.46 nM. |
| Spebrutinib (AVL-292)
Spebrutinib (AVL-292) is an oral, potent and selective small molecule covalent inhibitor of Btk (IC50 < 0.5 nM). |
| CNX-774
CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM. |
| GDC-0834
GDC-0834 is a novel potent and selective BTK inhibitor with IC50 of 5.9 nM. |
| CGI1746
CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM. |
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