| Name | NX-5948 |
| Description | NX-5948 (BTK-IN-24) is an orally bioavailable and blood-brain barrier-penetrable PROTAC BTK degrader with anti-inflammatory and antitumor activities. It induces BTK protein degradation via the cereblon E3 ligase complex, inhibiting B cell activation. |
| In vitro | NX-5948 (0.0001-1000 nM; 4 hrs) is a potent degrader of BTK in primary human B cells (DC50=0.34 nM) and inhibits BCR signaling. In Ramos cells, NX-5948 (10 nM; 0.25, 0.5, 1, 2, 4, 6, 18, 24 hr) rapidly catalyzes BTK degradation within 1 hr and completes the degradation process within 2 hr. [1]
NX-5948 induces BTK degradation in lymphoma cell lines and PBMC (DC50< 1 nM). [3] |
| In vivo | In a mouse model of collagen-induced arthritis (CIA), NX-5948 (10, 30 mg/kg; oral gavage; daily; days 18-36) demonstrated good efficacy and tolerability, inhibiting antibody titers and cytokine IL-6 levels. [1]
NX-5948 (3, 10, 30 mg/kg; oral gavage) caused dose- and time-dependent decreases in circulating BTK levels in mice and non-human primate and cynomolgus monkeys. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 3.3 mg/mL (4.09 mM), Sonication is recommended.
DMSO : 40 mg/mL (49.57 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
|
| Inhibitors Related | evobrutinib | (±)-Zanubrutinib | Bavdegalutamide | Sunvozertinib | Ibrutinib | dBET6 | IBT6A | Dbet57 | Orelabrutinib | ARV-825 | Remibrutinib | Vepdegestrant |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | CNS-Penetrant Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
