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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $77 | - | In Stock | |
| 5 mg | $156 | - | In Stock | |
| 10 mg | $235 | - | In Stock | |
| 25 mg | $376 | - | In Stock | |
| 50 mg | $567 | - | In Stock | |
| 100 mg | $787 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $198 | - | In Stock |
| 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. |
| Targets&IC50 | BTK in primary B cells (human):0.34 nM (DC50) |
| 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] |
| Synonyms | NX5948, BTK-IN-24 |
| Molecular Weight | 806.96 |
| Formula | C42H54N12O5 |
| Cas No. | 2649400-34-8 |
| Smiles | N(C=1N=C(C=NC1C(N)=O)N2C[C@@H](CCC2)N3C(=O)N(C)CC3)C4=CC=C(C=C4)C5CCN(CC6CCN(CC6)C=7C=CC(C(N[C@@H]8C(=O)NC(=O)CC8)=O)=NC7)CC5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 40 mg/mL (49.57 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (4.09 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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