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NX-5948
🥰Excellent
Catalog No. T75124Cas No. 2649400-34-8
Alias NX5948, BTK-IN-24
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.
NX-5948
🥰Excellent
Catalog No. T75124Alias NX5948, BTK-IN-24Cas No. 2649400-34-8
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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | 359 € | In Stock | |
| 5 mg | 796 € | In Stock | |
| 10 mg | 1.263 € | In Stock | |
| 25 mg | 2.546 € | In Stock | |
| 50 mg | 3.439 € | In Stock | |
| 1 mL x 10 mM (in DMSO) | 1.130 € | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
| 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] |
| Alias | 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 & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 40 mg/mL (49.57 mM), Sonication is recommended.  H2O: < 1 mg/mL(Insoluble) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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