Art. -Nr.: HY-153321

Bexobrutideg

(Synonyms: NX-5948; BTK-IN-24)

3 Cited Publications

Kundenbewertung

Based on 3 publication(s) in Google Scholar

Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker).
(Pink: Btk ligand (HY-170324); Blue: Cereblon ligand (HY-171893); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.25%
CAS. Nr.: 2649400-34-8
Formel: C₄₂H₅₄N₁₂O₅
Molecular Weight:806.96

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Bexobrutideg Chemical Structure

CAS. Nr.: 2649400-34-8

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker)^[1]^[2]^[3]. (Pink: Btk ligand (HY-170324); Blue: Cereblon ligand (HY-171893); Black: linker).

IC₅₀ & Target^[1]^[2]

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

Bexobrutideg (NX-5948) (BTK-IN-24; 0.0001-1000 nM; 4 h) is a potent degrader of BTK in primary human B cells (DC₅₀=0.34 nM) and inhibits BCR signaling^[1]. NX-5948 induces the degradation of BTK (DC₅₀< 1 nM) in lymphoma cell lines and PBMCs^[3].
Bexobrutideg (NX-5948) (10 nM; 0.25, 0.5, 1, 2, 4, 6, 18, 24 h) catalyzes rapid BTK degradation within 1 hour and is complete within 2 hours in Ramos cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Bexobrutideg (NX-5948) (BTK-IN-24; 10, 30 mg/kg; po; daily; Day 18 to 36) is efficacious and well-tolerated in a mouse collagen-induced arthritis (CIA) model and suppresses antibody titers and IL-6 cytokine levels^[1].
Bexobrutideg (NX-5948) (3, 10, 30 mg/kg; po) causes dose- and time-dependent reduction in BTK levels in circulating murine and non-human primate, cynomolgus monkey B cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Mouse collagen-induced arthritis (CIA) model^[1]
Dosage:

10, 30 mg/kg
Administration:

PO; daily; Day 18 to 36
Result:

Showed efficacious and well-tolerated in a mouse CIA model.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2649400-34-8
Appearance Solid
Molecular Weight 806.96
Formel C₄₂H₅₄N₁₂O₅
Color Off-white to yellow
SMILES

NC(C1=C(N=C(N2C[C@H](N3C(N(CC3)C)=O)CCC2)C=N1)NC4=CC=C(C5CCN(CC5)CC6CCN(C7=CN=C(C(N[C@@H]8C(NC(CC8)=O)=O)=O)C=C7)CC6)C=C4)=O
Synonyms

NX-5948; BTK-IN-24
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

All

Sort by:

Journal Impact Factor

Blood Adv

PLCG2 Exon-Skipped Variants: Insights into Their Potential Role in Chronic Lymphocytic Leukemia. [Abstract]

2026 Jun 5:bloodadvances.2025019077. PMID: 42263669
Res Sq

2026 May 15.
bioRxiv

IL-16 production is a mechanism of resistance to BTK inhibitors and R-CHOP in lymphomas. [Abstract]

2025 May 10:2025.05.07.652612. PMID: 40654846

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (123.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2392 mL

6.1961 mL

12.3922 mL

5 mM

0.2478 mL

1.2392 mL

2.4784 mL

10 mM

0.1239 mL

0.6196 mL

1.2392 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 3.33 mg/mL (4.13 mM); Clear solution

This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 3.33 mg/mL (4.13 mM); Clear solution

This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3.33 mg/mL (4.13 mM); Clear solution

This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mark Noviski, et al. NX-5948, a Selective Degrader of BTK, Significantly Reduces Inflammation in a Model of Autoimmune Disease. 2021 Nurix Therapeutics, Inc.

[2]. 4473 Initial Findings from a First-in-Human Phase 1a/b Trial of NX-5948, a Selective Bruton’s Tyrosine Kinase (BTK) Degrader, in Patients with Relapsed/Refractory B Cell Malignancies. Annual Meeting & Exposition, Monday, December 11, 2023.

[3]. Zi Liu, et al. An overview of PROTACs: a promising drug discovery paradigm. Mol Biomed. 2022 Dec 20;3(1):46. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2392 mL	6.1961 mL	12.3922 mL	30.9805 mL
	5 mM	0.2478 mL	1.2392 mL	2.4784 mL	6.1961 mL
	10 mM	0.1239 mL	0.6196 mL	1.2392 mL	3.0980 mL
	15 mM	0.0826 mL	0.4131 mL	0.8261 mL	2.0654 mL
	20 mM	0.0620 mL	0.3098 mL	0.6196 mL	1.5490 mL
	25 mM	0.0496 mL	0.2478 mL	0.4957 mL	1.2392 mL
	30 mM	0.0413 mL	0.2065 mL	0.4131 mL	1.0327 mL
	40 mM	0.0310 mL	0.1549 mL	0.3098 mL	0.7745 mL
	50 mM	0.0248 mL	0.1239 mL	0.2478 mL	0.6196 mL
	60 mM	0.0207 mL	0.1033 mL	0.2065 mL	0.5163 mL
	80 mM	0.0155 mL	0.0775 mL	0.1549 mL	0.3873 mL
	100 mM	0.0124 mL	0.0620 mL	0.1239 mL	0.3098 mL

Bexobrutideg

3 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Bexobrutideg

Immunology/Inflammation Compound Library

Protein Tyrosine Kinase Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Coagulation and Anti-coagulation Compound Library

PROTAC Library

Autoimmune Disease Compound Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Bexobrutideg

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bexobrutideg

Immunology/Inflammation Compound Library

Protein Tyrosine Kinase Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Coagulation and Anti-coagulation Compound Library

PROTAC Library

Autoimmune Disease Compound Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Bexobrutideg

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bexobrutideg Related Classifications

HY-153321 Related Classifications