Referencia número: HY-153220

Zelebrudomide

Name: Zelebrudomide
Brand: MedChemExpress
SKU: HY-153220
Price: 300.00 USD
Availability: InStock
Rating: 5 (2 reviews)

(Synonyms: NX-2127)

2 Cited Publications

Revisión del cliente

Based on 2 publication(s) in Google Scholar

Zelebrudomide is an orally active BTK-targeting PROTAC degrader, with DC₅₀ values of 4.5 nM and 31 nM against wild-type BTK and BTK^C481S mutant, respectively. Zelebrudomide recruits the cereblon E3 ubiquitin ligase complex to mediate the degradation of BTK. Zelebrudomide also acts as a molecular glue to bind the cereblon E3 ubiquitin ligase complex, mediating the degradation of IKZF1 and IKZF3. Zelebrudomide can be used in the research of B-cell malignancies.
(Pink: Btk ligand (HY-168302); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-168348)).

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza : 98.71%
No. CAS: 2416131-46-7
Fòrmula: C₃₉H₄₅N₉O₅
Peso molecular:719.83

Almacenamiento:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Zelebrudomide Chemical Structure

No. CAS: 2416131-46-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (2)
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Zelebrudomide is an orally active BTK-targeting PROTAC degrader, with DC₅₀ values of 4.5 nM and 31 nM against wild-type BTK and BTK^C481S mutant, respectively. Zelebrudomide recruits the cereblon E3 ubiquitin ligase complex to mediate the degradation of BTK. Zelebrudomide also acts as a molecular glue to bind the cereblon E3 ubiquitin ligase complex, mediating the degradation of IKZF1 and IKZF3. Zelebrudomide can be used in the research of B-cell malignancies^[1]. (Pink: Btk ligand (HY-168302); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-168348)).

IC₅₀ & Target

^[1]

IKZF1

57 nM (DC₅₀)

IKZF3

36 nM (DC₅₀)

IL-2

Ver todos los productos específicos de isoformas PROTACs :

Ver todos los productos específicos de isoformas IKZF Family :

Ver todos los productos específicos de isoformas Interleukin Related :

In Vitro

OthersAdaptive ImmunityCytokines & Chemokines

Others

Zelebrudomide (NX-2127) potently degrades wild-type BTK in TMD8 cells with a DC₅₀ of 4.5 nM; it also degrades the BTK^C481S mutant with a DC₅₀ of 31 nM, despite its reduced binding affinity for this mutant^[1].
Zelebrudomide (50 nM; 4 h) selectively degrades BTK in human peripheral blood mononuclear cells (PBMCs) from normal donors^[1].

Adaptive Immunity

Cytokines & Chemokines

Zelebrudomide (0.001-100 nM; 1-24 h) degrades IKZF1 (DC₅₀ = 57 nM) and IKZF3 (DC₅₀ = 36 nM) in primary human T cells, and induces IL-2 secretion in TCR-activated primary human T cells^[1].

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

In Vivo

Adaptive ImmunityAnti-cancer

Adaptive Immunity

Zelebrudomide (NX-2127) (0.3-90 mg/kg; p.o.; single dose, once daily for 5 consecutive days) induces dose-dependent in vivo BTK degradation in healthy mice^[1].
Zelebrudomide (10-100 mg/kg; p.o.; single dose, once daily for 14 consecutive days) induces potent, dose-dependent degradation of BTK and IKZF3 in cynomolgus monkeys^[1].

Anti-cancer

Adaptive Immunity

Zelebrudomide (10-90 mg/kg; p.o.; once daily for 5 consecutive days, once daily for 25 consecutive days) induces dose-dependent anti-tumor efficacy in TMD8 BTK^WT xenograft tumors and degrades BTK, IKZF1 and IKZF3^[1].
Zelebrudomide (10-90 mg/kg; p.o.; daily administration for 25 days) exhibits dose-dependent antitumor efficacy in Ibrutinib (HY-10997)-resistant TMD8 BTK^C481S xenograft tumors^[1].

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

Animal Model:

BALB/c mice; CD-1 mice^[1]
Dosage:

0.3, 3 mg/kg (single dose)
10, 30, 90 mg/kg (daily x5)
Administration:

p.o.; single dose; daily for 5 days
Result:

Suppressed mouse peripheral BTK in a dose-dependent fashion after single oral dosing across BALB/c and CD-1 strains.
Strengthened BTK suppression in BALB/c circulating B cells following five days of repeated oral administration with elevated inhibitory efficacy.

Animal Model:

BALB/c mice (xenograft model)^[1]
Dosage:

10, 30, 90 mg/kg
Administration:

p.o.; daily for 25 days; daily for 5 days
Result:

Exerted dose-dependent tumor growth inhibition of 35%, 73% and 99% following 25 days of daily oral treatment at 10, 30 and 90 mg/kg.
Dose-dependently depleted intratumoral BTK to 24%, 14% and 5% of baseline after five days of oral administration.
Downregulated intratumoral IKZF1 to 74%, 56% and 27% and intratumoral IKZF3 to 82%, 48% and 23% in a dose-responsive manner under the 5-day dosing regimen.

Animal Model:

BALB/c mice (xenograft model)^[1]
Dosage:

10, 30, 90 mg/kg
Administration:

p.o.; daily for 25 days
Result:

Achieved 17%, 43%, and 59% tumor growth inhibition (TGI), respectively.

Animal Model:

Cynomolgus monkeys^[1]
Dosage:

10, 30, 100 mg/kg
Administration:

p.o.; single dose; daily for 14 days
Result:

Induced dose-dependent BTK downregulation in monkey peripheral B cells upon single-dose treatment, and sustained BTK suppression below 10% baseline after 14 consecutive daily oral doses.
Dose-dependently lowered IKZF3 content in monkey circulating T cells following the 14-day repeated oral dosing regimen.

Ensayo clínico

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

Chemical Information

No. CAS 2416131-46-7
Appearance Solid
Peso molecular 719.83
Fòrmula C₃₉H₄₅N₉O₅
Color Light yellow to yellow
SMILES

O=C1C2=CC(N3C[C@H](CN4CCC(C5=CC=C(C=C5)NC6=C(N=CC(N7CCCCC7)=N6)C(N)=O)CC4)CC3)=CC=C2C(N1C8C(NC(CC8)=O)=O)=O
Synonyms

NX-2127
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (2)

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Blood Adv

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

2026 Jun 5:bloodadvances.2025019077. PMID: 42263669
Drug Metab Dispos

2026 Jul 14;54(8):100365. PMID: 42561496

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (138.92 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

1.3892 mL

6.9461 mL

13.8922 mL

5 mM

0.2778 mL

1.3892 mL

2.7784 mL

10 mM

0.1389 mL

0.6946 mL

1.3892 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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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.

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Robbins DW, et al. Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton's Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies. Journal of medicinal chemistry. 2024 Feb 22;67(4):2321-2336. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.3892 mL	6.9461 mL	13.8922 mL	34.7304 mL
	5 mM	0.2778 mL	1.3892 mL	2.7784 mL	6.9461 mL
	10 mM	0.1389 mL	0.6946 mL	1.3892 mL	3.4730 mL
	15 mM	0.0926 mL	0.4631 mL	0.9261 mL	2.3154 mL
	20 mM	0.0695 mL	0.3473 mL	0.6946 mL	1.7365 mL
	25 mM	0.0556 mL	0.2778 mL	0.5557 mL	1.3892 mL
	30 mM	0.0463 mL	0.2315 mL	0.4631 mL	1.1577 mL
	40 mM	0.0347 mL	0.1737 mL	0.3473 mL	0.8683 mL
	50 mM	0.0278 mL	0.1389 mL	0.2778 mL	0.6946 mL
	60 mM	0.0232 mL	0.1158 mL	0.2315 mL	0.5788 mL
	80 mM	0.0174 mL	0.0868 mL	0.1737 mL	0.4341 mL
	100 mM	0.0139 mL	0.0695 mL	0.1389 mL	0.3473 mL

Bioz

Zelebrudomide

2 Cited Publications

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Zelebrudomide

Publications Citing Use of MedChemExpress (MCE) Zelebrudomide

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas IKZF Family

Ver todos los productos específicos de isoformas Interleukin Related