Referencia número: HY-153220

Zelebrudomide

(Synonyms: NX-2127)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Zelebrudomide (NX-2127) (Compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk). Zelebrudomide inhibits proliferation of BTK^C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). Zelebrudomide catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. Zelebrudomide stimulates T cell activation and increases IL-2 production in primary human T Cells. (Pink: BTK ligand 10 (HY-168302); Black: (R)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168348); Blue: Thalidomide 5-fluoride (HY-W087383)
(Pink: Btk ligand (HY-168302); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-168303)).

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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Actividad biológica
- Descripciòn
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (1)
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
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Actividad biológica

Descripciòn

Zelebrudomide (NX-2127) (Compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk). Zelebrudomide inhibits proliferation of BTK^C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). Zelebrudomide catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. Zelebrudomide stimulates T cell activation and increases IL-2 production in primary human T Cells^[1]^[2]. (Pink: BTK ligand 10 (HY-168302); Black: (R)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168348); Blue: Thalidomide 5-fluoride (HY-W087383) (Pink: Btk ligand (HY-168302); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-168303)).

Ver todos los productos específicos de isoformas PROTACs :

In Vitro

Zelebrudomide (NX-2127) inhibits proliferation of BTK-C481S mutant TMD8 cells with an EC₅₀ value <30 nM^[1].
Zelebrudomide increases IL-2 production in primary human T Cells^[1].

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

In Vivo

Zelebrudomide (NX-2127) (1 mg/kg; po; once daily for 14 days) demonstrates potent degradation of BTK in cynomolgus monkeys in vivo^[1].
Zelebrudomide (po) leads to dose-proportional exposure in plasma and BTK degradation to <10% of baseline levels in circulating and splenic B cells^[1].
Zelebrudomide results in superior tumor growth inhibition (TGI) in both WT TMD8 and C481S mutant xenograft models in mouse^[1].

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

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		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 (1)

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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

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

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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)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (273 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 D W, et al. Nx-2127, a degrader of BTK and IMiD neosubstrates, for the treatment of B-cell malignancies. Blood, 2020, 136: 34.

[2]. Mato A, et al. A first-in-human phase 1 trial of NX-2127, a first-in-class oral BTK degrader with IMiD-like activity, in patients with relapsed and refractory B-cell malignancies. 2022.

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

Keywords

Zelebrudomide

1 Cited Publications

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Zelebrudomide

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

PROTAC Library

Autoimmune Disease Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

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Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Zelebrudomide

Ver todos los productos específicos de isoformas PROTACs

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Zelebrudomide

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

PROTAC Library

Autoimmune Disease Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Zelebrudomide

Ver todos los productos específicos de isoformas PROTACs

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Zelebrudomide Related Classifications

HY-153220 Related Classifications