country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-153220A

Copy Link Print Information

(R)-Zelebrudomide

(Synonyms: (R)-NX-2127)

Customer Review

Based on 1 Customer Validation

(R)-Zelebrudomide ((R)-NX-2127) is an isomer of Zelebrudomide (HY-153220). 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)).

For research use only. We do not sell to patients.

Purity: 98.93%
CAS No.: 3024312-52-2
Formula: C₃₉H₄₅N₉O₅
Molecular Weight:719.83

Storage:

4°C, protect from light

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

(R)-Zelebrudomide Chemical Structure

CAS No.: 3024312-52-2

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

(R)-Zelebrudomide ((R)-NX-2127) is an isomer of Zelebrudomide (HY-153220). 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

All PROTACs Isoforms :

All IKZF Family Isoforms :

All Interleukin Related Isoforms :

In Vitro

(R)-Zelebrudomide ((R)-NX-2127) is an isomer of Zelebrudomide (HY-153220). Zelebrudomide (NX-2127) 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^[1].
(R)-Zelebrudomide is an isomer of Zelebrudomide. Zelebrudomide (50 nM; 4 h) selectively degrades BTK in human peripheral blood mononuclear cells (PBMCs) from normal donors^[1].
(R)-Zelebrudomide is an isomer of Zelebrudomide. 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

(R)-Zelebrudomide ((R)-NX-2127) is an isomer of Zelebrudomide (HY-153220). Zelebrudomide (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].
(R)-Zelebrudomide is an isomer of Zelebrudomide. 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].
(R)-Zelebrudomide is an isomer of Zelebrudomide. Zelebrudomide (10-90 mg/kg; p.o.; daily administration for 5 consecutive days, daily administration for 25 consecutive days) induces dose-dependent anti-tumor efficacy in TMD8 BTK^WT xenograft tumors and degrades BTK, IKZF1 and IKZF3^[1].
(R)-Zelebrudomide is an isomer of Zelebrudomide. Zelebrudomide (10-90 mg/kg; p.o.; daily administration for 25 days) exerts 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.

Chemical Information

CAS No. 3024312-52-2
Appearance Solid
Molecular Weight 719.83
Formula 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

(R)-NX-2127
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 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)

References

[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]

Calculators

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote

Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

(R)-Zelebrudomide

Immunology/Inflammation Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

PROTAC Library

Autoimmune Disease Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

All PROTACs Isoforms

All IKZF Family Isoforms

All Interleukin Related Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

(R)-Zelebrudomide

Immunology/Inflammation Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

PROTAC Library

Autoimmune Disease Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

All PROTACs Isoforms

All IKZF Family Isoforms

All Interleukin Related Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

(R)-Zelebrudomide Related Classifications

HY-153220A Related Classifications