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Cat. No.: HY-153357

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NRX-0492

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Based on 1 Customer Validation

NRX-0492 is an orally active PROTAC-class BTK degrader. NRX-0492 catalyzes BTK ubiquitination and proteasome degradation (DC₅₀ ≤ 0.2 nM, DC₉₀ ≤ 0.5 nM). NRX-0492 inhibits B cell receptor (BCR) mediated signaling, transcription programs, and chemokine secretion. NRX-0492 has antitumor effects against chronic lymphocytic leukemia.NRX-0492 consists of a target protein ligand (red part) BTK-IN-40 (HY-170324), an E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383), and a PROTAC linker (black part) (3R)-3-Pyrrolidinemethanol (HY-60263).
(Pink: Btk ligand (HY-49421); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-60263)).

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

Purity: 98.30%
CAS No.: 2416130-57-7
Formula: C₄₃H₅₁N₁₁O₆
Molecular Weight:817.94

Storage:

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

NRX-0492 Chemical Structure

CAS No.: 2416130-57-7

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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
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

NRX-0492 is an orally active PROTAC-class BTK degrader. NRX-0492 catalyzes BTK ubiquitination and proteasome degradation (DC₅₀ ≤ 0.2 nM, DC₉₀ ≤ 0.5 nM). NRX-0492 inhibits B cell receptor (BCR) mediated signaling, transcription programs, and chemokine secretion. NRX-0492 has antitumor effects against chronic lymphocytic leukemia.NRX-0492 consists of a target protein ligand (red part) BTK-IN-40 (HY-170324), an E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383), and a PROTAC linker (black part) (3R)-3-Pyrrolidinemethanol (HY-60263). (Pink: Btk ligand (HY-49421); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-60263)).

IC₅₀ & Target

IC₅₀ values of 1.2 nM (wild-type BTK), 2.7 nM (C481S mutant BTK), and 1.2 nM (T474I mutant BTK)

All PROTACs Isoforms :

In Vitro

NRX-0492 shows high-affinity binding to wild-type and C481S/T474I mutant BTK with IC₅₀ values of 1.2 nM, 2.7 nM, and 1.2 nM, respectively^[1].
NRX-0492 (0.05-4 nM; 4 h) induces degradation of both wild-type and C481S mutant BTK in TMD8 cells, with DC₅₀ ≤0.2 nM and DC₉₀ ≤0.5 nM^[1].

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

In Vivo

NRX-0492 (30 mg/kg; p,o,; single or continuous dosing) induces BTK degradation in CLL cells from blood and spleen, reduces the proportion of Ki67⁺/CD69⁺ cells, and decreases splenic tumor burden in NOD/SCID/IL2Rγ^-/- (NSG) mice with CLL patient-derived xenografts^[1].

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

Chemical Information

CAS No. 2416130-57-7
Appearance Solid
Molecular Weight 817.94
Formula C₄₃H₅₁N₁₁O₆
Color Light yellow to yellow
SMILES

NC(C1=C(N=C(N2CCC[C@@H](N3CCN(C)C3=O)C2)C=N1)NC(C=C4)=CC=C4C(CC5)CCN5C[C@@H](C6)CCN6C7=CC=C(C(C(N8C9C(NC(CC9)=O)=O)=O)=C7)C8=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL (244.52 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

1.2226 mL

6.1129 mL

12.2258 mL

5 mM

0.2445 mL

1.2226 mL

2.4452 mL

10 mM

0.1223 mL

0.6113 mL

1.2226 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.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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]. Zhang D, et al. NRX-0492 degrades wild-type and C481 mutant BTK and demonstrates in vivo activity in CLL patient-derived xenografts. Blood. 2023 Mar 30;141(13):1584-1596. [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	1.2226 mL	6.1129 mL	12.2258 mL	30.5646 mL
	5 mM	0.2445 mL	1.2226 mL	2.4452 mL	6.1129 mL
	10 mM	0.1223 mL	0.6113 mL	1.2226 mL	3.0565 mL
	15 mM	0.0815 mL	0.4075 mL	0.8151 mL	2.0376 mL
	20 mM	0.0611 mL	0.3056 mL	0.6113 mL	1.5282 mL
	25 mM	0.0489 mL	0.2445 mL	0.4890 mL	1.2226 mL
	30 mM	0.0408 mL	0.2038 mL	0.4075 mL	1.0188 mL
	40 mM	0.0306 mL	0.1528 mL	0.3056 mL	0.7641 mL
	50 mM	0.0245 mL	0.1223 mL	0.2445 mL	0.6113 mL
	60 mM	0.0204 mL	0.1019 mL	0.2038 mL	0.5094 mL
	80 mM	0.0153 mL	0.0764 mL	0.1528 mL	0.3821 mL
	100 mM	0.0122 mL	0.0611 mL	0.1223 mL	0.3056 mL

Keywords

100 mg

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

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

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NRX-0492

Immunology/Inflammation Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

PROTAC Library

Autoimmune Disease Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

All PROTACs Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

NRX-0492

Immunology/Inflammation Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

PROTAC Library

Autoimmune Disease Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

All PROTACs Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

NRX-0492 Related Classifications

Cat. No.: HY-153357