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Cat. No.: HY-153357

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NRX-0492

고객리뷰

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)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 98.30%
CAS No.: 2416130-57-7
화학식: C₄₃H₅₁N₁₁O₆
분자량:817.94

보관:

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

사이즈

가격

재고

수량

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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
분자량 817.94
화학식 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
선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

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

견적 받기 해외재고보유

Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
용액&용해도
- In Vitro
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
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수량:

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

용액&용해도

순도&문서

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

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

NRX-0492 Related Classifications

HY-153357 Related Classifications