2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. NRX-0492

NRX-0492 is an orally active and potent degrader of BTK. NRX-0492 catalyzes ubiquitylation and proteasomal degradation of BTK with DC50≤0.2 nM and DC90≤0.5 nM, respectively. NRX-0492 inhibits B-cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion. Moreover, NRX-0492 also links a noncovalent BTK-binding domain to Cereblon. Cereblon is an adaptor protein of the E3 ubiquitin ligase complex.

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NRX-0492 Chemical Structure

NRX-0492 Chemical Structure

CAS No. : 2416130-57-7

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1 mg USD 213 In-stock
5 mg USD 468 In-stock
10 mg USD 750 In-stock
25 mg USD 1500 In-stock
50 mg USD 2400 In-stock
100 mg USD 3840 In-stock
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Based on 1 publication(s) in Google Scholar

NRX-0492 Related Antibodies

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Description

NRX-0492 is an orally active and potent degrader of BTK. NRX-0492 catalyzes ubiquitylation and proteasomal degradation of BTK with DC50≤0.2 nM and DC90≤0.5 nM, respectively. NRX-0492 inhibits B-cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion. Moreover, NRX-0492 also links a noncovalent BTK-binding domain to Cereblon. Cereblon is an adaptor protein of the E3 ubiquitin ligase complex[1].

Molecular Weight

817.94

Formula

C43H51N11O6
CAS No.
Appearance

Solid

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
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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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2226 mL 6.1129 mL 12.2258 mL
5 mM 0.2445 mL 1.2226 mL 2.4452 mL
View the Complete Stock Solution Preparation Table

* 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.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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NRX-0492 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NRX-04922416130-57-7NRX0492NRX 0492BtkBruton tyrosine kinaseorally activeubiquitylationproteasomalB-cell receptor (BCR)-mediated signalingCereblonE3 ubiquitin ligase complexInhibitorinhibitorinhibit

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