2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. NX-2127

NX-2127 is an orally and potent BTK inhibitor, inducing degradation of the mutated BTKC481S in cells. NX-2127 inhibits proliferation of BTKC481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells.

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

NX-2127 Chemical Structure

NX-2127 Chemical Structure

CAS No. : 2416131-46-7

Size Price Stock Quantity
5 mg USD 330 In-stock
10 mg USD 520 In-stock
25 mg USD 1040 In-stock
50 mg USD 1660 In-stock
100 mg USD 2650 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of NX-2127:

NX-2127 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

NX-2127 is an orally and potent BTK inhibitor, inducing degradation of the mutated BTKC481S in cells. NX-2127 inhibits proliferation of BTKC481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells[1][2].

In Vitro

NX-2127 inhibits proliferation of BTK-C481S mutant TMD8 cells with an EC50 value <30 nM[1].
NX-2127 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.

NX-2127 Related Antibodies
In Vivo

NX-2127 (1 mg/kg; po; once daily for 14 days) demonstrates potent degradation of BTK in cynomolgus monkeys in vivo[1].
NX-2127 (po) leads to dose-proportional exposure in plasma and BTK degradation to <10% of baseline levels in circulating and splenic B cells[1].
NX-2127 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.
Clinical Trial
Molecular Weight

719.83

Formula

C39H45N9O5
CAS No.
Appearance

Solid

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
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)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3892 mL 6.9461 mL 13.8922 mL
5 mM 0.2778 mL 1.3892 mL 2.7784 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 (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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.72%

COA (251 KB) HNMR (338 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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 (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.

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

NX-2127 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:

NX-21272416131-46-7NX2127NX 2127BtkBruton tyrosine kinaseBTK-C481S mutantTMD8 cellsIL-2primary human T Cellscynomolgus monkeysWT TMD8 xenograft modelsC481S mutant xenograft modelsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
NX-2127
Cat. No.:
HY-153220
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.