2. Protein Tyrosine Kinase/RTK PROTAC
  3. Btk PROTACs
  4. NX-5948

NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker).

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NX-5948 Chemical Structure

NX-5948 Chemical Structure

CAS No. : 2649400-34-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1438 Get quote
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10 mM * 1 mL in DMSO USD 1438 Get quote
Solid
1 mg USD 460 In-stock
5 mg USD 1012 Get quote
10 mg USD 1620 Get quote
25 mg USD 3240 Get quote
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Based on 1 publication(s) in Google Scholar

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Description

NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker)[1][2][3].

IC50 & Target[1][2]

Cereblon

 

In Vitro

NX-5948 (BTK-IN-24; 0.0001-1000 nM; 4 h) is a potent degrader of BTK in primary human B cells (DC50=0.34 nM) and inhibits BCR signaling[1]. NX-5948 induces the degradation of BTK (DC50< 1 nM) in lymphoma cell lines and PBMCs[3].
NX-5948 (10 nM; 0.25, 0.5, 1, 2, 4, 6, 18, 24 h) catalyzes rapid BTK degradation within 1 hour and is complete within 2 hours in Ramos cells[1].

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

NX-5948 Related Antibodies
In Vivo

NX-5948 (BTK-IN-24; 10, 30 mg/kg; po; daily; Day 18 to 36) is efficacious and well-tolerated in a mouse collagen-induced arthritis (CIA) model and suppresses antibody titers and IL-6 cytokine levels[1].
NX-5948 (3, 10, 30 mg/kg; po) causes dose- and time-dependent reduction in BTK levels in circulating murine and non-human primate, cynomolgus monkey B cells[1].

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

Animal Model: Mouse collagen-induced arthritis (CIA) model[1]
Dosage: 10, 30 mg/kg
Administration: PO; daily; Day 18 to 36
Result: Showed efficacious and well-tolerated in a mouse CIA model.
Molecular Weight

806.96

Formula

C42H54N12O5
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

NC(C1=C(N=C(N2C[C@H](N3C(N(CC3)C)=O)CCC2)C=N1)NC4=CC=C(C5CCN(CC5)CC6CCN(C7=CN=C(C(N[C@@H]8C(NC(CC8)=O)=O)=O)C=C7)CC6)C=C4)=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 : 50 mg/mL (61.96 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 1.2392 mL 6.1961 mL 12.3922 mL
5 mM 0.2478 mL 1.2392 mL 2.4784 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.33 mg/mL (4.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3.33 mg/mL (4.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 1.2392 mL 6.1961 mL 12.3922 mL 30.9805 mL
5 mM 0.2478 mL 1.2392 mL 2.4784 mL 6.1961 mL
10 mM 0.1239 mL 0.6196 mL 1.2392 mL 3.0980 mL
15 mM 0.0826 mL 0.4131 mL 0.8261 mL 2.0654 mL
20 mM 0.0620 mL 0.3098 mL 0.6196 mL 1.5490 mL
25 mM 0.0496 mL 0.2478 mL 0.4957 mL 1.2392 mL
30 mM 0.0413 mL 0.2065 mL 0.4131 mL 1.0327 mL
40 mM 0.0310 mL 0.1549 mL 0.3098 mL 0.7745 mL
50 mM 0.0248 mL 0.1239 mL 0.2478 mL 0.6196 mL
60 mM 0.0207 mL 0.1033 mL 0.2065 mL 0.5163 mL
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NX-5948 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-59482649400-34-8BTK-IN-24NX5948NX 5948BtkPROTACsBruton tyrosine kinaseOrallychimeric targeting moleculeCTMcereblon E3 ligaseCRBNB cellTMD8BTKicollageninduced arthritisCIAInhibitorinhibitorinhibit

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