A PROTAC that drives BTK degradation
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NX-5948

Item No. 43484

Technical Information
Formal Name
3-[[4-[1-[[1-[6-[[[(3S)-2,6-dioxo-3-piperidinyl]amino]carbonyl]-3-pyridinyl]-4-piperidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-[(3R)-3-(3-methyl-2-oxo-1-imidazolidinyl)-1-piperidinyl]-2-pyrazinecarboxamide
CAS Number
2649400-34-8
Synonyms
  • Bexobrutideg
Molecular Formula
C42H54N12O5
Formula Weight
Purity
≥98%
A crystalline solid
DMSO: Sparingly soluble: 1-10 mg/ml
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=C7)C(N[C@H]8CCC(NC8=O)=O)=O)CC6)C=C4)=O
InChi Code
InChI=1S/C42H54N12O5/c1-50-21-22-54(42(50)59)32-3-2-16-53(26-32)35-24-45-37(38(43)56)39(48-35)46-30-6-4-28(5-7-30)29-14-17-51(18-15-29)25-27-12-19-52(20-13-27)31-8-9-33(44-23-31)40(57)47-34-10-11-36(55)49-41(34)58/h4-9,23-24,27,29,32,34H,2-3,10-22,25-26H2,1H3,(H2,43,56)(H,46,48)(H,47,57)(H,49,55,58)/t32-,34+/m1/s1
InChi Key
HPTPDBYCFHFWJG-CWTKIQHKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    NX-5948 is a proteolysis-targeting chimera (PROTAC) that drives the degradation of Bruton’s tyrosine kinase (BTK).1,2 It induces the degradation of BTK in OCI-LY10 diffuse large B cell lymphoma (DLBCL) cells with a half-maximal degradation concentration (DC50) value of 0.07 nM.2 NX-5948 inhibits the proliferation of wild-type BTK-expressing OCI-LY10 and TMD8 DLBCL cells and mutant BTKC481S-expressing TMD8 cells (IC50s = 0.1, 0.6, and 16 nM, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, F., Sun, W., Ma, Z., et alA validated liquid chromatography-tandem mass spectrometry assay for the determination of NX-5948 in beagle dog plasma: Application to a pharmacokinetic study. Biomed. Chromatogr. 39(3), e6090 (2025).

    2. Ren, J., Huang, Y., Wang, J., et alDiscovery of TQ-3959 as a potent and orally bioavailable BTK PROTAC degrader incorporating a novel benzisoxazole-based CRBN ligand for the treatment of B-cell malignancies. J. Med. Chem. Online ahead of print, (2025).