2-Pyrazinecarboxamide, 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]- manufacturers
- NX-5948
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- $77.00
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2026-07-27
- CAS:2649400-34-8
- Purity: 98.29%
- Supply Ability: 10g
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| | 2-Pyrazinecarboxamide, 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]- Basic information |
| | 2-Pyrazinecarboxamide, 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]- Chemical Properties |
| Boiling point | 1052.9±65.0 °C(Predicted) | | density | 1.41±0.1 g/cm3(Predicted) | | pka | 10.60±0.40(Predicted) | | form | Solid | | color | Off-white to light yellow | | InChIKey | HPTPDBYCFHFWJG-CWTKIQHKSA-N | | SMILES | C1(C(N)=O)=NC=C(N2CCC[C@@H](N3C(=O)N(C)CC3)C2)N=C1NC1=CC=C(C2CCN(CC3CCN(C4=CC=C(C(N[C@H]5CCC(=O)NC5=O)=O)N=C4)CC3)CC2)C=C1 |
| | 2-Pyrazinecarboxamide, 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]- Usage And Synthesis |
| Uses | 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]. | | 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].
| 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.
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| | IC 50 | Cereblon | | References | [1] Mark Noviski, et al. NX-5948, a Selective Degrader of BTK, Significantly Reduces Inflammation in a Model of Autoimmune Disease. 2021 Nurix Therapeutics, Inc.
[2] 4473 Initial Findings from a First-in-Human Phase 1a/b Trial of NX-5948, a Selective Bruton’s Tyrosine Kinase (BTK) Degrader, in Patients with Relapsed/Refractory B Cell Malignancies. Annual Meeting & Exposition, Monday, December 11, 2023.
[3] Zi Liu, et al. An overview of PROTACs: a promising drug discovery paradigm. Mol Biomed. 2022 Dec 20;3(1):46. DOI:10.1186/s43556-022-00112-0 |
| | 2-Pyrazinecarboxamide, 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]- Preparation Products And Raw materials |
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