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]-
![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]- Structure](CAS/20210305/GIF/2649400-34-8.gif)
- CAS No.
- 2649400-34-8
- Chemical Name:
- 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]-
- Synonyms
- NX-5948;Bexobrutideg;BTK-IN-24;BTK-IN-24(NX-5948);NX 5948 New;3-[[4-[1-[[1-[6-[[(S)-2,6-Dioxo-3-piperidyl]carbamoyl]-3-pyridyl]-4-piperidyl]methyl]-4-piperidyl]phenyl]amino]-5-[(R)-3-(3-methyl-2-oxoimidazolidin-1-yl)-1-piperidyl]pyrazine-2-carboxamide;3-((4-(1-((1-(6-(((S)-2,6-dioxopiperidin-3-yl)carbamoyl)pyridin-3-yl)piperidin-4-yl)methyl)piperidin-4-yl)phenyl)amino)-5-((R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl)pyrazine-2-carboxamide;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;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]-
- CBNumber:
- CB713138317
- Molecular Formula:
- C42H54N12O5
- Molecular Weight:
- 806.96
- MDL Number:
- MOL File:
- 2649400-34-8.mol
- MSDS File:
- SDS
- TDS File:
- TDS
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]- 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 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319 |
| Precautionary statements | P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330 |
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]- price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 43484 | NX-5948 ≥98% | 2649400-34-8 | 1mg | $44 | 2026-04-30 | Buy |
| Cayman Chemical | 43484 | NX-5948 ≥98% | 2649400-34-8 | 5mg | $209 | 2026-04-30 | Buy |
| Cayman Chemical | 43484 | NX-5948 ≥98% | 2649400-34-8 | 10mg | $308 | 2026-04-30 | Buy |
| Cayman Chemical | 43484 | NX-5948 ≥98% | 2649400-34-8 | 25mg | $550 | 2026-04-30 | Buy |
| ChemScene | CS-0676328 | Bexobrutideg ≥98% | 2649400-34-8 | 50mg | $539 | 2026-06-04 | Buy |
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, Uses, Production
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. |
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
Raw materials
Preparation Products
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]- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai XingMo Biotechnology Co., Ltd. | +86 13524779951; 13524779951 | 2075692521@qq.com | China | 294 | 55 |
| WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd. | 17702719238 | sales@sun-shinechem.com | China | 1197 | 64 |
| Shanghai Hope Chem Co., Ltd.， | +21-18501659228 18501659228 | info@hope-chem.com | China | 538 | 55 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4860 | 55 | |
| Shanghai Beckham Medical Technology Co., Ltd | 13816613772 | huahero21@sina.com | China | 2996 | 55 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9799 | 58 |
| Chengdu Novel Biomedical Co., Ltd. | 028-85255396 18302801538 | cdnovell@163.com | China | 2444 | 58 |
| Lanzhou Kangyuxin Biotechnology Co., Ltd. | 0943-8293106 | sales@kyxpharma.com | China | 3552 | 58 |
| Chunchuang (Wuhan) Technology Co., Ltd | 15727060112 | yutianchun2007@126.com | China | 9867 | 58 |
| Bide Pharmatech Ltd. | 400-1647117 13681763483 | product02@bidepharm.com | China | 59929 | 58 |
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2649400-34-8 (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]-) Related Search:
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