PRN1008 manufacturers
- Rilzabrutinib
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- $100.00 / 1mg
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2025-09-22
- CAS:1575596-29-0
- Min. Order:
- Purity: 99.76%
- Supply Ability: 10g
- Rilzabrutinib
-
- $100.00 / 1mg
-
2025-09-22
- CAS:1575596-29-0
- Min. Order:
- Purity: 99.76%
- Supply Ability: 10g
- Rilzabrutinib
-
- $0.00 / 1g
-
2025-09-11
- CAS:1575596-29-0
- Min. Order: 1g
- Purity: More Than 99%
- Supply Ability: 100kg/Month
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| | PRN1008 Basic information |
| Product Name: | PRN1008 | | Synonyms: | PRN-1008-E;1-Piperidinepropanenitrile, 3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-α-[2-methyl-2-[4-(3-oxetanyl)-1-piperazinyl]propylidene]-β-oxo-, (αE,3R)-;Rilzabrutinib (PRN-1008);Rilzabrutinib;PRN-1008,inhibit,Rilzabrutinib,PRN 1008,Inhibitor,Btk,Bruton tyrosine kinase;(R,E)-2-(3-(4-amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carbonyl)-4-methyl-4-(4-(oxetan-3-yl)piperazin-1-yl)pent-2-enenitrile;Rilzabrutinib, 10 mM in DMSO;Rilzabrutinb | | CAS: | 1575596-29-0 | | MF: | C36H40FN9O3 | | MW: | 665.77 | | EINECS: | | | Product Categories: | | | Mol File: | 1575596-29-0.mol |  |
| | PRN1008 Chemical Properties |
| Boiling point | 882.5±65.0 °C(Predicted) | | density | 1.39±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO:120.0(Max Conc. mg/mL);180.24(Max Conc. mM) | | form | Solid | | pka | 6.24±0.70(Predicted) | | color | White to off-white | | InChIKey | LCFFREMLXLZNHE-CNPRKNKUNA-N | | SMILES | NC1N=CN=C2N([C@@H]3CCCN(C(=O)/C(/C#N)=C/C(N4CCN(C5COC5)CC4)(C)C)C3)N=C(C3C=CC(OC4C=CC=CC=4)=CC=3F)C=12 |&1:7,r| |
| | PRN1008 Usage And Synthesis |
| Uses | Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM. | | in vivo | In vivo Rilzabrutinib demonstrates enduring pharmacodynamic effects after the compound has cleared from circulation, consistent with extended target residence time. Rilzabrutinib also reverses and completely suppresses collagen-induced arthritis in rats in a dose dependent manner which allows correlation of target occupancy and disease modification[2]. | | IC 50 | BTK: 1.3 nM (IC50); BMX: 1.0 nM (IC50); ITK: 440 nM (IC50); TEC: 0.8 nM (IC50); RLK: 1.2 nM (IC50); BLK: 6.3 nM (IC50); EGFR: 520 nM (IC50); ERBB2: 3900 nM (IC50); ERBB4: 11.3 nM (IC50) | | References | [1] Smith PF, et al. A phase I trial of PRN1008, a novel reversible covalent inhibitor of Bruton's tyrosine kinase, in healthy volunteers. Br J Clin Pharmacol. 2017 Nov;83(11):2367-2376. DOI:10.1111/bcp.13351
[2] Hill RJ, Bradshaw JM, Bisconte A, Tam D, Owens TD, Brameld KA, Smith PF, Funk JO, Goldstein DM, Nunn PA. Preclinical Characterization of PRN1008, a Novel Reversible Covalent Inhibitor of BTK that Shows Efficacy in a RAT Model of Collagen-Induced Arthritis. Annals of the Rheumatic Diseases 2015; 74(Suppl 2): 216. |
| | PRN1008 Preparation Products And Raw materials |
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