PRN1008
- Product Name
- PRN1008
- CAS No.
- 1575596-29-0
- Chemical Name
- PRN1008
- Synonyms
- Rilzabrutinib;PRN-1008-E;SAR-444671;Rilzabrutinb;Rilzabrutinib (PRN-1008);Rilzabrutinib, 10 mM in DMSO;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;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)-
- CBNumber
- CB64796680
- Molecular Formula
- C36H40FN9O3
- Formula Weight
- 665.77
- MOL File
- 1575596-29-0.mol
PRN1008 Property
- 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|
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H372Causes damage to organs through prolonged or repeated exposure
- Precautionary statements
-
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P314Get medical advice/attention if you feel unwell.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- CS-0043590
- Product name
- PRN1008
- Purity
- 99.49%
- Packaging
- 5mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0043590
- Product name
- PRN1008
- Purity
- 99.49%
- Packaging
- 10mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0043590
- Product name
- PRN1008
- Purity
- 99.49%
- Packaging
- 25mg
- Price
- $1100
- Updated
- 2021/12/16
- Product number
- CS-0043590
- Product name
- PRN1008
- Purity
- 99.49%
- Packaging
- 50mg
- Price
- $1500
- Updated
- 2021/12/16
- Product number
- CS-0043590
- Product name
- PRN1008
- Purity
- 99.49%
- Packaging
- 100mg
- Price
- $2100
- Updated
- 2021/12/16
PRN1008 Chemical Properties,Usage,Production
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
Raw materials
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View Lastest Price from PRN1008 manufacturers
- Product
- Rilzabrutinib 1575596-29-0
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2025-09-10