ChemicalBook > CAS DataBase List > PRN1008

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
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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|
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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..…

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0043590
Product name
PRN1008
Purity
99.49%
Packaging
5mg
Price
$350
Updated
2021/12/16
ChemScene
Product number
CS-0043590
Product name
PRN1008
Purity
99.49%
Packaging
10mg
Price
$550
Updated
2021/12/16
ChemScene
Product number
CS-0043590
Product name
PRN1008
Purity
99.49%
Packaging
25mg
Price
$1100
Updated
2021/12/16
ChemScene
Product number
CS-0043590
Product name
PRN1008
Purity
99.49%
Packaging
50mg
Price
$1500
Updated
2021/12/16
ChemScene
Product number
CS-0043590
Product name
PRN1008
Purity
99.49%
Packaging
100mg
Price
$2100
Updated
2021/12/16
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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

Preparation Products

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PRN1008 Suppliers

China 57 United States 2 Global 59
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32435
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354;
Email
support@targetmol.com
Country
United States
ProdList
39035
Advantage
58
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View Lastest Price from PRN1008 manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
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

1575596-29-0, PRN1008Related Search:


  • 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
  • Rilzabrutinib (PRN-1008)
  • 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
  • SAR-444671
  • 1575596-29-0