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
More
Less

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|
More
Less

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..…

More
Less

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
More
Less

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

More
Less

PRN1008 Suppliers

China 57 United States 2 Global 59
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
Advantage
58
Chunchuang (Wuhan) Technology Co., Ltd
Tel
15727060112
Email
yutianchun2007@126.com
Country
China
ProdList
9814
Advantage
58
Taizhou Nanfeng Pharmaceutical Research Institute
Tel
nanfengdrug@163.com; 18616377689
Email
nanfengdrug@163.com
Country
China
ProdList
20009
Advantage
58
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
Tel
17702719238 18971495150;
Email
sales@sun-shinechem.com
Country
China
ProdList
1077
Advantage
64
Sichuan Wei Keqi Biological Technology Co., Ltd.
Tel
028-81700200 18116577057
Fax
028-81705658
Email
3003855609@qq.com
Country
China
ProdList
7778
Advantage
56
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
ChengDu TongChuangYuan Pharmaceutical Co.Ltd
Tel
028-83379370 13880556291
Fax
028-87747383
Email
tcy@tcypharm.com
Country
China
ProdList
7218
Advantage
58
Chuzhou KeMail Chemical Technology Co., Ltd
Tel
0550-5196001 15000891977
Fax
0550-5196001
Email
wj520wjxby@126.com
Country
China
ProdList
1944
Advantage
55
Jinan Kabotang Biological Technology Co.,Ltd.
Tel
0531-61320525 15866703830
Email
figo.gao@foxmail.com
Country
China
ProdList
5178
Advantage
58
Jurong Coupling Biotechnology Co., Ltd.
Tel
19231718652
Email
278191416@qq.com
Country
China
ProdList
482
Advantage
58
More
Less

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