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MedKoo Cat#: 462574 | Name: Rilzabrutinib
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Rilzabrutinib, also known as PRN1008, is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK).

Chemical Structure

Rilzabrutinib
Rilzabrutinib
CAS#1575596-29-0

Theoretical Analysis

MedKoo Cat#: 462574

Name: Rilzabrutinib

CAS#: 1575596-29-0

Chemical Formula: C36H40FN9O3

Exact Mass: 665.3238

Molecular Weight: 665.77

Elemental Analysis: C, 64.95; H, 6.06; F, 2.85; N, 18.93; O, 7.21

Price and Availability

Size Price Availability Quantity
25mg USD 550.00 2 Weeks
50mg USD 950.00 2 Weeks
100mg USD 1,650.00 2 Weeks
1g USD 4,850.00 2 Weeks
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Related CAS #
No Data
Synonym
PRN1008; PRN 1008; PRN-1008; Rilzabrutinib;
IUPAC/Chemical Name
(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
InChi Key
LCFFREMLXLZNHE-GBOLQPHISA-N
InChi Code
InChI=1S/C36H40FN9O3/c1-36(2,45-15-13-43(14-16-45)26-21-48-22-26)18-24(19-38)35(47)44-12-6-7-25(20-44)46-34-31(33(39)40-23-41-34)32(42-46)29-11-10-28(17-30(29)37)49-27-8-4-3-5-9-27/h3-5,8-11,17-18,23,25-26H,6-7,12-16,20-22H2,1-2H3,(H2,39,40,41)/b24-18+/t25-/m1/s1
SMILES Code
NC1=C2C(C3=C(C=C(OC4=CC=CC=C4)C=C3)F)=NN([C@H]5CN(CCC5)C(/C(C#N)=C/C(C)(N6CCN(C7COC7)CC6)C)=O)C2=NC=N1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO and ethanol
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO and ethanol
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Rilzabrutinib has an an IC50 of 1.3 nM.
In vitro activity:
Rilzabrutinib inhibited Btk-dependent pathways of platelet aggregation upon GPVI, VWF/GPIb, and FcγRIIA activation. It is less potent than remibrutinib but still has antiplatelet activity. Reference: Front Cardiovasc Med. 2021 Sep 24;8:749022. https://pubmed.ncbi.nlm.nih.gov/34631841/
In vivo activity:
PRN1008 monotherapy may have some beneficial effects in some cases of canine pemphigus foliaceus. All four dogs showed reduction in lesions and a decrease in their canine Pemphigus Disease Activity Index score during the first two weeks of rilzabrutinib treatment. Three dogs continued to improve and sustained near complete remission by 20 weeks. Reference: Vet Dermatol. 2020 Oct;31(5):410-e110. https://pubmed.ncbi.nlm.nih.gov/32803903/
Solvent mg/mL mM
Solubility
DMSO 100.0 150.20
Ethanol 100.0 150.20
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 665.77 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Duan R, Goldmann L, Brandl R, Spannagl M, Weber C, Siess W, von Hundelshausen P. Effects of the Btk-Inhibitors Remibrutinib (LOU064) and Rilzabrutinib (PRN1008) With Varying Btk Selectivity Over Tec on Platelet Aggregation and in vitro Bleeding Time. Front Cardiovasc Med. 2021 Sep 24;8:749022. doi: 10.3389/fcvm.2021.749022. PMID: 34631841; PMCID: PMC8498029. 2. Goodale EC, White SD, Bizikova P, Borjesson D, Murrell DF, Bisconte A, Francesco M, Hill RJ, Masjedizadeh M, Nunn P, Gourlay SG, Jordan TJM, Emery CB, Outerbridge CA. Open trial of Bruton's tyrosine kinase inhibitor (PRN1008) in the treatment of canine pemphigus foliaceus. Vet Dermatol. 2020 Oct;31(5):410-e110. doi: 10.1111/vde.12878. Epub 2020 Aug 17. PMID: 32803903. 3. Smith PF, Krishnarajah J, Nunn PA, Hill RJ, Karr D, Tam D, Masjedizadeh M, Funk JO, Gourlay SG. 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. Epub 2017 Aug 1. PMID: 28636208; PMCID: PMC5651318.
In vitro protocol:
1. Duan R, Goldmann L, Brandl R, Spannagl M, Weber C, Siess W, von Hundelshausen P. Effects of the Btk-Inhibitors Remibrutinib (LOU064) and Rilzabrutinib (PRN1008) With Varying Btk Selectivity Over Tec on Platelet Aggregation and in vitro Bleeding Time. Front Cardiovasc Med. 2021 Sep 24;8:749022. doi: 10.3389/fcvm.2021.749022. PMID: 34631841; PMCID: PMC8498029.
In vivo protocol:
1. Goodale EC, White SD, Bizikova P, Borjesson D, Murrell DF, Bisconte A, Francesco M, Hill RJ, Masjedizadeh M, Nunn P, Gourlay SG, Jordan TJM, Emery CB, Outerbridge CA. Open trial of Bruton's tyrosine kinase inhibitor (PRN1008) in the treatment of canine pemphigus foliaceus. Vet Dermatol. 2020 Oct;31(5):410-e110. doi: 10.1111/vde.12878. Epub 2020 Aug 17. PMID: 32803903. 2. Smith PF, Krishnarajah J, Nunn PA, Hill RJ, Karr D, Tam D, Masjedizadeh M, Funk JO, Gourlay SG. 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. Epub 2017 Aug 1. PMID: 28636208; PMCID: PMC5651318.
1: Smith PF, Krishnarajah J, Nunn PA, 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;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.