Home Angiogenesis BTK inhibitor Orelabrutinib For research use only.

Orelabrutinib

Synonyms: ICP-022

Orelabrutinib is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK). Orelabrutinib has potential antineoplastic activity.

Orelabrutinib Chemical Structure

Orelabrutinib Chemical Structure

CAS No. 1655504-04-3

Purity & Quality Control

Batch: S960001 DMSO]86 mg/mL]false]Ethanol]10 mg/mL]false]Water]Insoluble]false Purity: 99.95%
99.95

Orelabrutinib Related Products

Signaling Pathway

BTK Signaling Pathways

BTK Signaling Pathway

Biological Activity

Description Orelabrutinib is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK). Orelabrutinib has potential antineoplastic activity.
Targets
BTK [1]
In vitro
In vitro

Orelabrutinib potently inhibits BTK enzymatic activity with an IC50 value of 1.6 nM. In KINOMEscan assay conducted in parallel at 1 μM against a panel of 456 kinases, orelabrutinib only targets BTK with > 90% inhibition while ibrutinib inhibits additional many other kinases including EGFR, TEC and BMX, demonstrating orelabrutinib's superior kinase selectivity.[2]
In Vivo
In vivo

Orelabrutinib has a favorable PK profile with an ideal T1/2 (~1.5-4 h) and good oral bioavailability (~20-80%) as well as prolonged BTK target occupancy in preclinical PK/PD studies. The superior selectivity translates into improved safety profile and large safety window in the GLP toxicology studies in rats and dogs.[2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05491044 Recruiting
CLL/SLL
Peking University People''s Hospital
 January 1 2022 Phase 2
NCT05021770 Not yet recruiting
Refractory and Relapsed Primary CNS Lymphoma|PCNSL|Non Hodgkin Lymphoma
Huiqiang Huang|Guangdong 999 Brain Hospital|Sun Yat-sen University
 December 2021 Phase 1|Phase 2
NCT05020288 Not yet recruiting
Immune Thrombocytopenia|Bruton''s Tyrosine Kinase
Shandong University
 September 1 2021 Phase 2
NCT04441450 Completed
Healthy Volunteers
Beijing InnoCare Pharma Tech Co. Ltd.
 July 1 2019 Not Applicable

Chemical Information & Solubility

Molecular Weight 427.49 Formula

C26H25N3O3
CAS No. 1655504-04-3 SDF --
Smiles C=CC(=O)N1CCC(CC1)C2=NC(=C(C=C2)C(=O)N)C3=CC=C(C=C3)OC4=CC=CC=C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 86 mg/mL ( (201.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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