Orelabrutinib (ICP-022)

Catalog No.S9600

For research use only.

Orelabrutinib (ICP-022) is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK). Orelabrutinib has potential antineoplastic activity.

Orelabrutinib (ICP-022) Chemical Structure

CAS No. 1655504-04-3

Purity & Quality Control

Choose Selective BTK Inhibitors

Biological Activity

Description Orelabrutinib (ICP-022) is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK). Orelabrutinib has potential antineoplastic activity.
Targets
BTK [1]
()
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

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]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 86 mg/mL
(201.17 mM)
Water Insoluble
Ethanol '10 mg/mL

Chemical Information

Molecular Weight 427.49
Formula

C26H25N3O3

CAS No. 1655504-04-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C=CC(=O)N1CCC(CC1)C2=NC(=C(C=C2)C(=O)N)C3=CC=C(C=C3)OC4=CC=CC=C4

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05021770 Not yet recruiting Drug: Orelabrutinib|Drug: Thiotepa 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 Drug: Orelabrutinib Immune Thrombocytopenia|Bruton''s Tyrosine Kinase Shandong University September 1 2021 Phase 2
NCT04441450 Completed Drug: [14C]ICP-022 Healthy Volunteers Beijing InnoCare Pharma Tech Co. Ltd. July 1 2019 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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