Olmutinib (BI 1482694)

Catalog No.S8294 Synonyms: HM61713

For research use only.

Olmutinib (BI 1482694) is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor (TKI). Also a potent inhibitor of Bruton's tyrosine kinase.

Olmutinib (BI 1482694) Chemical Structure

CAS No. 1353550-13-6

Selleck's Olmutinib (BI 1482694) has been cited by 4 Publications

Purity & Quality Control

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Biological Activity

Description Olmutinib (BI 1482694) is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor (TKI). Also a potent inhibitor of Bruton's tyrosine kinase.
Targets
mutant EGFR [1] BTK [2]
(Cell-free assay)
13.9 nM
In vitro

HM61713 causes potent inhibition in cell lines H1975 (L858R and T790M) and HCC827 (exon 19 deletion). It has a low potency for NSCLC cell line H358 harboring wild-type EGFR (GI50 of 2225 nM)[1].

In vivo HM61713 has a half-life of over 24 h for EGFR inhibition. In the in vivo studies of xenograft models with grafts of H1975 and HCC827, HM61713 is active against the tumors without showing any side effects[1].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 97 mg/mL
(199.34 mM)
Ethanol 23 mg/mL
(47.26 mM)
Water Insoluble

Chemical Information

Molecular Weight 486.59
Formula

C26H26N6O2S

CAS No. 1353550-13-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC4=C(C(=N3)OC5=CC=CC(=C5)NC(=O)C=C)SC=C4

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02722161 Completed Drug: [14C]BI 1482694 Healthy Boehringer Ingelheim April 2016 Phase 1
NCT02485652 Terminated Drug: HM61713 Non Small Cell Lung Cancer Hanmi Pharmaceutical Company Limited August 31 2015 Phase 2
NCT01894399 Completed Drug: HM61713 Healthy Volunteers Hanmi Pharmaceutical Company Limited September 2013 Phase 1

(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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