Home Protein Tyrosine Kinase EGFR inhibitor - BTK inhibitor Olmutinib (BI 1482694) For research use only.

Olmutinib (BI 1482694)

Synonyms: HM61713

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

Olmutinib (BI 1482694) Chemical Structure

CAS: 1353550-13-6

Selleck's Olmutinib (BI 1482694) has been cited by 5 publications

Purity & Quality Control

Batch: S829401 DMSO] 97 mg/mL] false] Ethanol] 23 mg/mL] false] Water] Insoluble] false Purity: 99.96%
99.96

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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
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
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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02722161 Completed
Healthy
Boehringer Ingelheim
 April 2016 Phase 1
NCT02485652 Terminated
Non Small Cell Lung Cancer
Hanmi Pharmaceutical Company Limited
 August 31 2015 Phase 2
NCT01894399 Completed
Healthy Volunteers
Hanmi Pharmaceutical Company Limited
 September 2013 Phase 1

Chemical Information & Solubility

Molecular Weight 486.59 Formula

C26H26N6O2S
CAS No. 1353550-13-6 SDF Download Olmutinib (BI 1482694) SDF
Smiles CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC4=C(C(=N3)OC5=CC=CC(=C5)NC(=O)C=C)SC=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 97 mg/mL ( (199.34 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 23 mg/mL

Water : Insoluble


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In vivo
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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.
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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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