Home Protein Tyrosine Kinase EGFR inhibitor Olmutinib (BI 1482694)

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Olmutinib (BI 1482694) EGFR inhibitor

Cat.No.S8294

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) EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 486.59

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 97 mg/mL (199.34 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 23 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 add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 486.59 Formula

C26H26N6O2S

 Storage (From the date of receipt)
CAS No. 1353550-13-6 Download SDF Storage of Stock Solutions

Synonyms HM61713 Smiles CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC4=C(C(=N3)OC5=CC=CC(=C5)NC(=O)C=C)SC=C4

Mechanism of Action

Targets/IC50/Ki
mutant EGFR
BTK
(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).
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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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