Lazertinib (YH25448,GNS-1480)

Catalog No.S8724

Lazertinib (YH25448,GNS-1480) Chemical Structure

Molecular Weight(MW): 554.64

Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.

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Biological Activity

Description Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.
Targets
Del19/T790M [1]
(Cell-free assay)
L858R/T790M EGFR [1]
(Cell-free assay)
Del19 [1]
(Cell-free assay)
L85R [1]
(Cell-free assay)
WT EGFR [1]
(Cell-free assay)
1.7 nM 2 nM 5 nM 20.6 nM 76 nM
In vitro

Lazertinib targets the activating EGFR mutations Del19 and L858R, as well as the T790M mutation, while sparing wild type. In NSCLC cell lines and primary cancer cells from patients harboring EGFR mutations, YH25448 more potently inhibits cancer cell growth and significantly increases tumor cell apoptosis compared to osimertinib[1]. In the cell proliferation assays, GI50 values of lazertinib are 6 nM, 5 nM, and 711 nM for H1975 cells (L858R/T790M), PC9 cells (del19) and H2073 cells (wt), respectively[2].

In vivo

In an in vivo mouse model implanted with H1975 cells, once-daily YH25448 treatment results in indramatic dose-dependent tumor regression in both subcutaneous and intracranial lesions with no abnormal signs such as skin keratosis. The plasma half-life of YH25448 is 5.9-6.8 hr, while the tumor to plasma AUC0-last ratio is 3.0-5.1 in tumor-bearing mice. YH25448 shows excellent penetration of the blood-brain bartier, achieving CSF concentrations exceeding the IC50 value for pEGFR inhibition. YH25448 shows superior efficacy for tumor regression in an EGFR mutant brain metastasis model[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: Ba/F3 cells
  • Concentrations: 5, 10, 100 nM
  • Incubation Time: 6 h
  • Method:

    Ba/F3 cells overexpressing the indicated EGFR mutant are treated with YH25448 or osimertinib for 6 hours at the indicated concentrations. pEGFR levels are detected by Western blot analysis.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: An intracranial tumor growth model (BALB/c nude mice inoculate with H1975-luc cells)
  • Formulation: --
  • Dosages: 10 and 25 mg/kg
  • Administration: --
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 4 mg/mL (7.21 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 554.64
Formula

C30H34N8O3

CAS No. 1903008-80-9
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03556436 Completed Non-Small Cell Lung Cancer Yuhan Corporation|Seoul National University Hospital July 3 2018 Phase 1
NCT03556436 Completed Non-Small Cell Lung Cancer Yuhan Corporation|Seoul National University Hospital July 3 2018 Phase 1
NCT03046992 Recruiting EGFR Gene Mutation Yuhan Corporation February 15 2017 Phase 1|Phase 2
NCT03046992 Recruiting EGFR Gene Mutation Yuhan Corporation February 15 2017 Phase 1|Phase 2

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

Tel: +1-832-582-8158 Ext:3

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EGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID