Lazertinib

Synonyms: YH25448,GNS-1480

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.

Lazertinib Chemical Structure

Lazertinib Chemical Structure

CAS: 1903008-80-9

Selleck's Lazertinib has been cited by 4 publications

Purity & Quality Control

Batch: Purity: 99.92%
99.92

Lazertinib Related Products

Signaling Pathway

Choose Selective EGFR Inhibitors

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
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].

Cell Research 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.

In Vivo
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].

Animal Research Animal Models An intracranial tumor growth model (BALB/c nude mice inoculate with H1975-luc cells)
Dosages 10 and 25 mg/kg
Administration --
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05896683 Completed
Healthy
Janssen Research & Development LLC
May 30 2023 Phase 1
NCT05601973 Recruiting
Non Small Cell Lung Cancer
ETOP IBCSG Partners Foundation|Janssen Pharmaceuticals
March 27 2023 Phase 2
NCT05742594 Completed
Healthy
Janssen Research & Development LLC
January 3 2023 Phase 1
NCT05162274 Completed
Healthy Adult Volunteers
Yuhan Corporation
November 30 2021 Phase 1
NCT05112952 Completed
Hepatic Impairment|Healthy
Janssen Research & Development LLC
November 30 2021 Phase 1

Chemical Information & Solubility

Molecular Weight 554.64 Formula

C30H34N8O3

CAS No. 1903008-80-9 SDF --
Smiles CN(C)CC1=CN(N=C1C2=CC=CC=C2)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N5CCOCC5)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 5 mg/mL ( (9.01 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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