Lazertinib

SKU: orb1689983

Description

Lazertinib (GNS-1480) is a potent, irreversible, and mutant-selective EGFR tyrosine kinase inhibitor. It demonstrates high potency against oncogenic EGFR mutants, particularly Del19/T790M and L858R/T790M, with significantly lower activity against wild-type EGFR. This profile supports its research use in vitro and in vivo for studying resistance mechanisms and targeted therapies in non-small cell lung cancer.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1903008-80-9
• MW: 554.64
• Purity: 99.96% (May vary between batches)
• Formula: C₃₀H₃₄N₈O₃
• SMILES: COc1cc(N2CCOCC2)c(NC(=O)C=C)cc1Nc1nccc(n1)-n1cc(CN(C)C)c(n1)-c1ccccc1
• Target: EGFR
• Solubility: H2O:Insoluble;DMSO:6 mg/mL (10.82 mM);Ethanol:Insoluble

Bioactivity

• Target IC50:
  EGFR (WT):76 nM|EGFR (L858R/T790M):2 nM|L85R:20.6 nM|Del19/T790M:1.7 nM|Del19:5 nM
• In Vivo:
  In an in vivo mouse model implanted with H1975 cells, once-daily Lazertinib treatment results in dramatic dose-dependent tumour regression in both subcutaneous and intracranial lesions with no abnormal signs such as skin keratosis. The plasma half-life of Lazertinib is 5.9-6.8 hr, while a tumour to plasma AUC0-last ratio is 3.0-5.1 in tumour-bearing mice. Lazertinib shows excellent penetration of the blood-brain barrier, achieving CSF concentrations exceeding the IC50 value for pEGFR inhibition. Lazertinib shows superior efficacy for tumour regression in an EGFR mutant brain metastasis model.
• In Vitro:
  In NSCLC cell lines and primary cancer cells from patients harbouring EGFR mutations, YH25448 more potently inhibits cancer cell growth and significantly increases tumour cell apoptosis compared to osimertinib. 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.
• Cell Research:
  Concentrations: 5, 10, 100 nM. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

YH 25448, YH25448, YH-25448, inhibit, HER1, Inhibitor, Lazertinib, Lazertinib (YH25448), GNS 1480, GNS1480, GNS-1480, Epidermal growth factor receptor, EGFR, EGFR (del19), EGFR (T790M), EGFR (T790M/L858R), EGFR (wildtype), ErbB-1

Compound Identifiers

PubChem CID

121269225