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Lazertinib

Catalog No. T4485   CAS 1903008-80-9
Synonyms: Lazertinib (YH25448), GNS-1480, YH25448

Lazertinib (GNS-1480) is an effective, 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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Lazertinib Chemical Structure
Lazertinib, CAS 1903008-80-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
2 mg In stock $ 59.00
5 mg In stock $ 93.00
10 mg In stock $ 153.00
25 mg In stock $ 272.00
50 mg In stock $ 343.00
100 mg In stock $ 497.00
500 mg In stock $ 1,150.00
1 mL * 10 mM (in DMSO) In stock $ 112.00
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Purity: 99.96%
Purity: 99.53%
Purity: 98.7%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Lazertinib (GNS-1480) is an effective, 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.
Targets&IC50 Del19:5 nM, Del19/T790M:1.7 nM, L85R:20.6 nM, WT EGFR:76 nM, L858R/T790M EGFR:2 nM
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[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.
In vivo In an in vivo mouse model implanted with H1975 cells, once-daily YH25448 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 YH25448 is 5.9-6.8 hr, while a tumour to plasma AUC0-last ratio is 3.0-5.1 in tumour-bearing mice. YH25448 shows excellent penetration of the blood-brain barrier, achieving CSF concentrations exceeding the IC50 value for pEGFR inhibition. YH25448 shows superior efficacy for tumour regression in an EGFR mutant brain metastasis model[1].
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.
Synonyms Lazertinib (YH25448), GNS-1480, YH25448
Molecular Weight 554.64
Formula C30H34N8O3
CAS No. 1903008-80-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5.55 mg/mL (10 mM), Sonification is recommended

Ethanol: Insoluble

H2O: Insoluble

TargetMolReferences and Literature

1. Byoung Chul Cho, et al. YH25448, a 3rd Generation EGFR-TKI, in Patients with EGFR-TKI-resistant NSCLC: Phase I/II Study Results.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Drug Repurposing Compound Library Anti-Ovarian Cancer Compound Library Anti-Colorectal Cancer Compound Library Bioactive Compound Library NO PAINS Compound Library

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Keywords

Lazertinib 1903008-80-9 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Lazertinib (YH25448) ErbB-1 GNS1480 GNS-1480 Inhibitor Epidermal growth factor receptor HER1 YH 25448 YH-25448 GNS 1480 YH25448 inhibit inhibitor

 

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