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Lazertinib

🥰Excellent
Catalog No. T4485Cas No. 1903008-80-9
Alias YH25448, Lazertinib (YH25448), GNS-1480

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.

Lazertinib

Lazertinib

🥰Excellent
Purity: 99.53%
Catalog No. T4485Alias YH25448, Lazertinib (YH25448), GNS-1480Cas No. 1903008-80-9
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.
Pack SizePriceAvailabilityQuantity
1 mg$41In Stock
5 mg$93In Stock
10 mg$153In Stock
25 mg$253In Stock
50 mg$343In Stock
100 mg$497In Stock
500 mg$1,150In Stock
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Purity:99.53%
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Product Introduction

Bioactivity
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
EGFR (L858R/T790M):2 nM, EGFR (WT):76 nM, L85R:20.6 nM, Del19/T790M:1.7 nM, Del19:5 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 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[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.
AliasYH25448, Lazertinib (YH25448), GNS-1480
Chemical Properties
Molecular Weight554.64
FormulaC30H34N8O3
Cas No.1903008-80-9
SmilesCOc1cc(N2CCOCC2)c(NC(=O)C=C)cc1Nc1nccc(n1)-n1cc(CN(C)C)c(n1)-c1ccccc1
Relative Density.1.27 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 5.55 mg/mL (10 mM), Sonication is recommended.
Ethanol: Insoluble
H2O: Insoluble
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8030 mL9.0149 mL18.0297 mL90.1486 mL
5 mM0.3606 mL1.8030 mL3.6059 mL18.0297 mL
10 mM0.1803 mL0.9015 mL1.8030 mL9.0149 mL

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