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Lazertinib

SKU: orb1689983

Description

Lazertinib

Research Area

Cardiovascular Research, Signal Transduction

Images & Validation

Key Properties

CAS Number1903008-80-9
MW554.64
Purity99.96%
FormulaC30H34N8O3
SMILESCOc1cc(N2CCOCC2)c(NC(=O)C=C)cc1Nc1nccc(n1)-n1cc(CN(C)C)c(n1)-c1ccccc1
TargetEGFR
SolubilityH2O: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 o the blood-brain barrier, achieving CSF concentration exceedin the IC50 value for pEGFR inhibition. Lazertinib shows superior efficacy for tumour regression in an EGFR mutant brain metastasis mode.
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 osimertini. 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
concentration : 5, 10, 100 nM. Ba/F3 cells overexpressin the indicated EGFR mutant are treated with YH25448 or osimertinib for 6 hours a the indicated concentration . pEGFR levels are detected by Western blot analysis.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
DisclaimerFor 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

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Key Properties

No computed properties available.

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Lazertinib (orb1689983)

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Available Sizes

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1 mg
$ 90.00
5 mg
$ 140.00
1 ml x 10 mM (in DMSO)
$ 160.00
10 mg
$ 200.00
25 mg
$ 300.00
50 mg
$ 390.00
100 mg
$ 540.00
500 mg
$ 1,190.00
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