Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5.55 mg/mL (10 mM), Sonification is recommended
Ethanol: Insoluble
H2O: Insoluble
You can also refer to dose conversion for different animals. More
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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