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Lazertinib

Cat. No. M9938
Lazertinib Structure
Synonym:

YH-25448; GNS-1480

Size Price Availability Quantity
5mg USD 160  USD160 In stock
10mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

Lazertinib, also known as YH-25448 and GNS-1480, is an oral active, highly potent, mutant-selective and irreversible EGFR Tyrosine-kinase inhibitors (TKIs) targets both the T790M mutation and activating EGFR mutations while sparing wild type-EGFR. Lazertinib (YH25448) has good blood brain barrier (BBB) penetration property.

Chemical Information
Molecular Weight 554.64
Formula C30H34N8O3
CAS Number 1903008-80-9
Solubility (25°C) DMSO 6 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] No authors listed. Cancer Discov. Lazertinib Is Safe and Effective in Non-Small Cell Lung Cancer

[2] Sohita Dhillon. Correction to: Lazertinib: First Approval

[3] Sohita Dhillon. Lazertinib: First Approval

[4] Misako Nagasaka, et al. Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC

[5] Myung-Ju Ahn, et al. Lazertinib in patients with EGFR mutation-positive advanced non-small-cell lung cancer: results from the dose escalation and dose expansion parts of a first-in-human, open-label, multicentre, phase 1-2 study

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Keywords: Lazertinib, YH-25448; GNS-1480 supplier, EGFR/HER2, inhibitors, activators

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