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Dosimertinib

Cat. No. M21108
Dosimertinib Structure
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Biological Activity

Dosimertinib is a highly potent, selective, orally effective EGFR inhibitor for the study of non-small cell lung cancer.

Chemical Information
Molecular Weight 504.64
Formula C28H28D5N7O2
CAS Number 2403760-70-1
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] Yvette N Lamb. Target Oncol. Osimertinib: A Review in Previously Untreated, EGFR Mutation-Positive, Advanced NSCLC

[2] Ying Cheng, et al. Target Oncol. Osimertinib Versus Comparator EGFR TKI as First-Line Treatment for EGFR-Mutated Advanced NSCLC: FLAURA China, A Randomized Study

[3] Sabine Schmid, et al. Lung Cancer. Mechanisms of osimertinib resistance and emerging treatment options

[4] Alessandro Leonetti, et al. Br J Cancer. Resistance mechanisms to osimertinib in EGFR-mutated non-small cell lung cancer

[5] J Remon, et al. Ann Oncol. Osimertinib and other third-generation EGFR TKI in EGFR-mutant NSCLC patients

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