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Mefatinib

Cat. No. M29079
Mefatinib Structure
Synonym:

Mifanertinib dimaleate

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Biological Activity

Mefatinib is a potent tyrosine kinase inhibitor with antineoplastic activity.

Chemical Information
Molecular Weight 698
Formula C29H27ClF3N5O10
CAS Number 1989592-50-8
Form Solid
Storage 4°C, dry, sealed
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] Mingyao Wang, et al. Signal Transduct Target Ther. Gefitinib and fostamatinib target EGFR and SYK to attenuate silicosis: a multi-omics study with drug exploration

[2] Wen-Zhao Zhong, et al. J Clin Oncol. Gefitinib Versus Vinorelbine Plus Cisplatin as Adjuvant Treatment for Stage II-IIIA (N1-N2) EGFR-Mutant NSCLC: Final Overall Survival Analysis of CTONG1104 Phase III Trial

[3] Cuilan Sun, et al. Respir Res. FGL1 regulates acquired resistance to Gefitinib by inhibiting apoptosis in non-small cell lung cancer

[4] Yukio Hosomi, et al. J Clin Oncol. Gefitinib Alone Versus Gefitinib Plus Chemotherapy for Non-Small-Cell Lung Cancer With Mutated Epidermal Growth Factor Receptor: NEJ009 Study

[5] Vanita Noronha, et al. J Clin Oncol. Gefitinib Versus Gefitinib Plus Pemetrexed and Carboplatin Chemotherapy in EGFR-Mutated Lung Cancer

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