AG1557 is a potent and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with pIC50 value of 8.194.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 A G Ellis, et al. J Chromatogr B Biomed Sci Appl. High-performance liquid chromatographic analysis of the tyrphostin AG1478, a specific inhibitor of the epidermal growth factor receptor tyrosine kinase, in mouse plasma
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Blu-945 is a potent inhibitor of selective epidermal growth factor receptor (EGFR).
Sunvozertinib (DZD9008) is an effective inhibitor of ErbBs (EGFR, Her2, especially mutants) and BTK.
(S)-Sunvozertinib ((S)-DZD9008) is the S-enantiomer of Sunvozertinib, EGFR exon 20 NPH and ASV insertion, EGFR L858R/T790M mutation and Her2 exon 20 YVMA insertion (IC50 was 51.2 nM, 51.9 nM, 1 nM and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.
(Rac)-JBJ-04-125-02 is a racemate of JBJ-04-125-02, which is a potent, selectively mutated, allosteric and oral active EGFR inhibitor. The IC50 of EGFRL858R/T790M was 0.26 nM.
AZ7550 Mesylate is an active metabolite of AZD9291, AZ7550 inhibits IGF1R activity,IC50 1.6 μM.
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