Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
|Solubility (25°C)||DMSO 12.5 mg/mL|
|Storage||2-8°C, dry, sealed|
|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.
|Related EGFR/HER2 Products|
ORM-5029 is a HER2/HER3-specific dual-targeted antibody degrader coupling (AnDC) for studies related to HER2-positive breast cancer.
CH7233163 is a non-covalent ATP-competitive EGFR- del19 /T790M/C797S inhibitor that can achieve potent inhibitory activity and mutation selection by exploiting multiple interactions with the αC helix conformation of EGFR, with antitumor activity, and can be used in studies related to non-small cell lung cancer (NSCLC).
BLU-701 is a highly selective, potent EGFR tyrosine kinase inhibitor (TKI) with activity against EGFR-activating mutations and C797S-resistant mutations for studies related to non-small cell lung cancer (NSCLC).
BI-4020 is a fourth-generation, orally active, non-covalent EGFR tyrosine kinase macrocyclic inhibitors (TKIs). It inhibits the triple mutant EGFR del19 T790M C797S mutant (IC50=0.2 nM in the BaF3 cell line), the double mutant EGFR del19 T790M, and the single mutant EGFR del19 (IC50=1 nM). and also retains activity against EGFR wt (IC50=190 nM), which can be used in studies related to non-small cell lung cancer (NSCLC).
BBT-176 is a novel, EGFR tyrosine kinase inhibitor (TKI) targeting the C797S mutation for studies related to non-small cell lung cancer (NSCLC).
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