ARRY-380 is an orally bioavailable, potent, selective, small-molecule tyrosine kinase HER2 and p95-HER2 inhibitor with an IC50 of 8 and 7 nM, respectively. However, ARRY-380 inhibits EGFR with an IC50 of 4 μM. ARRY-380 is about 500-fold selective for HER2 versus EGFR. ARRY-380 produces significantly antitumor activities in multiple HER2-dependent tumor xenograft models and generates additive activity in combination with standard-of-care agents. ARRY-380 is in a phase I clinical trial for the treatment of breast cancer
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 100 mg/mL|
|Related EGFR/HER2 Products|
Anlotinib is a EGFR inhibitor extracted from patent 2015185012 A1, compound 1，which can be used to treat non-small cell lung cancer.
Cetuximab, a novel molecular-targeted agent,is an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EGFR to block ligand stimulation. MW : 145.781 KD.
EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild-type receptor.
Gefitinib Hcl(ZD-1839 Hcl) is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR.
Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.