Avitinib (Abivertinib; AC0010) is a third-generation irreversible EGFR tyrosine kinase inhibitor, with potential antineoplastic activity. Avitinib (Abivertinib; AC0010) inhibits cell proliferation, reduces colony-forming capacity, and induces apoptosis and cell cycle arrest in AML cells, especially those harboring FLT3-ITD mutations.
In vivo, AC0010 (500 mg/kg; oral) administration daily resulted in complete remission of tumors with EGFR active and T790M mutations for over 143 days with no weight loss in a xenografte model.
|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.
|Solubility||DMSO 80 mg/mL|
|Related EGFR/HER2 Products|
TX1-85-1 is an ErbB3 inhibitor with IC50 of 23 nM, it is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3.
AZD3759 hydrochloride is an orally available inhibitor of the epidermal growth factor receptor (EGFR) with potential antineoplastic activity.
Tucatinib, also known as Irbinitinib and ONT-380, is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (HER2).
Lazertinib, also known as YH-25448 and GNS-1480, is an oral active, highly potent, mutant-selective and irreversible EGFR Tyrosine-kinase inhibitors (TKIs) targets both the T790M mutation and activating EGFR mutations while sparing wild type-EGFR.
Pyrotinib (SHR-1258) is an orally bioavailable, potent and selective EGFR/HER2 dual inhibitor, with IC50 values of 13 and 38 nM, respectively.
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