
CAS
859212-16-1
Formulation
A crystalline solid
Purity
≥95%
MW
576,6
Shipment
-20
Long Term Storage
-20
Shelf Life
1460
Description
Bcr-Abl, a fusion protein with deregulated tyrosine kinase activity, is highly expressed in chronic myelogenous leukemia (CML). Bafetinib is a rationally developed tyrosine kinase inhibitor based on the chemical structure of imatinib (Item No. 13139), with modifications added to improve binding and potency against Bcr-Abl kinase (IC50 = 5.8 nM).{30982} It is 25- to 55-fold more potent than imatinib in vitro and ≥10-fold more potent in vivo.{30982} Bafetinib inhibits 12 out of the 13 most frequent imatinib-resistant Bcr-Abl point mutations, but not the T315I mutation and also targets the Src family kinase Lyn (IC50 = 19 nM), which has been associated with resistance to imatinib in CML.{30982}
ESCLUSIVAMENTE PER USO DI RICERCA (RUO) e non per uso terapeutico o diagnostico su uomini o animali. Il prodotto NON è un Dispositivo Medico o un Diagnostico in Vitro.
PRODUCT FOR RESEARCH USE ONLY (RUO) and not for therapeutic or diagnostic use on humans or animals. The product is NOT a Medical Device or an In-Vitro Diagnostic (IVD).