Bcr-Abl

Bcr-Abl

Most patients with chronic myelogenous leukemia (CML) are treated in the first instance with Bcr-Abl tyrosine-kinase inhibitors (TKI). A chromosomal abnormality that results in the formation of a so-called Philadelphia chromosome is the root cause of more than 90% of CML cases. This abnormality results from the fusion of the break point cluster (Bcr) gene at chromosome 22 with the Abelson (Abl) tyrosine kinase gene at chromosome 9, creating a chimeric oncogene (Bcr-Abl) and a constitutively active Bcr-Abl tyrosine kinase that has been linked to the pathogenesis of CML. The tyrosine kinase has been selectively inhibited by substances.

Bcr-Abl related products

Structure Cat No. Product Name CAS No. Product Description
V0679 Bafetinib (INNO-406; NS187) 859212-16-1 Bafetinib (formerly INNO406; NS-187),an investigational anticancer drug originally developed by Nippon Shinyaku and later licensed to CytRx, is an orally bioavailable dual Bcr-Abl/Lyn inhibitor with potential antineoplastic activity.
V0680 Degrasyn (WP-1130) 856243-80-6 Degrasyn (formerly also known as WP1130) is a novel, potent, and selective small molecule inhibitor of deubiquitinases (DUBs such as USP5, USP14, USP9x, UCH-L1, and UCH37).
V0678 GNF-2 778270-11-4 GNF-2 (GNF 2; GNF2) is a highly potent, selective and allosteric/non-ATP competitive inhibitor of Bcr-Abl with potential anticancer activity.
V0674 GNF-5 778277-15-9 GNF-5 (GNF 5; GNF5), aGNF-2 analog with better pharmacokinetic profiles, is a potent,selective and allosteric/non-ATP competitive Bcr-Abl inhibitor with potential anticancer activity.
V0672 GNF-7 839706-07-9 GNF-7 (GNF7; GNF 7) is a novel, potent, orally bioactive/bioavailable Bcr-Abl kinase inhibitor with potential anticancer activity.
V0671 Nilotinib (AMN107; Tasigna) 641571-10-0 Nilotinib (formerly also known asAMN-107, AMN107; trade name Tasigna) is a potent, orally bioavailable aminopyrimidine-based Bcr-Abl inhibitor with antineoplastic activity.
V0675 Olverembatinib Dimesylate (GZD824) 1421783-64-3 Olverembatinib Dimesylate (GZD-824; HQP-1351; trade name in China: Nailike), the dimesylate salt ofGZD824 (HQP1351),is a novel, potent, orally bioavailable Bcr-Abl inhibitor with potential antineoplastic activity.
V0676 PD173955 260415-63-2 PD173955 (PD-173955), asrc-selective tyrosine kinase inhibitor, is a novel and potent Bcr-Abl inhibitor with potential anticancer activity.
V0673 Radotinib (IY 5511; Supect) 926037-48-1 Radotinib (formerly IY-5511; IY5511; trade name Supect) is a novel, potent,selective, orally bioavailable, and 2nd generationBCR-ABL1 tyrosine kinase inhibitor with potential antineoplastic activity.
V0677 Rebastinib (DCC2036) 1020172-07-9 Rebastinib (formerly also known asDCC-2036), a novel, potent andorally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity, is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50s of 0.8 nM and 4 nM.
V41836 Vodobatinib (SCO-088, SUN-K706; K-0706) 1388803-90-4 Vodobatinib (K0706) is a potent, third-generation, orally bioactive Bcr-Abl1 tyrosine kinase inhibitor (TKI) (antagonist) with IC50 of 7 nM.
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