|Description||Nilotinib monohydrochloride monohydrate is an orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. It binds to and stabilizes the inactive conformation of the kinase domain of the Abl protein of the Bcr-Abl fusion protein, resulting in the inhibition of the Bcr-Abl-mediated proliferation of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) cells. It also inhibits the receptor tyrosine kinases platelet-derived growth factor receptor (PDGF-R) and c-kit, a receptor tyrosine kinase mutated and constitutively activated in most gastrointestinal stromal tumors (GISTs).|
PD-173955 is a src tyrosine kinase inhibitor. PD173955 inhibited Bcr-Abl-dependent cell growth. PD173955 showed cell cycle arrest in G(1). PD173955 has an IC(50...
Flumatinib mesylate, a derivative of imatinib, is a multi-kinase inhibitor for c-Abl, PDGFRβ and c-Kit. It is currently in Phase I and II clinical trials in Chi...
Dasatinib, also known as BMS-354825, is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and...
ZM306416 is a vascular endothelial growth factor receptor (VEGFR) antagonist.
GNF-7 is a type-II T315I inhibitor. GNF-7 inhibits Ack1 and germinal center kinase (GCK). GNF-7 is among the first type-II inhibitors capable of inhibiting T315...
Bafetinib is a potent and selective dual Bcr-Abl/Lyn inhibitor, but it does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and ...
Asciminib, also known as ABL001, is a potent and selective allosteric Bcr-Abl inhibitor. Asciminib inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
DCC-2036(Rebastinib) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR
Bafetinib, also known as INNO-406, is an orally bioavailable 2-phenylaminopyrimidine derivative with potential antineoplastic activity. Bafetinib specifically ...
Dasatinib hydrochloride is a potent and dual Abl/ Src inhibitor. It inhibits c-Kit (WT)/c-Kit (D816V).
Nilotinib monohydrochloride monohydrate
Nilotinib monohydrochloride monohydrate is an orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. It ...
Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM.
Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively.
CHMFL-ABL-053 is a potent and orally available inhibitor of BCR-ABL (IC50 = 70nM) without inhibitory activity against c-KIT kinase that is a common target of BC...
GZD824 potently suppressed proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC(50) values of 0.2 and 0.13 nM, respectively. It also display...
DPH is a potent cell permeable c-Abl activator. It binds and alters the conformation of the myristoyl binding site of c-Abl tyrosine kinase. DPH exhibits potent...