bcr-ablt315i

GZD856 is an orally bioavailable PDGFRα/β inhibitor (IC50s: 68.6 and 136.6 nM) with anti-lung cancer activities.

DB07107 is a potent inhibitor of drug resistant T315I mutant Bcr-Abl tyrosine kinase and a potent Akt1 inhibitor (IC50: 360 nM).

AK-HW-90 (compound 2B) is a potent pan-Bcr-Abl inhibitor that shows significant inhibitory activity against Imatinib-resistant mutants. It inhibits the resistant Bcr-AblT315I mutant with an IC50 of 0.65 nM. AK-HW-90 offers potential anti-cancer properties and can be utilized in chronic myeloid leukemia (CML) research.

KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R, EGFR.

Olverembatinib dimesylate (GZD824 Dimesylate) is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I).

Olverembatinib (GZD 824) is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT, IC50: 0.34 nM) and Bcr-Abl(T315I, IC50: 0.68 nM).

GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.

GZD856 formic is a potent, orally active inhibitor of PDGFRα/β and Bcr-Abl T315I, demonstrating IC50 values of 68.6 nM and 136.6 nM for PDGFRα/β, respectively, and 19.9 nM and 15.4 nM for native Bcr-Abl and the T315I mutant, respectively. This compound exhibits significant antitumor activity.

SGX393 is an inhibitor of the CML mutant Bcr-AblT315I, thereby preempting in vitro resistance when combined with nilotinib or dasatinib.