ON012380

ON012380 (1 nM-1 μM; 30 min pre-incubation, 20 min kinase reaction) potently inhibits wild-type BCR-ABL kinase activity with an IC₅₀ of 9.0 nM, and acts synergistically with Imatinib (HY-15463) to reduce the IC₅₀ to 0.83 nM^[1].
ON012380 (0.1 nM-1000 nM; 30 min pre-incubation, 20 min kinase reaction) acts as a substrate-competitive inhibitor of wild-type BCR-ABL, with IC₅₀ values unaffected by ATP concentration but increased by higher Crk substrate concentrations^[1].
ON012380 (30 min pre-incubation, 20 min kinase reaction) potently inhibits the kinase activity of the Imatinib-resistant BCR-ABL^T315I mutant with an IC₅₀ of 1.5 nM^[1].
ON012380 (72 h) reduces viability of K562 and 32Dcl3-p210BCR-ABL cells with an LD₅₀ of 10-15 nM^[1].
ON012380 (10 nM-1000 nM; 24 h) dose-dependently inhibits BCR-ABL kinase activity and suppresses STAT-5 phosphorylation in K562 cells^[1].
ON012380 (72 h) reduces viability of all tested Imatinib-resistant BCR-ABL mutant-expressing 32Dcl3 cell lines with LD₅₀ values ranging from 5.9 nM to 10.0 nM^[1].
ON012380 (1 nM-1000 nM; 24 h) dose-dependently inhibits BCR-ABL^T315I kinase activity and suppresses STAT-5 phosphorylation in 32Dcl3-BCR-ABL^T315I cells^[1].
ON012380 potently inhibits growth of cells expressing wild-type Bcr-Abl and all tested Imatinib-resistant Bcr-Abl mutants (including BCR-ABL^T315I) at concentrations < 10 nM, and also inhibits PDGFR- and Lyn-dependent cell proliferation with an IC₅₀ of approximately 80 nM^[2].
ON012380 (1.38-9 nM) potently inhibits wild-type Bcr-Abl kinase activity with an IC₅₀ of 9 nM and the Imatinib-resistant Bcr-Abl^T315I mutant with an IC₅₀ of 1.38 nM via non-ATP competitive binding^[3].
ON012380 (<10 nM) induces apoptosis and cell death in Ph+ CML cells expressing the Imatinib-resistant BCR-ABL^T315I isoform^[3].
ON012380 (2-24 h) reduces viability and induces apoptosis in IL-3-dependent BaF3 cells, wild-type BCR-ABL-transformed BaF3 cells, and BCR-ABL^T315I-mutant BCR-ABL-transformed BaF3 cells, with no significant inhibition of BCR-ABL signaling (Stat5 and CrkL phosphorylation)^[4].
ON012380 reduces viability with an IC₅₀ of ~300 nM and induces apoptosis in K562, BV-173, and T315I-mutant BCR-ABL-expressing BV-173R CML cells, but has limited activity in Lyn-overexpressing K562R cells, with no associated inhibition of BCR-ABL or Lyn kinase signaling^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.