Isoform | Mutation locus | IC50 (nM) | IC50 (nM) | IC50 (nM) | IC50 (nM) |
---|---|---|---|---|---|
Ba/F3 transfectants | leukemia cell lines | ||||
Inhibition of proliferation | Induction of apotosis | Inhibition of proliferation | Induction of apotosis | ||
BCR/ABL | fusion | n.r.* | n.r.* | not reached (K562) | n.r.* (K562) |
FLT3 WT | N/A | 49 | 11 | ||
FLT3 ITD, 10% FBS | juxtamembrane domain | 9 | 5 | <1 (MOLM14) | 3 (MOLM14) |
FLT3 ITD, 0.5%FBS | juxtamembrane domain | <1 | N/D | ||
FLT3 K663Q | tyrosine kinase domain I | 14 | 23 | ||
FLT D835V | tyrosine kinase domain II | 172 | 888 | ||
FLT3 D835Y | tyrosine kinase domain II | 84 | 24 | ||
KIT WT | N/A | 474 | n.r.* | 77 (M0-7e) | 210 (MO-7e) |
KIT D816F | tyrosine kinase domain II | 2871 | 6254 | ||
KIT D816V, 10% FBS | tyrosine kinase domain II | 3074 | 8982 | 1727 (HMC1.2) | n.r.* (HMC1.2) |
KIT D816V, 0.5% FBS | tyrosine kinase domain II | 633 | N/A | ||
KIT D816Y, 0.5% FBS | tyrosine kinase domain II | 366 | 611 | 445 (p815) | 341 (p815) |
parental | N/A | n.r.* | n.r.* | ||
parental + DMSO | N/A | n.r.* | n.r.* |