Table 4. Potency of FLT3 inhibitors.
FLT3-inhibitor | FLT3-ITD autophorphorylation, IC50, medium (nM) | FLT3-ITD autophorphorylation, IC50, plasma (nM) | Ref. |
---|---|---|---|
AC220 | 1 | 18.4 | [97,98,106] |
Tandutinib (MLN518) | 6 | ~ 200 | [93,96] |
Sorafenib (BAY43-9006) | 3 | 308 – 484 | [62,106] |
Sunitinib (SU11248) | 1 | NR | [98,106] |
Midostaurin (PKC412) | 3 – 6 | 1000 – 1800 | [84,106] |
Lestaurtinib (CEP-701) | 2 | 700 | [98,106] |
FLT3: FMS-like tyrosine kinase 3; ITD: Internal tandem duplication; NR: Not reported.