Table 1 Indole-based FLT3 inhibitors
Compound name and its structure | Description | Refs. | |
|---|---|---|---|
| Target | FLT3, PKC, Syk, FLT-1, AKT, KIT, PDGFR-ẞ, and VEGFDR1/2 | |
Binding mode to FLT3 kinase | Type I | ||
Mutation point | N676K/S/D, A627T/P, F691L, and G697R/S | ||
In vitro targeted AML cells (IC50) | 1–10 nM (in Ba/F3 cells expressing FLT3-D835V/D835del/ I836del/D853H/D835A/ D835E/D835Y/ D835N), and 4.14 nM (in Ba/F3 expressing FLT3-ITD) | ||
| Target | FLT3, TrKA, JAK2, and VEGFR | |
Binding mode to FLT3 kinase | Type I | ||
Mutation point | A627P | ||
FLT3 Potency (IC50) | 2.9, 11.9, and 3Â nM (FLT3-ITD (in AML monocytes), FLT3-wt (in AML monocytes), FLT3-ITD (in Ba/F3 cells), respectively) | ||
In vitro targeted AML cells (IC50) | 5Â nM (in Ba/F3 cells expressing FLT3-ITD) | ||
| Target | Dual FLT3, and MnK2 | [69] |
Binding mode to FLT3 kinase | Type I | ||
FLT3 Potency (IC50) | 0.34 μM | ||
In vitro targeted AML cells (IC50) | 0.6 μM | ||
| Target | FLT3-ITD-F691L | [70] |
Binding mode to FLT3 kinase | Type I | ||
FLT3 Potency (IC50) | 114Â nM | ||
In vitro targeted AML cells (IC50) | 0.34 μM | ||
| Target | FLT3 | [71] |
Binding mode to FLT3 kinase | Type II | ||
FLT3 Potency (IC50) | 5.5 μM | ||
In vitro targeted AML cells (IC50) | 1.4–5.7 μM | ||
