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Tandutinib (MLN518, CT53518) is an orally active multitargeted tyrosine kinase inhibitor of FLT3 (IC50 = 0.22 μM), and it also inhibits c-Kit and PDGFR with IC50 values of 0.17 μM and 0.20 μM, respectively. Tandutinib has the ability to cross the blood-brain barrier.
Tandutinib inhibited FLT3 phosphorylation, downstream signaling and malignant growth in vitro and in animal models. In cellular assays, Tandutinib inhibited the autophosphorylation of these receptors with an IC50 of approximately 200 nM. Both the W51 mutant and the WT FLT3 receptor showed a significant inhibition of receptor autophosphorylation with Tandutinib treatment. In studies of 5 different FLT3/ITD expressing cells, Tandutinib inhibited cell growth with an IC50 of 10-30 nM in all cases.
Tandutinib (60 mg/kg; oral gavage; daily; for 35 days; athymic nude mice) treatment causes a statistically significant increase in survival that was extended on average by 20 days.
| Cell Experiment | |
|---|---|
| Cell lines | AML cells expressing FLT3-ITD |
| Preparation method | AML cell lines HL60 (AML-M3) and AML193 (AML-M5), KG-1, KG-1a, THP-1, and ALL cell line RS4;11 were purchased from ATCC (Bethesda, MD). Cells (initial count of 0.3* 105–1.0 *105) were washed three times in RPMI 1640 medium and plated in 1 ml of complete growth media (without IL-3 for the Ba/F3 cells) in the presence of increasing concentrations of CT53518 (0.004–30 μM). Cells were grown for 3–7 days in tissue culture, and viable cells, determined by Trypan blue dye exclusion, were counted. |
| Concentrations | 0.004-30 μM |
| Incubation time | 3 days |
| Animal Experiment | |
|---|---|
| Animal models | Ba/F3 nude mouse model of FLT3-ITD-mediated leukemia |
| Formulation | 0.5% methyl cellulose |
| Dosages | 60 mg/kg BID day 7-57 |
| Administration | oral gavage |
| Molecular Weight | 562.7 |
| Formula | C31H42N6O4 |
| CAS Number | 387867-13-2 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related FLT3 Products |
|---|
| 4SC-203
4SC-203 is a potent multikinase inhibitor with potential antineoplastic activity. |
| AKN-028
AKN-028, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. |
| FLT3-IN-3
FLT3-IN-3 is a potent FLT3 inhibitor with IC50s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively. |
| MAX-40279
MAX-40279 is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. |
| FLT3-IN-10
FLT3-IN-10 is a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3). |
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