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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 |
|---|
| Quizartinib (AC220)
Quizartinib (AC220) is a uniquely potent and selective FLT3 inhibitor. |
| KW-2449
KW-2449 is a novel multitargeted kinase inhibitor of FLT3, ABL and Aurora kinase with IC50 values of 6.6 nM, 14 nM and 48 nM. |
| TCS 359
TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM. |
| CGP52421
CGP52421 is a FLT3 inhibitor, which is also an metabolite of midostaurin (PKC412). |
| Crotonoside
Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the treatment of AML. |
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