LT-540-717

Chemical Structure : LT-540-717

Catalog No.: PC-25801Not For Human Use, Lab Use Only.

LT-540-717 is a potent, selective and orally available FLT3 inhibitor with IC50 of 0.62 nM, inhibits FLT3 mutations FLT3 (ITD), FLT3 (D835V), FLT3 (ITD, D835V), FLT3 (ITD, F69L) with IC50 of 18.22, 1.54, 0.58 and 1.61 nM, respectively.

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Biological Activity

LT-540-717 is a potent, selective and orally available FLT3 inhibitor with IC50 of 0.62 nM, inhibits FLT3 mutations FLT3 (ITD), FLT3 (D835V), FLT3 (ITD, D835V), FLT3 (ITD, F69L) with IC50 of 18.22, 1.54, 0.58 and 1.61 nM, respectively.
LT-540-717 displays <100-fold selectivity over CDK4/cycD3, CDK6/CycD1 and CDK7/CycH/MAT1, exhibits little inhibitory activity against other kinases.
LT-540-717 shows the strongest proliferation-inhibition efficacy against MV4-11 cells with IC50 of 0.02 uM.
LT-540-717 shows much more potent anti-proliferative activities against cell lines containing FLT3 (ITD) mutant (MV4-11 and MOLM-13) than cell lines containing wild-type FLT3 or expressing FLT3.
LT-540-717 (25 mg/kg, QD and 50 mg/kg, QD) exhibited antitumor efficacy in MV4-11 xenograft model.

Physicochemical Properties

M.Wt	456.51
Formula	C24H24N8O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-((6-Phenoxypyrimidin-4-yl)amino)-N-(4-(piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide

References

1. Yanle Zhi, et al. Eur J Med Chem. 2023 Aug 5:256:115448.

LT-540-717

Biological Activity

Physicochemical Properties

References

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