Chemical Structure : FLT3 inhibitor 17
CAS No.:
FLT3 inhibitor 17
Catalog No.: PC-21367Not For Human Use, Lab Use Only.
FLT3 inhibitor 17 is a potent, highly selective FLT3 inhibitor with IC50 of 1.2 nM and 1.4 nM for FLT3 WT and FLT3-D835Y, shows low activity against VEGFR, FGFR, PDGFR, c-KIT, and RET.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
FLT3 inhibitor 17 is a potent, highly selective FLT3 inhibitor with IC50 of 1.2 nM and 1.4 nM for FLT3 WT and FLT3-D835Y, shows low activity against VEGFR, FGFR, PDGFR, c-KIT, and RET.
FLT3 inhibitor 17 inhibits FLT3 WT, FLT3-ITD and FLT3 D835Y with IC50 of ~1 nM, weakly inhibits c-KIT and RET with IC50 of 837 nM and 18000 nM.
FLT3 inhibitor 17 shows very limited activity against cardiovascular kinases FGFR1/2 and PDGFRα/β, with IC50 values >2690 nM, also displays minimal inhibition of over 180 other kinases.
FLT3 inhibitor 17 exhibits antiproliferative effects on Molm14cell lines containing mutated FLT3:Molm-14 (FLT3-ITD), Molm-14 (FLT3-ITD/D835Y) and Molm-14 (FLT3-ITD/F691L) with GI50 values of 2-23 nM, reduces the levels of phosphorylated FLT3 in Molm-14 cells.
Physicochemical Properties
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M.Wt
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374.45
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Formula
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C21H22N6O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(2S,6R)-4-(3-(4-(1H-pyrazol-4-yl)phenyl)imidazo[1,2-b]pyridazin-6-yl)-2,6-dimethylmorpholine
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References
1. Sintim HO, et al. ChemMedChem. 2023 Nov 16:e202300442.
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