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Gilteritinib

Chemical Structure : Gilteritinib

CAS No.: 1254053-43-4

Gilteritinib (ASP2215, ASP-2215)

Catalog No.: PC-43033Not For Human Use, Lab Use Only.

Gilteritinib (ASP2215) is a potent FLT3/AXL inhibitor with IC50 of 0.73 nM/0.29 nM respectively; also inhibits LTK and ALK (IC50=0.35 nM and 1.2 nM respectively).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Gilteritinib (ASP2215) is a potent FLT3/AXL inhibitor with IC50 of 0.73 nM/0.29 nM respectively; also inhibits LTK and ALK (IC50=0.35 nM and 1.2 nM respectively).
Gilteritinib (ASP2215) shows >800-fold selectivity over c-Kit.
Gilteritinib (ASP2215) inhibits the growth of Ba/F3 cells expressing either FLT3-ITD, FLT3-D835Y, FLT3-ITD-D835Y, FLT3-ITD-F691 L, and FLT3-ITD-F691I, with IC50 of 1.8 nM, 1.6 nM, 2.1 nM, 22 nM, and 49 nM, respectively.
Gilteritinib (ASP2215) is orally bioactive.

Physicochemical Properties

M.Wt 552.7115
Formula C29H44N8O3
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

Ethanol: 100 mM

Chemical Name/SMILES

2-Pyrazinecarboxamide, 6-ethyl-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[(tetrahydro-2H-pyran-4-yl)amino]-

References

1. Mori M, et al. Invest New Drugs. 2017 May 17. doi: 10.1007/s10637-017-0470-z.

2. Lee LY, et al. Blood. 2017 Jan 12;129(2):257-260.

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