Gilteritinib

Name: Gilteritinib
Brand: Tocris Bioscience
SKU: 7891

Tocris Bioscience, part of Bio-Techne | Catalog # 7891

Citations (2)

COA / SDS

Potent FLT3 inhibitor; also potently inhibits AXL

Key Product Details

Description:	Potent FLT3 inhibitor; also potently inhibits AXL
Chemical Name:	6-Ethyl-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[(tetrahydro-2H-pyran-4-yl)amino]-2-pyrazinecarboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	552.71

View Full Technical Details for Gilteritinib

Technical Data
Citations

Biological Activity for Gilteritinib

Gilteritinib is a potent Fms-like tyrosine kinase 3 (FLT3) and AXL inhibitor (IC₅₀ = 0.29 nM and 0.73 nM, for FLT3 and AXL, respectively). In vivo, Gilteritinib reduces tumor growth and improves survival in xenograft and intra-bone marrow transplantation models of FLT3 mutated acute myeloid leukemia. Gilteritinib is orally bioavailable.

Technical Data for Gilteritinib

M. Wt	552.71
Formula	C₂₉H₄₄N₈O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1254053-43-4
InChi Key	GYQYAJJFPNQOOW-UHFFFAOYSA-N
Smiles	O=C(N)C=1N=C(C(=NC1NC2=CC=C(C(OC)=C2)N3CCC(N4CCN(C)CC4)CC3)NC5CCOCC5)CC

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Gilteritinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	5.53	10

Preparing Stock Solutions for Gilteritinib

The following data is based on the product molecular weight 552.71.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	18.09 mL	90.46 mL	180.93 mL
0.5 mM	3.62 mL	18.09 mL	36.19 mL
1 mM	1.81 mL	9.05 mL	18.09 mL
5 mM	0.36 mL	1.81 mL	3.62 mL

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References for Gilteritinib

References are publications that support the biological activity of the product.

Mori Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3 mutated acute myeloid leukemia. Invest.New Drugs 2017 PMID: 28516360