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Gilteritinib

Cat. No. 7891 Submit a Review Datasheet / COA / SDS
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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)
Datasheet
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Biological Activity Technical Data Solubility Calculators Datasheets References

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 Data for Gilteritinib

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 et al (2017) Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3 mutated acute myeloid leukemia. Invest.New Drugs 35 556 PMID: 28516360

If you know of a relevant reference for Gilteritinib, please let us know.

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Keywords: Gilteritinib, Gilteritinib supplier, FLT3, AXL, inhibitors, inhibits, FMS-like, receptor, tyrosine, kinase-3, acute, myeloid, leukemia, xenograft, AML, orally, bioavailable, , in, vivo, 7891, Tocris Bioscience

Citations for Gilteritinib

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