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Gilteritinib

Gilteritinib structure

CAS No:
1254053-43-4
Formula:
C29H44N8O3
Chemical Name:
Gilteritinib
Synonyms:
ASP2215(Gilteritinib);Gilteritinib;2-Pyrazinecarboxamide, 6-ethyl-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[(tetrahydro-2H-pyran-4-yl)amino]-;6-Ethyl-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[(tetrahydro-2H-pyran-4-yl)amino]-2-pyrazinecarboxamide;6-ethyl-3-((3-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)-5-((tetrahydro-2H-pyran-4-yl)amino)pyrazine-2-carboxamide;Gilteritinib (ASP2215);6-Ethyl-3-((3-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)-amino)-5-((tetrahydr;Gilteritinib(free base)
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Gilteritinib is an inhibitor of FMS-related tyrosine kinase 3 (FLT3; IC50= 5 nM for the wild-type enzyme). It inhibits mutant forms of FLT3, including FLT3 with the internal tandem duplication mutation (FLT3-ITD), FLT3-ITD expressing the F691L mutation, and FLT3 with various tyrosine kinase domain mutations (FLT3-TKD; IC50s =1.4-1.8, 12.2, and 0.7-2 nM, respectively). Gilteritinib also inhibits Axl and c-Kit with IC50values of 41 and 102 nM, respectively. It decreases the viability of blast cells isolated from patients with relapsed acute myeloid leukemia (AML) in a concentration-dependent manner. Formulations containing gilteritinib have been used in the treatment of AML.

ChEBI: Gilteritinib is a member of the class of pyrazines that is pyrazine-2-carboxamide which is substituted by {3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}nitrilo, (oxan-4-yl)nitrilo and ethyl groups at positions 3,5 and 6, respectively. It is a potent inhibitor of FLT3 and AXL tyrosine kinase receptors (IC50 = 0.29 nM and 0.73 nM, respectively). Approved by the FDA for the treatment of acute myeloid leukemia in patients who have a FLT3 gene mutation. It has a role as an apoptosis inducer, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor and an antineoplastic agent. It is a N-methylpiperazine, a member of piperidines, a secondary amino compound, a monomethoxybenzene, a member of pyrazines, a primary carboxamide, an aromatic amine and a member of oxanes.

Class: receptor tyrosine kinase; Treatment: AML, SM; Other name: ASP-2215; Oral bioavailability > 61%; Elimination half-life = 113 h; Protein binding = 94%

Gilteritinib Basic Attributes

Molecular Weight：

552.71

Exact Mass：

552.71

Color/Form：

Off-white to pale pink

Characteristics

Density：

1.242±0.06 g/cm3(Predicted)

Melting Point：

>157°C (dec.)

Boiling Point：

696.9±55.0 °C(Predicted)

PKA：

14.39±0.50(Predicted)

Critical Temperature & Pressure：

-20°C

Gilteritinib Use and Manufacturing

Gilteritinib is an AXL inhibitor in cancer.

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CAS No.: 1254053-43-4

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CAS No.: 1254053-43-4

Grade: Chemical Grade

Content: 98%

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