ChemicalBook CAS DataBase List 1254053-43-4

1254053-43-4

Name	ASP-2215
CAS	1254053-43-4
Molecular Formula	C29H44N8O3
MDL Number	MFCD28144685
Molecular Weight	552.71
MOL File	1254053-43-4.mol

Chemical Properties

Melting point	>157°C (dec.)
Boiling point	696.9±55.0 °C(Predicted)
density	1.242±0.06 g/cm3(Predicted)
storage temp.	-20°C
solubility	Soluble in DMSO (25 mg/ml)
form	solid
pka	14.39±0.50(Predicted)
color	Off-white to pale pink
Stability:	Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChIKey	GYQYAJJFPNQOOW-UHFFFAOYSA-N
SMILES	C1(C(N)=O)=NC(CC)=C(NC2CCOCC2)N=C1NC1=CC=C(N2CCC(N3CCN(C)CC3)CC2)C(OC)=C1

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H315-H319-H335
Precautionary statements	P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P321-P362+P364-P332+P313-P337+P313-P403+P233-P405-P501

Hazard Information

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 IC₅₀ values 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.

Uses

Gilteritinib is an AXL inhibitor in cancer.

Definition

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.

Brand name

Xospata

General Description

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

target

FLT3, AXL

References

Lee et al. (2017) Preclinical studies of gilteritinib, a next-generation FLT3 inhibitor; Blood?129 257 Thomas et al. (2021) Gilteritinib Inhibits Glutamine Uptake and Utilization in FLT-3-ITD-Positive AML; Cancer Ther.?20 2207

Questions And Answer

Spectrum Detail

Supplier

Shanghai Famo Bio-chemical Technology Company Ltd.

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AN PharmaTech Co Ltd

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Xishi Chemical (Shanghai) Co., Ltd.

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