Home Protein Tyrosine Kinase FLT3 inhibitor - Axl inhibitor Gilteritinib (ASP2215) For research use only.

Gilteritinib (ASP2215)

Gilteritinib (ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).

Gilteritinib (ASP2215) Chemical Structure

Gilteritinib (ASP2215) Chemical Structure

CAS No. 1254053-43-4

Purity & Quality Control

Gilteritinib (ASP2215) Related Products

Signaling Pathway

FLT3 Signaling Pathways

FLT3 Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV4-11 cells Cell cycle assay 1, 3, 10, and 30 nM 24 h The mean proportion of MV4-11 cells in G1 phase were significantly increased at gilteritinib concentrations of 3 (69.0%; P<0.01) and 10 nM (70.7%; P<0.001). 31069015
MOLM-13 cells Apoptosis assay 1, 3, 10, 30, and 100 nM 48 h significant increases in the percentage of annexin V-positive cells at concentrations of 30 nM (32.0%) and 100 nM (52.4%) versus control (4.1%) 31069015
32D/TKD cells Function assay 50 nM  6 h Inhibiton of the phosphorylation of Akt on T308 29507660
TF-1 cells Function assay 0, 20, 80, 200 and 500 nM 1 h gilteritinib has an IC50 against wild-type c-Kit of 102 nM 27908881
BA/F3 Function assay Inhibition Assay: A recombinant retrovirus was created from expression plasmid FLAG-EML4-ALKv1/pMX-iresCD8 in which cDNA for EMLA-ALK fusion protein v1 was integrated, and injected into mouse lymphoid cell line BA/F3 cells. Using a magnetic bead reagent f, IC50 = 0.0015 μM. ChEMBL
BA/F3 Function assay Inhibition Assay: A recombinant retrovirus was created from expression plasmid FLAG-EML4-ALKv1/pMX-iresCD8 in which cDNA for EMLA-ALK fusion protein v1 was integrated, and injected into mouse lymphoid cell line BA/F3 cells. Using a magnetic bead reagent f, IC50 = 0.0015 μM. ChEMBL
Vero Antiviral assay 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr, IC50 = 6.76 μM. ChEMBL
Vero Cell viability assay 72 hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr, CC50 = 37.16 μM. ChEMBL
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Biological Activity

Description Gilteritinib (ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).
Targets
FLT3 [1]
(Cell-free assay)		 Axl [1]
(Cell-free assay)
0.29 nM 0.73 nM
In vitro
In vitro Gilteritinib demonstrates potent inhibitory activity against the internal tandem duplication (FLT3-ITD) and FLT3-D835Y point mutations in cellular assays using MV4-11 and MOLM-13 cells as well as Ba/F3 cells expressing mutated FLT3. Gilteritinib decreases the phosphorylation levels of FLT3 and its downstream targets in both cellular and animal models. Gilteritinib inhibits the activity of eight of the 78 tested kinases by over 50% at concentrations of either 1 nM (FLT3, LTK, ALK, and AXL) or 5 nM (TRKA, ROS, RET, and MER)[1]. Gilteritinib treatment for 48h results in an induction of apoptosis in MV4-11 cells as determined by an increase in annexin V-positive cells. Gilteritinib also decreases the expression of anti-apoptotic proteins such as MCL-1, BCL2L10, and survivin, which are reported to be important in chemotherapy sensitivity, following 24h treatment[2].
Cell Research Cell lines MV4-11 cells
Concentrations 0.1 nM, 1 nM, and 10 nM
Incubation Time 2 h
Method

MV4-11 cells are treated with DMSO or increasing concentrations of gilteritinib for 2 hours. Immunoprecipitation and immunoblot for phosphorylated FLT3 and total FLT3 are performed.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-STAT5 / STAT5 / p-AKT / AKT / p-ERK / ERK p-c-kit / c-kit p-FLT3(Y591) / FLT3 28516360
In Vivo
In vivo In vivo, gilteritinib is distributed at high levels in xenografted tumors after oral administration. The decreased FLT3 activity and high intratumor distribution of gilteritinib translates to tumor regression and improved survival in xenograft and intra-bone marrow transplantation models of FLT3-driven AML. This antitumor activity is associated with a durable inhibition of phospho-FLT3 and phospho-STAT5. Furthermore, treatment with gilteritinib decreases the leukemic burden and prolongs survival in a mouse IBMT model. No overt toxicity is seen in mouse models treated with gilteritinib[1].
Animal Research Animal Models MV4-11 xenografted mice (Nude mice)
Dosages 1 mg/kg, 6 mg/kg, and 10 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06022003 Recruiting
AML Adult|Refractory AML|Relapsed Adult AML|FLT3-TKD Mutation|FLT3-ITD
French Innovative Leukemia Organisation|Acute Leukemia French Association
 January 13 2024 Phase 2
NCT05520567 Recruiting
Acute Myeloid Leukemia (AML)|FLT3-mutated Acute Myeloid Leukemia
Astellas Pharma Global Development Inc.|Astellas Pharma Inc
 January 27 2023 Phase 1|Phase 2
NCT05791890 Active not recruiting
Acute Myeloid Leukemia
University of Rome Tor Vergata
 May 31 2022 --

Chemical Information & Solubility

Molecular Weight 552.71 Formula

C29H44N8O3
CAS No. 1254053-43-4 SDF Download Gilteritinib (ASP2215) SDF
Smiles CCC1=C(N=C(C(=N1)C(=O)N)NC2=CC(=C(C=C2)N3CCC(CC3)N4CCN(CC4)C)OC)NC5CCOCC5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 4 mg/mL ( (7.23 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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