Art. -Nr.: HY-12432

Gilteritinib

(Synonyms: ASP2215)

44 Cited Publications

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Based on 44 publication(s) in Google Scholar

Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC₅₀s of 0.29 nM/0.73 nM, respectively.

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Reinheit: 99.84%
CAS. Nr.: 1254053-43-4
Formel: C₂₉H₄₄N₈O₃
Molecular Weight:552.71

Speicherung:

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Gilteritinib Chemical Structure

CAS. Nr.: 1254053-43-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (44)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
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Biologische Aktivität

Beschreibung

Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC₅₀s of 0.29 nM/0.73 nM, respectively.

IC₅₀ & Target

Axl

Alle TAM Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.7 nM Compound: Gilteritinib	Antiproliferative activity against mouse BaF3 FLT3-D835 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 FLT3-D835 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 32659083]
BaF3	IC₅₀	1.6 nM Compound: Gilteritinib	Antiproliferative activity against mouse BaF3 FLT3-ITD cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 FLT3-ITD cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 32659083]
BaF3	IC₅₀	1.8 nM Compound: 7; ASP2215	Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD by cell-titre glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD by cell-titre glo luminescent cell viability assay	[PMID: 33719439]
BaF3	IC₅₀	2.1 nM Compound: 7; ASP2215	Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-D835Y mutant by cell-titre glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-D835Y mutant by cell-titre glo luminescent cell viability assay	[PMID: 33719439]
BaF3	IC₅₀	7.6 nM Compound: 1	Antiproliferative activity against mouse BaF3/TEL-AXL cells incubated for 72 hrs by SRB or CCK8 assay Antiproliferative activity against mouse BaF3/TEL-AXL cells incubated for 72 hrs by SRB or CCK8 assay	[PMID: 33733758]
BaF3	GI₅₀	2 nM Compound: ASP-2215	Antiproliferative activity against mouse Ba/F3 cells harbouring FLT3 D835Y mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring FLT3 D835Y mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
BaF3	GI₅₀	258.6 nM Compound: ASP-2215	Antiproliferative activity against mouse Ba/F3 cells harbouring FLT3 ITD F691I mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring FLT3 ITD F691I mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
BaF3	GI₅₀	5 nM Compound: ASP-2215	Antiproliferative activity against mouse Ba/F3 cells harbouring FLT3 ITD D835Y mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring FLT3 ITD D835Y mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
BaF3	GI₅₀	82.8 nM Compound: ASP-2215	Antiproliferative activity against mouse Ba/F3 cells harbouring FLT3 ITD F691L mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring FLT3 ITD F691L mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
BaF3	GI₅₀	1.6 nM Compound: 3e	Growth inhibition of mouse BaF3 cells transfected with FLT3-D835Y assessed as inhibition of cell growth measured after 48 hrs by MTT assay Growth inhibition of mouse BaF3 cells transfected with FLT3-D835Y assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 35923716]
BaF3	GI₅₀	1.8 nM Compound: 3e	Growth inhibition of mouse BaF3 cells transfected with FLT3-ITD assessed as inhibition of cell growth measured after 48 hrs by MTT assay Growth inhibition of mouse BaF3 cells transfected with FLT3-ITD assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 35923716]
BaF3	IC₅₀	0.48 nM Compound: Gilteritinib	Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD-D835Y mutant assessed as inhibition of cell growth Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD-D835Y mutant assessed as inhibition of cell growth	[PMID: 37838343]
BaF3	IC₅₀	0.6 nM Compound: Gilteritinib	Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD mutant assessed as inhibition of cell growth Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD mutant assessed as inhibition of cell growth	[PMID: 37838343]
BaF3	IC₅₀	0.62 nM Compound: Gilteritinib	Antiproliferative activity against mouse BaF3 cells harboring FLT3-D835V mutant assessed as inhibition of cell growth Antiproliferative activity against mouse BaF3 cells harboring FLT3-D835V mutant assessed as inhibition of cell growth	[PMID: 37838343]
BaF3	IC₅₀	0.66 nM Compound: Gilteritinib	Antiproliferative activity against mouse BaF3 cells harboring FLT3-D835F mutant assessed as inhibition of cell growth Antiproliferative activity against mouse BaF3 cells harboring FLT3-D835F mutant assessed as inhibition of cell growth	[PMID: 37838343]
BaF3	IC₅₀	1.05 nM Compound: Gilteritinib	Antiproliferative activity against mouse BaF3 cells harboring FLT3-F691L mutant assessed as inhibition of cell growth Antiproliferative activity against mouse BaF3 cells harboring FLT3-F691L mutant assessed as inhibition of cell growth	[PMID: 37838343]
CCRF-CEM	GI₅₀	2.771 μM Compound: Gilteritinib	Antiproliferative activity against FLT3-independent human CEM cells assessed as cell growth inhibition by resorufin dye based fluorescence analysis Antiproliferative activity against FLT3-independent human CEM cells assessed as cell growth inhibition by resorufin dye based fluorescence analysis	[PMID: 37535845]
HeLa	IC₅₀	3201 nM Compound: Gilteritinib	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth	[PMID: 37838343]
HepG2	GI₅₀	2.2 μM Compound: 8	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by WST assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by WST assay	[PMID: 32272419]
K562	GI₅₀	1.006 μM Compound: 8	Antiproliferative activity against human K562 cells assessed as cell growth inhibition by WST assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition by WST assay	[PMID: 32272419]
K562	GI₅₀	2.254 μM Compound: Gilteritinib	Antiproliferative activity against FLT3-independent human K562 cells assessed as cell growth inhibition by resorufin dye based fluorescence analysis Antiproliferative activity against FLT3-independent human K562 cells assessed as cell growth inhibition by resorufin dye based fluorescence analysis	[PMID: 37535845]
K562	IC₅₀	>1000 nM Compound: Gilteritinib	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay	[PMID: 38056299]
Kasumi 1	GI₅₀	0.124 μM Compound: Gilteritinib	Antiproliferative activity against human Kasumi 1 cells harboring KIT N822K mutant assessed as cell growth inhibition by resorufin dye based fluorescence analysis Antiproliferative activity against human Kasumi 1 cells harboring KIT N822K mutant assessed as cell growth inhibition by resorufin dye based fluorescence analysis	[PMID: 37535845]
MCF7	IC₅₀	1296.13 nM Compound: Gilteritinib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth	[PMID: 37838343]
MM1.S	IC₅₀	203.47 nM Compound: Gilteritinib	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth	[PMID: 37838343]
MOLM-13	GI₅₀	0.004 μM Compound: Gilteritinib	Antiproliferative activity against drug-resistant human MOLM-13 cells expressing FLT3-ITD-D835Y mutant assessed as cell growth inhibition incubated for 72 hrs by resorufin dye based fluorescence analysis Antiproliferative activity against drug-resistant human MOLM-13 cells expressing FLT3-ITD-D835Y mutant assessed as cell growth inhibition incubated for 72 hrs by resorufin dye based fluorescence analysis	[PMID: 37535845]
MOLM-13	GI₅₀	0.005 μM Compound: Gilteritinib	Antiproliferative activity against FLT3-dependent human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by resorufin dye based fluorescence analysis Antiproliferative activity against FLT3-dependent human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by resorufin dye based fluorescence analysis	[PMID: 37535845]
MOLM-13	GI₅₀	0.034 μM Compound: Gilteritinib	Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as cell growth inhibition by resorufin dye based fluorescence analysis Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as cell growth inhibition by resorufin dye based fluorescence analysis	[PMID: 37535845]
MOLM-13	IC₅₀	0.77 nM Compound: Gilteritinib	Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth	[PMID: 37838343]
MOLM-13	IC₅₀	10917.3 nM Compound: Gilteritinib	Antiproliferative activity against Sunitinib-resistant human MOLM-13 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against Sunitinib-resistant human MOLM-13 cells incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
MOLM-13	IC₅₀	2321 nM Compound: Gilteritinib	Antiproliferative activity against Quizartinib-resistant human MOLM-13 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against Quizartinib-resistant human MOLM-13 cells incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
MOLM-13	IC₅₀	67.5 nM Compound: Gilteritinib	Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
MOLM-14	GI₅₀	1.91 nM Compound: 8	Antiproliferative activity against human MOLM14 cells harboring ITD/D835Y mutant assessed as cell growth inhibition by MTT assay Antiproliferative activity against human MOLM14 cells harboring ITD/D835Y mutant assessed as cell growth inhibition by MTT assay	[PMID: 32272419]
MOLM-14	GI₅₀	3.29 nM Compound: 8	Antiproliferative activity against human MOLM14 cells harboring ITD mutant assessed as cell growth inhibition by MTT assay Antiproliferative activity against human MOLM14 cells harboring ITD mutant assessed as cell growth inhibition by MTT assay	[PMID: 32272419]
MOLM-14	GI₅₀	4.94 nM Compound: 8	Antiproliferative activity against wild type human MOLM14 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against wild type human MOLM14 cells assessed as cell growth inhibition by MTT assay	[PMID: 32272419]
MOLM-14	GI₅₀	5.24 nM Compound: 8	Antiproliferative activity against human MOLM14 cells harboring ITD/F691L mutant assessed as cell growth inhibition by MTT assay Antiproliferative activity against human MOLM14 cells harboring ITD/F691L mutant assessed as cell growth inhibition by MTT assay	[PMID: 32272419]
MOLM-14	IC₅₀	1.8 nM Compound: Gilteritinib	Antiproliferative activity against human MOLM-14 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human MOLM-14 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 32659083]
MOLM-14	IC₅₀	5.47 nM Compound: Gilteritinib	Antiproliferative activity against human MOLM-14 cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against human MOLM-14 cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay	[PMID: 38056299]
MOLM-14	IC₅₀	58.78 nM Compound: Gilteritinib	Antiproliferative activity against human MOLM-14 cells harboring FLT3-F691L mutant assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against human MOLM-14 cells harboring FLT3-F691L mutant assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay	[PMID: 38056299]
MOLM-14	IC₅₀	7.83 nM Compound: Gilteritinib	Antiproliferative activity against human MOLM-14 cells harboring FLT3-D835Y mutant assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against human MOLM-14 cells harboring FLT3-D835Y mutant assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay	[PMID: 38056299]
MV4-11	GI₅₀	0.0009 μM Compound: 8	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition by Celltiter-Glo luminescent assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition by Celltiter-Glo luminescent assay	[PMID: 32272419]
MV4-11	GI₅₀	0.9 nM Compound: 8	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition by Celltiter-Glo luminescent assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition by Celltiter-Glo luminescent assay	[PMID: 32272419]
MV4-11	GI₅₀	0.002 μM Compound: Gilteritinib	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by resazurin assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by resazurin assay	[PMID: 33516985]
MV4-11	GI₅₀	0.026 μM Compound: Gilteritinib	Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as cell growth inhibition by resorufin dye based fluorescence analysis Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as cell growth inhibition by resorufin dye based fluorescence analysis	[PMID: 37535845]
MV4-11	IC₅₀	1.179 nM Compound: Gilteritinib	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37544183]
MV4-11	IC₅₀	1.34 nM Compound: Gilteritinib	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth	[PMID: 37838343]
MV4-11	GI₅₀	2.9 nM Compound: 4	Growth inhibition of human MV4-11 cells measured after 72 hrs by alamar blue cell viability assay Growth inhibition of human MV4-11 cells measured after 72 hrs by alamar blue cell viability assay	[PMID: 37866334]
MV4-11	IC₅₀	6.89 nM Compound: 6; S7754	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 38007910]
MV4-11	IC₅₀	40.2 nM Compound: Gilteritinib	Antiproliferative activity against human MV4-11 cells expressing FLT3-ITD mutant incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells expressing FLT3-ITD mutant incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
MV4-11	IC₅₀	0.9 nM Compound: 9	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability by WAT-8 reagent based analysis Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability by WAT-8 reagent based analysis	[PMID: 39094274]
NOMO-1	GI₅₀	1.601 μM Compound: Gilteritinib	Antiproliferative activity against FLT3-independent human NOMO-1 cells assessed as cell growth inhibition by resorufin dye based fluorescence analysis Antiproliferative activity against FLT3-independent human NOMO-1 cells assessed as cell growth inhibition by resorufin dye based fluorescence analysis	[PMID: 37535845]
PBMC	IC₅₀	7027.5 nM Compound: Gilteritinib	Antiproliferative activity against human PBMC cells assessed as inhibition of cell growth Antiproliferative activity against human PBMC cells assessed as inhibition of cell growth	[PMID: 37838343]
Vero	CC₅₀	37.16 μM Compound: Gilteritinib	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	6.76 μM Compound: Gilteritinib	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730
Vero C1008	CC₅₀	>500 nM Compound: 20	Cytotoxicity against African green monkey Vero E6 cells Cytotoxicity against African green monkey Vero E6 cells	[PMID: 33539089]

In Vitro

Of the 78 tyrosine kinases tested, Gilteritinib (ASP2215) inhibits FLT3, leukocyte tyrosine kinase (LTK), anaplastic lymphoma kinase (ALK), and AXL kinases by over 50% at 1 nM with an IC₅₀ value of 0.29 nM for FLT3, approximately 800-fold more potent than for c-KIT^[1]. 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). The IC₅₀s are 0.29 nM for FLT3 and 0.73 nM for AXL. Gilteritinib inhibits FLT3 at an IC₅₀ that is approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM). The antiproliferative activity of Gilteritinib is evaluated against MV4-11 and MOLM-13 cells, which endogenously express FLT3-ITD. After 5 days of treatment, Gilteritinib inhibits the growth of MV4-11 and MOLM-13 cells with mean IC₅₀s of 0.92 nM (95% CI: 0.23-3.6 nM) and 2.9 nM (95% CI: 1.4-5.8 nM), respectively. Growth suppression of MV4-11 cells is accompanied by inhibition of FLT3 phosphorylation. Relative to vehicle control cells, phosphorylated FLT3 levels are 57%, 8%, and 1% after 2 h of treatment with 0.1 nM, 1 nM, and 10 nM Gilteritinib, respectively. In addition, doses as low as 0.1 nM or 1 nM result in the suppression of phosphorylated ERK, STAT5, and AKT, all of which are downstream targets of FLT3 activation. To investigate the effects of Gilteritinib on AXL inhibition, MV4-11 cells that expressed exogenous AXL are treated with Gilteritinib. At concentrations of 1 nM, 10 nM, and 100 nM for 4 h, Gilteritinib treatment decreases phosphorylated AXL levels by 38%, 29%, and 22%, respectively^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In MV4-11 xenografted-mice, the concentration of Gilteritinib (ASP2215) in tumors is more than 20-fold higher than that in plasma with oral administration of Gilteritinib at 10 mg/kg for 4 days. Treatment of Gilteritinib for 28 days results in dose-dependent inhibition of MV4-11 tumor growth and induces complete tumor regression at more than 6 mg/kg. Further, Gilteritinib decreases tumor burden in bone marrow and prolonged the survival of mice intravenously transplanted with MV4-11 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1254053-43-4
Appearance Solid
Molecular Weight 552.71
Formel C₂₉H₄₄N₈O₃
Color Light yellow to yellow
SMILES

NC(C1=NC(CC)=C(NC2CCOCC2)N=C1NC3=CC(OC)=C(N4CCC(N5CCN(C)CC5)CC4)C=C3)=O
Synonyms

ASP2215
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Publications (44)

All Flow CytometryRT-PCRIn Vivo Efficacy StudyWBCell Proliferation/Viability Assay

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Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878

Gilteritinib purchased from MedChemExpress. Usage Cited in: Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]

Western blot readout for phospho-SMAD in U-2 OS cells treated with inhibitor Gilteritinib (1 µM; 30 min) in the presence or absence of BMP2. S
Cancer Cell

In vivo models of subclonal oncogenesis and dependency in hematopoietic malignancy. [Abstract]

2024 Nov 11;42(11):1955-1969.e7. PMID: 39532065

Gilteritinib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 Nov 11;42(11):1955-1969.e7. [Abstract]

Kaplan-Meier survival curve of mice engrafted with Cd45.1 WT cells and bone marrow cells from symptomatic Npm1Lox-C-Flt3GL-ITD mice. Mice were treated with control chow (grey). placed on a Tamoxifen chow diet (red) for 4 weeks, or treated with gilteritinib (p.o.; 60 mg/kg; three times weekly) for 4 weeks (green); treatment was withdrawn at the indicated time point (n=7–10).
Cancer Discov

C/EBPa confers dependence to fatty acid anabolic pathways and vulnerability to lipid oxidative stress-induced ferroptosis in FLT3-mutant leukemia. [Abstract]

2023 Jul 7;13(7):1720-1747. PMID: 37012202
Nat Cancer

Targeting a lineage-specific PI3Kɣ-Akt signaling module in acute myeloid leukemia using a heterobifunctional degrader molecule. [Abstract]

2024 Jul;5(7):1082-1101. PMID: 38816660

Gilteritinib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2024 Jul;5(7):1082-1101. [Abstract]

Growth inhibition, IC50 and AUC values, of OCI-AML2 cells transduced with either a non-targeting control, two PIK3CG-directed, or two PIK3R5-directed sgRNAs and treated with increasing concentrations of the FLT3 inhibitors, Gilteritinib (10-1000 nM) and Sorafenib (10-1000 nM), or KIT inhibitors, Amuvanib and Telatinib
Hemasphere

CEBP and ZEB2 alterations define three distinct subtypes of B-cell acute lymphoblastic leukemia. [Abstract]

2026 Jun 15;10(6):e70383. PMID: 42306066
Acta Pharm Sin B

2026 Feb 10.
Autophagy

Inhibition of PINK1 senses ROS signaling to facilitate neuroblastoma cell pyroptosis. [Abstract]

2025 Mar 31. PMID: 40160153
Sci Adv

Targeting OXPHOS de novo purine synthesis as the nexus of FLT3 inhibitor-mediated synergistic antileukemic actions. [Abstract]

2022 Sep 16;8(37):eabp9005. PMID: 36112677

Gilteritinib purchased from MedChemExpress. Usage Cited in: Sci Adv. 2022 Sep 16;8(37):eabp9005. [Abstract]

Knockdown of CDK9 or DHODH but not CDK7 with shRNA increases the frequency of apoptotic AML cell lines with Gilteritinib. Parental, scrambled, or gene-targeting shRNA-stable MOLM-13 cells were treated with Gileritinib (8 nM ; 120 h) and stained with annexin V/PI for flow cytometry analysis.

Gilteritinib purchased from MedChemExpress. Usage Cited in: Sci Adv. 2022 Sep 16;8(37):eabp9005. [Abstract]

The relative expressions of selected genes in pro-proliferation/anti-apoptosis, OXPHOS, purine de novo biosynthesis, mevalonate metabolism, glycolysis, and glutamine transport pathways and PTK2, KRT18, and PRMT5 in scrambled, shCDK9-, shPRMT5-, and shDHODH-stable MOLM-13 in response to vehicle or Gilteritinib (8 nM; 48-96 h) treatment were measure by real-time PCR with respect to GAPDH. Values are expressed as fold changes (means ± SEM, n = 3) relative to vehicle-treated scrambled cells. *P < 0.05 and **P < 0.01. Treatment durations are indicated.
Blood Cancer J

Superior preclinical efficacy of co-treatment with BRG1/BRM and FLT3 inhibitor against AML cells with FLT3 mutations. [Abstract]

2025 Mar 15;15(1):40. PMID: 40089460
Blood Cancer J

Effective Menin inhibitor-based combinations against AML with MLL rearrangement or NPM1 mutation (NPM1c). [Abstract]

2022 Jan 11;12(1):5. PMID: 35017466
J Control Release

Antibody-mediated ratiometric delivery of FLT3 and CDK4/6 dual inhibitors for targeted treatment of acute myeloid leukemia. [Abstract]

2025 Jun 5:113934. PMID: 40482924
J Control Release

Lipopolymer mediated siRNA delivery targeting aberrant oncogenes for effective therapy of myeloid leukemia in preclinical animal models. [Abstract]

2024 Mar:367:821-836. PMID: 38360178
Blood Cancer Discov

ZNF384 Fusion Oncoproteins Drive Lineage Aberrancy in Acute Leukemia. [Abstract]

2022 May 5;3(3):240-263. PMID: 35247902
Cell Rep Med

Metformin synergizes with gilteritinib in treating FLT3-mutated leukemia via targeting PLK1 signaling. [Abstract]

2024 Jul 16;5(7):101645. PMID: 39019012
Cancer Lett

FLT3-selective PROTAC: Enhanced safety and increased synergy with Venetoclax in FLT3-ITD mutated acute myeloid leukemia. [Abstract]

2024 Jun 28:592:216933. PMID: 38705564
Acta Biomater

Lipopolymer/siRNA complexes engineered for optimal molecular and functional response with chemotherapy in FLT3-mutated acute myeloid leukemia. [Abstract]

2024 Sep 3:S1742-7061(24)00505-1. PMID: 39236794
Haematologica

MDM2- and FLT3-inhibitors in the treatment of FLT3-ITD acute myeloid leukemia, specificity and efficacy of NVP-HDM201 and midostaurin. [Abstract]

2018 Nov;103(11):1862-1872. PMID: 29976747
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
Biomed Pharmacother

Gilteritinib reverses ABCB1-mediated multidrug resistance: Preclinical in vitro and animal investigations. [Abstract]

2024 Oct 28:180:117603. PMID: 39471652
Biomed Pharmacother

PLM-101 is a novel and potent FLT3/RET inhibitor with less adverse effects in the treatment of acute myeloid leukemia. [Abstract]

2023 Sep:165:115066. PMID: 37392657
Cell Rep

Targeting systemic and tumor metabolic balances with ketogenic diets enhance efficacy of therapy in FLT3-ITD acute myeloid leukemia. [Abstract]

2026 Mar 28;45(4):117185. PMID: 41904949
Cell Rep

Phosphoproteomic subtyping of gastric cancer reveals dynamic transformation with chemotherapy and guides targeted cancer treatment. [Abstract]

2024 Sep 25:114774. PMID: 39357518
Comput Biol Med

Synergy and antagonism between azacitidine and FLT3 inhibitors. [Abstract]

2024 Feb:169:107889. PMID: 38199214
Cancer Cell Int

Arsenic trioxide potentiates Gilteritinib-induced apoptosis in FLT3-ITD positive leukemic cells via IRE1a-JNK-mediated endoplasmic reticulum stress. [Abstract]

2020 Jun 17;20:250. PMID: 32565734

Gilteritinib purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2020 Jun 17;20:250. [Abstract]

MV4-11 and MOLM13 cells are treated with Gilteritinib (2.5 nM) and/or ATO (0.5 µM) for 48 h and protein levels of P-FLT3 and FLT3 are determined by Western blot. Gilteritinib exhibits a strong inhibition on the phosphorylated FLT3 even at a low concentration of 2.5 nM, but had little effect on total FLT3 and USP10.

Gilteritinib purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2020 Jun 17;20:250. [Abstract]

Proliferation assay demonstrates that FLT3-ITD mutant cells (MV4-11 and MOLM13) are more sensitive to Gilteritinib compared with FLT3-WT cells (THP1 and HL60).
Cell Biol Toxicol

RNF38 promotes gilteritinib resistance in acute myeloid leukemia via inducing autophagy by regulating ubiquitination of LMX1A. [Abstract]

2024 Nov 28;40(1):105. PMID: 39604755
Eur J Med Chem

Discovery of indirubin-3'-aminooxy-acetamide derivatives as potent and selective FLT3/D835Y mutant kinase inhibitors for acute myeloid leukemia. [Abstract]

2022 Jul 5;237:114356. PMID: 35489222
Polymers

Potentiating Gilteritinib Efficacy Using Nanocomplexation with a Hyaluronic Acid-Epigallocatechin Gallate Conjugate. [Abstract]

2024 Jan 12;16(2):225. PMID: 38257023
Front Pharmacol

Influence of YES1 Kinase and Tyrosine Phosphorylation on the Activity of OCT1. [Abstract]

2021 Mar 8;12:644342. PMID: 33790797
Eur J Pharm Sci

Design, synthesis, formulation, and bioevaluation of ZZP-2, a FLT3-ITD inhibitor for the treatment of acute myeloid leukemia. [Abstract]

2026 Mar 1:218:107440. PMID: 41520929
Mol Cancer Res

GATM-Mediated Creatine Biosynthesis Enables Maintenance of FLT3-ITD-Mutant Acute Myeloid Leukemia. [Abstract]

2022 Feb;20(2):293-304. PMID: 34635505
Cancers

The FMS like Tyrosine Kinase 3 (FLT3) Is Overexpressed in a Subgroup of Multiple Myeloma Patients with Inferior Prognosis. [Abstract]

2020 Aug 19;12(9):2341. PMID: 32825035
Cancers

Cotargeting of XPO1 Enhances the Antileukemic Activity of Midostaurin and Gilteritinib in Acute Myeloid Leukemia. [Abstract]

2020 Jun 14;12(6):1574. PMID: 32545904
Pharm Res

Preclinical Prediction of Resistance Mutations and Proposal of Sequential Treatment Strategies for ALK-positive Lung Cancer Using Next-generation ALK Inhibitors. [Abstract]

2025 Sep;42(9):1497-1509. PMID: 40993323
Target Oncol

Prediction of Resistance Mutations Against Upcoming Anaplastic Lymphoma Kinase Inhibitors. [Abstract]

2022 Nov;17(6):695-707. PMID: 36201110
Sci Rep

Targeted therapy of human leukemia xenografts in immunodeficient zebrafish. [Abstract]

2021 Mar 11;11(1):5715. PMID: 33707624
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
Expert Rev Clin Immunol

TFDP1 activates SPC25-mediated glutamine metabolism to repress anti-tumor immunity of NK cells in lung adenocarcinoma. [Abstract]

2025 Jun 25:1-11. PMID: 40552366
Cancer Res Commun

Pim kinase inhibitors increase gilteritinib cytotoxicity in FLT3-ITD acute myeloid leukemia through GSK-3β activation and c-Myc and Mcl-1 proteasomal degradation. [Abstract]

2024 Feb 16;4(2):431-445. PMID: 38284896
Mol Pharmacol

Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake. [Abstract]

2022 Jun;101(6):381-389. PMID: 35383108
Separations

2023 Apr 25, 10(5), 278.
bioRxiv

2025 May 29.
Research Square Preprint

2023 Dec 6.
J Oncol

Homoharringtonine Synergized with Gilteritinib Results in the Downregulation of Myeloid Cell Leukemia-1 by Upregulating UBE2L6 in FLT3-ITD-Mutant Acute Myeloid (Leukemia) Cell Lines. [Abstract]

2021 Sep 21:2021:3766428. PMID: 34594375
Charles University

2020 Jul.

Lösungsmittel & Löslichkeit

In Vitro:

Ethanol : 100 mg/mL (180.93 mM; ultrasonic and adjust pH to 2 with HCl)

DMSO : 2 mg/mL (3.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8093 mL

9.0463 mL

18.0927 mL

5 mM

0.3619 mL

1.8093 mL

3.6185 mL

10 mM

0.1809 mL

0.9046 mL

1.8093 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (18.09 mM); Suspended solution; Need ultrasonic

Protokoll

Kinase Assay^[2]

The kinase inhibitory activity of Gilteritinib is tested against a panel of 78 tested kinases using ATP concentrations that are approximately equal to the K_m value for each kinase in a TK-ELISA or off-chip mobility shift assay. Initially, two concentrations of Gilteritinib (1 nM and 5 nM) are tested to assess each compound’s inhibitory effect on TK activity. Further studies are then conducted using a dose range of Gilteritinib to determine IC₅₀ values for kinases in which activity is inhibited by >50% with 1 nM Gilteritinib as well as for c-KIT. TK-ELISA and MSA assays are used to conduct IC₅₀ studies for FLT3, LTK, AXL, and c-KIT; the HTRF KinEASE-TK assay is performed to assess the IC₅₀ value of echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[2]

The effect of Gilteritinib on MV4-11 and MOLM-13 cells is assessed using the CellTiter-Glo Luminescent Cell Viability Assay. Subsequent studies are conducted to examine the effect of Gilteritinib and Quizartinib on Ba/F3 cells expressing either FLT3-ITD, FLT3-D835Y, FLT3-ITD-D835Y, FLT3-ITD-F691 L, or FLT3-ITD-F691I. MV4-11 and MOLM-13 cells are treated with DMSO or increasing concentrations of Gilteritinib (0.01, 0.1, 1, 10, and 100 nM) for 5 days, and cell viability is measured using CellTiter-Glo^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
Antitumor activity is evaluated in nude mice transplanted with MV4-11 AML cells. The pharmacokinetics in xenografted mice is also investigated. MV4-11 xenografted-mice are treated with oral administration of Gilteritinib at 10 mg/kg for 4 days. Treatment of Gilteritinib for 28 days results in dose-dependent inhibition of MV4-11 tumor growth and induces complete tumor regression at more than 6 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. ASP2215, a novel FLT3/AXL inhibitor: Preclinical evaluation in acute myeloid leukemia (AML). 2014 ASCO Annual Meeting.

[2]. Mori M, et al. Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3 mutated acute myeloid leukemia. Invest New Drugs. 2017 Oct;35(5):556-565. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	1.8093 mL	9.0463 mL	18.0927 mL	45.2317 mL
Ethanol	5 mM	0.3619 mL	1.8093 mL	3.6185 mL	9.0463 mL
	10 mM	0.1809 mL	0.9046 mL	1.8093 mL	4.5232 mL
	15 mM	0.1206 mL	0.6031 mL	1.2062 mL	3.0154 mL
	20 mM	0.0905 mL	0.4523 mL	0.9046 mL	2.2616 mL
	25 mM	0.0724 mL	0.3619 mL	0.7237 mL	1.8093 mL
	30 mM	0.0603 mL	0.3015 mL	0.6031 mL	1.5077 mL
	40 mM	0.0452 mL	0.2262 mL	0.4523 mL	1.1308 mL
	50 mM	0.0362 mL	0.1809 mL	0.3619 mL	0.9046 mL
	60 mM	0.0302 mL	0.1508 mL	0.3015 mL	0.7539 mL
	80 mM	0.0226 mL	0.1131 mL	0.2262 mL	0.5654 mL
	100 mM	0.0181 mL	0.0905 mL	0.1809 mL	0.4523 mL

Keywords

Gilteritinib

44 Cited Publications

100 mg Angebot einholen

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Gilteritinib

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Publications Citing Use of MedChemExpress (MCE) Gilteritinib

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Biologische Aktivität

Chemical Information

Publications (44)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Gilteritinib Related Classifications

Art. -Nr.: HY-12432