Gilteritinib (Synonyms: ASP2215)

Name: Gilteritinib
Brand: MedChemExpress
SKU: HY-12432
Rating: 5.0 (32 reviews)

Cat. No.: HY-12432 Purity: 99.34%: FAQs
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Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC₅₀s of 0.29 nM/0.73 nM, respectively.

For research use only. We do not sell to patients.

Gilteritinib Chemical Structure

CAS No. : 1254053-43-4

Size	Price	Stock	Quantity
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
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Based on 32 publication(s) in Google Scholar

Other Forms of Gilteritinib:

30 Publications Citing Use of MCE Gilteritinib

Proliferation Assay

: 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).

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Axl Mer Tyro3

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Description

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

IC₅₀ & Target

Axl

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	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	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	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	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	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	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	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]
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]
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	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]
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	0.002 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]
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

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.

Clinical Trial

Molecular Weight

552.71

Formula

C₂₉H₄₄N₈O₃

CAS No.

1254053-43-4

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Volume _(start)

Concentration _(final)

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In Vivo:

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.69%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (249 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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]. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

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

Gilteritinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gilteritinib1254053-43-4ASP2215ASP 2215ASP-2215FLT3TAM ReceptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Tyro3AxlMerInhibitorinhibitorinhibit

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Gilteritinib (Synonyms: ASP2215)

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30 Publications Citing Use of MCE Gilteritinib

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Complete Stock Solution Preparation Table

Gilteritinib Related Classifications

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