Gilteritinib (ASP2215)

Catalog No.S7754

Gilteritinib (ASP2215) Chemical Structure

Molecular Weight(MW): 552.71

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).

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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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV4-11 cells NG\BNnpE\WyuIHP5Z4xmKGG|c3H5 MYmxMEA{NCBzMDygZY5lKDNyIH7N NELHWIszPCCq NGi1OYJVcGVibXXhckBxem:yb4L0bY9vKG:oIF3WOE0yOSClZXzsd{BqdiCJMTDwbIF{\SC5ZYLlJJNq\26rZnnjZY51dHliaX7jdoVie2WmIHH0JIdqdHSncnn0bY5q[iClb37j[Y51emG2aX;ud{Bw\iB|IDi2PU4xLTtiUEywMlAyMSCjbnSgNVAhdk1iKEewMlcmQyCSPECuNFAyMS5? M1;sd|MyODZ7MEG1
MOLM-13 cells NXr2TXF2SXCxcITvd4l{KGG|c3H5 MYSxMEA{NCBzMDygN|AtKGGwZDCxNFAhdk1? M3rudFQ5KGh? NFXIc4Z{cWewaX\pZ4FvfCCrbnPy[YF{\XNiaX6geIhmKHCncnPlcpRi\2Vib3[gZY5v\XirbjDWMZBwe2m2aY\lJINmdGy|IHH0JINwdmOnboTyZZRqd26|IH;mJFMxKG6PIDizNk4xLSliYX7kJFExOCCwTTCoOVIvPCVrII\ldpN2eyClb370do9tKCh2LkGlLS=> NIfh[mo{OTB4OUCxOS=>
32D/TKD cells NUX4UHFlTnWwY4Tpc44h[XO|YYm= Ml;ROVAhdk4EoB?= MlToOkBp NFG0Z4tKdmirYnn0c44hd2ZidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBCc3Rib36gWFMxQA>? Ml\kNlk2ODd4NkC=
TF-1 cells MWfGeY5kfGmxbjDhd5NigQ>? NIDaTmQxNCB{MDygPFAtKDJyMDDhcoQhPTByIH7N NVzrVGVpOSCq NUjwWVU1\2mudHXybZRqdmmkIHjhd{BidiCLQ{WwJIFo[Wmwc4Sge4lt\C22eYDlJIMuU2m2IH;mJFExOiCwTR?= MWGyO|kxQDh6MR?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT5 / STAT5 / p-AKT / AKT / p-ERK / ERK; 

PubMed: 28516360     


Immunoblot for phosphorylated AKT, ERK, and STAT5 in gilteritinib-treated MV4–11 cells. Blots from one study, which was done in triplicate, are shown.

p-c-kit / c-kit; 

PubMed: 27908881     


TF-1 cells were treated with increasing concentrations gilteritinib in RPMI/10% FBS for 1 hour. Immunoprecipitation and immunoblotting were performed to detect the phosphorylation status of c-Kit and total c-Kit.

p-FLT3(Y591) / FLT3; 

PubMed: 30344940     


Cells were treated with or without 10 nM gilteritinib, or midostaurin for 6 h, and immunoblotting was performed using the indicated antibodies.

28516360 27908881 30344940
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].

Protocol

Cell Research:

[1]

- Collapse
  • 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.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: MV4-11 xenografted mice (Nude mice)
  • Formulation: 0.5% methylcellulose solution
  • Dosages: 1 mg/kg, 6 mg/kg, and 10 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (180.92 mM)
Ethanol 85 mg/mL (153.78 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 552.71
Formula

C29H44N8O3

CAS No. 1254053-43-4
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03730012 Recruiting Drug: gilteritinib|Drug: atezolizumab Acute Myeloid Leukemia (AML)|Acute Myeloid Leukemia With FMS-like Tyrosine Kinase (FLT3) Mutation Astellas Pharma Global Development Inc.|Astellas Pharma Inc June 19 2019 Phase 1|Phase 2
NCT03964038 Completed Drug: gilteritinib|Drug: gilteritinib mini tablet Healthy Volunteer Astellas Pharma Global Development Inc.|Astellas Pharma Inc May 21 2019 Phase 1
NCT02456883 Completed Drug: gilteritinib|Drug: 14C-labeled gilteritinib Advanced Solid Tumors|Pharmacokinetics of 14C-labeled Gilteritinib Astellas Pharma Global Development Inc.|Astellas Pharma Inc March 4 2016 Phase 1
NCT02571816 Completed Drug: ASP2215 Hepatic Impairment|Healthy Astellas Pharma Global Development Inc.|Astellas Pharma Inc October 23 2015 Phase 1

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.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    Do you have recommendations for the formulation of giltertinib (ASP-2215) in mice (for in vivo studies)?

  • Answer:

    You can use "5% DMSO+40% PEG 300+5% Tween 80+ddH2O" clear at 5mg/ml as a IP formula.

FLT3 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID