Gilteritinib (ASP2215)
For research use only.
Catalog No.S7754
10 publications

CAS No. 1254053-43-4
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).
Purity & Quality Control
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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). | |||||||||||||||||||||||||||||||||||||
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Targets |
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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]. |
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Cell Data |
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Assay |
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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: |
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Animal Research: |
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Solubility (25°C)
In vitro | DMSO | 100 mg/mL (180.92 mM) |
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Water | Insoluble | |
Ethanol | '85 mg/mL |
* 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 |
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Formula | C29H44N8O3 |
CAS No. | 1254053-43-4 |
Storage |
powder in solvent |
Synonyms | N/A |
Smiles | CCC1=C(N=C(C(=N1)C(=O)N)NC2=CC(=C(C=C2)N3CCC(CC3)N4CCN(CC4)C)OC)NC5CCOCC5 |
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
Dosage | mg/kg | Average weight of animals | g | Dosing volume per animal | ul | Number of animals | ||||
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: : mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL,)
Method for preparing in vivo formulation:Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80,mix and clarify, next add μL ddH2O,mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Clinical Trial Information
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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NCT04140487 | Recruiting | Drug: Azacitidine|Drug: Gilteritinib|Drug: Venetoclax | Recurrent Acute Myeloid Leukemia|Recurrent Myelodysplastic Syndrome|Refractory Acute Myeloid Leukemia|Refractory Myelodysplastic Syndrome | M.D. Anderson Cancer Center|National Cancer Institute (NCI) | December 17 2019 | Phase 1|Phase 2 |
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 |
NCT03625505 | Recruiting | Drug: Venetoclax|Drug: Gilteritinib | Acute Myeloid Leukemia (AML) | AbbVie|Astellas Pharma Inc Genentech Inc. | October 18 2018 | 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.
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