1. Protein Tyrosine Kinase/RTK
  2. FLT3
    TAM Receptor

Gilteritinib (Synonyms: ASP2215)

Cat. No.: HY-12432 Purity: 99.55%
Data Sheet SDS Handling Instructions

Gilteritinib is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/<1 nM respectively.

For research use only. We do not sell to patients.
Gilteritinib Chemical Structure

Gilteritinib Chemical Structure

CAS No. : 1254053-43-4

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Gilteritinib is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/<1 nM respectively.

IC50 & Target

IC50: 0.29 nM (FLT3), <1 nM (AXL)[1]

In Vitro

Of the 78 tyrosine kinases tested, Gilteritinib (ASP2215) inhibits FLT3, LTK, 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, the inhibition of which is linked to a potential risk of myelosuppression. Gilteritinib inhibits the growth of MV4-11 cells, which harbor FLT3-ITD, with an IC50 value of 0.92 nM, accompanied with inhibition of pFLT3, pAKT, pSTAT5, pERK, and pS6. Gilteritinib also inhibits the growth of Ba/F3 cells expressing FLT3-ITD and/or FLT3-D835 mutation with similar activity. Colony formation of human granulocyte-macrophage decreased to 58% in response to Gilteritinib at 100 nM, more than 100-fold higher than required for MV4-11. Gilteritinib shows potent antileukemic activity against AML with either or both FLT3-ITD and FLT3-D835 mutations[1]. Gilteritinib is a FLT3/AXL tyrosine kinase inhibitor. It inhibits the function of FLT3 and AXL, molecules involved in the growth of cancer cells. Additionally, Gilteritinib also inhibits AXL, a known resistance mechanism to chemotherapies in a variety of solid and hematological malignancies[2].

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].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02571816 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Healthy|Hepatic Impairment October 2015 Phase 1
NCT02181660 Astellas Pharma Inc Acute Myeloid Leukemia (AML) June 16, 2014 Phase 1
NCT02561455 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Advanced Solid Tumors|Acute Myeloid Leukemia April 28, 2016 Phase 1|Phase 2
NCT02014558 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Acute Myeloid Leukemia October 9, 2013 Phase 1|Phase 2
NCT02495233 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Non-Small-Cell Lung Cancer September 8, 2015 Phase 1|Phase 2
NCT03182244 Astellas Pharma Inc Acute Myeloid Leukemia With FMS-like Tyrosine Kinase (FLT3) Mutation September 2017 Phase 3
NCT02236013 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Acute Myeloid Leukemia January 7, 2015 Phase 1
NCT02752035 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Acute Myeloid Leukemia (AML)|Acute Myeloid Leukemia With FMS-like Tyrosine Kinase (FLT3) Mutation August 1, 2016 Phase 2|Phase 3
NCT02310321 Astellas Pharma Inc Acute Myeloid Leukemia February 26, 2015 Phase 1
NCT03070093 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Acute Myeloid Leukemia (AML)|FMS-like Tyrosine Kinase-3 (FLT3) Mutations
NCT02927262 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Acute Myeloid Leukemia (AML)|Acute Myeloid Leukemia With FMS-like Tyrosine Kinase (FLT3) / Internal Tandem Duplication (ITD) Mutation January 10, 2017 Phase 3
NCT02421939 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Leukemia, Acute Myeloid (AML) October 20, 2015 Phase 3
NCT02571816 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Healthy|Hepatic Impairment October 2015 Phase 1
NCT02181660 Astellas Pharma Inc Acute Myeloid Leukemia (AML) June 16, 2014 Phase 1
NCT02561455 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Advanced Solid Tumors|Acute Myeloid Leukemia April 28, 2016 Phase 1|Phase 2
NCT02014558 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Acute Myeloid Leukemia October 9, 2013 Phase 1|Phase 2
NCT02495233 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Non-Small-Cell Lung Cancer September 8, 2015 Phase 1|Phase 2
NCT03182244 Astellas Pharma Inc Acute Myeloid Leukemia With FMS-like Tyrosine Kinase (FLT3) Mutation September 2017 Phase 3
NCT02236013 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Acute Myeloid Leukemia January 7, 2015 Phase 1
NCT02752035 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Acute Myeloid Leukemia (AML)|Acute Myeloid Leukemia With FMS-like Tyrosine Kinase (FLT3) Mutation August 1, 2016 Phase 2|Phase 3
NCT02310321 Astellas Pharma Inc Acute Myeloid Leukemia February 26, 2015 Phase 1
NCT03070093 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Acute Myeloid Leukemia (AML)|FMS-like Tyrosine Kinase-3 (FLT3) Mutations
NCT02927262 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Acute Myeloid Leukemia (AML)|Acute Myeloid Leukemia With FMS-like Tyrosine Kinase (FLT3) / Internal Tandem Duplication (ITD) Mutation January 10, 2017 Phase 3
NCT02421939 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Leukemia, Acute Myeloid (AML) October 20, 2015 Phase 3
NCT02997202 Astellas Pharma Global Development, Inc.|National Heart, Lung, and Blood Institute (NHLBI)|Blood and Marrow Transplant Clinical Trials Network|Astellas Pharma Inc Acute Myeloid Leukemia June 7, 2017 Phase 3
NCT02456883 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Advanced Solid Tumors|Pharmacokinetics of 14C-labeled Gilteritinib March 4, 2016 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Cell Assay
[1]

Gilteritinib is dissolved in DMSO and stored, and then diluted with appropriate media before use[1].

Antiproliferative activity is evaluated against several AML cell lines with assessment of the inhibition of pFLT3 and downstream molecules using Western blot and flow cytometry[1]. 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 ASP2215 at 10 mg/kg for 4 days. Treatment of ASP2215 for 28 days results in dose-dependent inhibition of MV4-11 tumor growth and induces complete tumor regression at more than 6 mg/kg. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

552.71

Formula

C₂₉H₄₄N₈O₃

CAS No.

1254053-43-4

Storage

Powder4°C, stored under nitrogen

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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