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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $122 In-stock
5 mg $100 In-stock
10 mg $150 In-stock
50 mg $470 In-stock
100 mg $880 In-stock
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    Gilteritinib purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367). pii: eaan4368.

    Kinobead western Blot readout for selected inhibitor:protein combinations.

    Gilteritinib purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367). pii: eaan4368.

    Immunoblot analysis in MV-4-11 cells and MOLM-13, FLT3-WT and FLT3-ITD transfected HEK293 cells, and Ba/F3 FLT3-ITD cells revealed FLT3 target engagement for Golvatinib and Cabozantinib.

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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].

    References
    Preparing Stock Solutions
    Concentration Volume 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
    Please refer to the solubility information to select the appropriate solvent.
    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

    4°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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    Inquiry Information

    Product Name:
    Gilteritinib
    Cat. No.:
    HY-12432
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