Gilteritinib

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 10mg
ArtNr HY-12432-10mg
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
Synonyms
ASP2215, ASP-2215
CAS No.
1254053-43-4
Purity
>98%
MW
5527115
Formula
C29H44N8O3
Solubility
10 mM in DMSO
Biological 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].
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Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 10mg
Lieferbar: In stock
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Rabatt: -10,0%
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