GILTERITINIB (ASP2215)

Background Information:

Gilteritinib (ASP2215) is a potent FLT3/AXL inhibitor,
showingstronganti-leukemic activity against AML (Acute Myeloid
Leukemia)by acting on either or both FLT3-ITD and FLT3-D835 mutations.
In vitro at 1 nM concentration, among the 78 tyrosine kinases tested, it
hits FLT3, LTK, ALK, and AXL kinases by over 50% 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.
It inhibited the growth of MV4-11 cells harboring FLT3-ITD, with an IC50
value of 0.92 nM, accompanied with the inhibition of pFLT3, pAKT,
pSTAT5, pERK, and pS6. It decreased tumor burden in bone marrow and
prolonged the survival of mice intravenously transplanted with MV4-11
cells.

Reference:

1. *Soluble in 0.1 N HCl aqueous solution (28.5mg/ml, 50 mM).

APIM050155: GILTERITINIB (ASP2215)

CAS No.: 1254053-43-4.
Molecular Formula: C₂₉H₄₄N₈O₃ • H₂O.
Molecular Weight: 570.7 (or refer to Certificate of Analysis, batch-specific).
Purity: >99.5% (HPLCs at 220 and 254 nm).
QC: HPLC-MS, ¹HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.