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Chemical Structure| 1254053-43-4 Chemical Structure| 1254053-43-4

Structure of Gilteritinib
CAS No.: 1254053-43-4

Chemical Structure| 1254053-43-4

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Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM, respectively.

Synonyms: ASP2215

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Product Details of Gilteritinib

CAS No. :1254053-43-4
Formula : C29H44N8O3
M.W : 552.71
SMILES Code : O=C(C1=NC(CC)=C(NC2CCOCC2)N=C1NC3=CC=C(N4CCC(N5CCN(C)CC5)CC4)C(OC)=C3)N
Synonyms :
ASP2215
MDL No. :MFCD28144685
InChI Key :GYQYAJJFPNQOOW-UHFFFAOYSA-N
Pubchem ID :49803313

Safety of Gilteritinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Gilteritinib

RTK

Isoform Comparison

Biological Activity

Target
  • FLT3

    FLT3, IC50:0.29 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MOLM-13 15 nM BCL2 knockdown combined with gilteritinib significantly reduced cell viability PMC7574303
MV4-11 2.5–10 nM 48 h gilteritinib combined with venetoclax showed synergism in FLT3-ITD cell lines PMC7574303
MOLM-13 cells 0.232 nM 24 hours To evaluate the killing effect of Gilteritinib on AML cells, the results showed that Gilteritinib significantly increased the expression of NKG2DLs and FLT3. PMC8896098
MV4-11 cells 0.66 nM 24 hours To evaluate the killing effect of Gilteritinib on AML cells, the results showed that Gilteritinib significantly increased the expression of NKG2DLs and FLT3. PMC8896098
MOLM14 cells 100 nM 72 hours To evaluate the growth inhibitory effect of HSN748 on MOLM14 cells, results showed that HSN748 exhibited significant growth inhibition at low concentrations. PMC11178545
MOLM-13 12.5 nM 24 h To evaluate the apoptosis-inducing effect of combined Gilteritinib and CUDC-907 treatment on FLT3-ITD AML cell lines, the results showed that the combined treatment significantly induced apoptosis PMC8184771
MV4-11 12.5 nM 24 h To evaluate the apoptosis-inducing effect of combined Gilteritinib and CUDC-907 treatment on FLT3-ITD AML cell lines, the results showed that the combined treatment significantly induced apoptosis PMC8184771
MV4-11 10 nM 6 hours Using SILAC-based proteomics, the effect of FLT3 inhibitors on the nascent proteome was analyzed, revealing that Gilteritinib treatment increased the translation of autophagy-related proteins in MV4-11 cells. PMC9522593
MOLM-14 10 nM 6 hours Using SILAC-based proteomics, the effect of FLT3 inhibitors on the nascent proteome was analyzed, revealing that Gilteritinib treatment increased the translation of autophagy-related proteins in MOLM-14 cells. PMC9522593
32D-FLT3-ITD 0.2-100 nM 6 hours Flow cytometry analysis of GFP-LC3B/mCherry ratio revealed that Gilteritinib induced autophagy in FLT3-ITD-expressing 32D-FLT3-ITD cells in a concentration-dependent manner. PMC9522593

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice AML xenograft model Intraperitoneal injection 5mg/kg body weight Days 3, 8, 12, and 16, lasting 21 days To evaluate the therapeutic effect of Gilteritinib combined with FLT3scFv/NKG2D-CAR T cells on AML mice, the results showed that the combination therapy significantly reduced tumor burden and prolonged survival time. PMC8896098
Mice MOLM14 and MOLM14-FLT3ITD-F691L cell transplantation model Oral 40 mg/(kg·d) for 7 consecutive days To evaluate the antitumor effect of HSN748 in vivo, results showed that HSN748 significantly inhibited tumor growth and prolonged the survival of mice. PMC11178545
Mice MV4-11 xenograft model Oral 20 mg/kg Once daily for 6 weeks To evaluate the survival-prolonging effect of combined Gilteritinib and CUDC-907 treatment on FLT3-ITD AML mouse model, the results showed that the combined treatment significantly prolonged the survival of mice PMC8184771
Mice MV4-11R cell xenograft model Oral 25 mg/kg Ceritinib, 75 mg/kg SHP099 Daily, continuous treatment To evaluate the in vivo efficacy of Gilteritinib in combination with Defactinib in FLT3-mutated AML, showing that the combination significantly prolonged the time to leukemia symptom-related endpoint. PMC9522596
Mice NSG mice Oral 0.02 mmol/kg PA in 2.5 g/kg BSA Once daily for 10 days In NSG mice, the combination of Gilteritinib with the autophagy inhibitor ROC-325 significantly delayed leukemia progression and extended overall survival. PMC9522593

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT06734585 Acute Myeloid Leukemia RECRUITING 2025-06-30 HK852001, Hong Kong, Hong Kong
NCT03315299 AML NO_LONGER_AVAILABLE - Children's Hospital Los Angele... More >>s, Los Angeles, California, 90027, United States Less <<
NCT06667973 Acute Myeloid Leukemia|FLT3 Ge... More >>ne Mutation|Adult AML|Diagnosis Less << PHASE2 NOT_YET_RECRUITING 2025-03-30 -
NCT05791890 Acute Myeloid Leukemia ACTIVE_NOT_RECRUITING 2024-12-31 Maria Ilaria Del Principe, Rom... More >>a, RM, 00133, Italy Less <<
NCT02561455 Advanced Solid Tumors|Acute My... More >>eloid Leukemia Less << PHASE1|PHASE2 COMPLETED 2020-07-28 Site US10005, Phoenix, Arizona... More >>, 85084, United States|Site US10003, Baltimore, Maryland, 21201, United States|Site US10006, New York, New York, 10032, United States|Site US10007, New York, New York, 10065, United States|Site US10001, Cleveland, Ohio, 44195, United States|Site US10004, Hershey, Pennsylvania, 17033, United States|Site US10008, Philadelphia, Pennsylvania, 19104, United States Less <<
NCT04699877 Renal Impaired|Gilteritinib|No... More >>rmal Renal Function|Pharmacokinetics of ASP2215 Less << PHASE1 COMPLETED 2022-07-18 National Institute of Clinical... More >> Research, Garden Grove, California, 92844, United States|Orange County Research Institute, Tustin, California, 92780, United States|Orlando Clinical Research Center, Orlando, Florida, 32809, United States|Site BG35901, Sofia, 1000, Bulgaria Less <<
NCT02571816 Hepatic Impairment|Healthy PHASE1 COMPLETED 2016-03-05 Site US10001, Miami, Florida, ... More >>33014, United States Less <<
NCT02181660 Acute Myeloid Leukemia (AML) PHASE1 COMPLETED 2016-06-27 Site JP00002, Aichi, Japan|Sit... More >>e JP00003, Fukuoka, Japan|Site JP00001, Gunma, Japan|Site JP00004, Tokyo, Japan|Site JP00005, Tokyo, Japan Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.81mL

0.36mL

0.18mL

9.05mL

1.81mL

0.90mL

18.09mL

3.62mL

1.81mL

Dissolving Methods
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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