1. Protein Tyrosine Kinase/RTK
    Neuronal Signaling
    Apoptosis
  2. FLT3
    Trk Receptor
    Apoptosis
  3. FLT3/TrKA-IN-1

FLT3/TrKA-IN-1 

Cat. No.: HY-146749
Handling Instructions

FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML).

For research use only. We do not sell to patients.

FLT3/TrKA-IN-1 Chemical Structure

FLT3/TrKA-IN-1 Chemical Structure

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Description

FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML)[1].

IC50 & Target[1]

TrkA

23.6 nM (IC50)

FLT3

43.8 nM (IC50)

FLT3-ITD

97.2 nM (IC50)

FLT3-TKD

92.5 nM (IC50)

In Vitro

FLT3/TrKA-IN-1 (compound 4ACP) (1000, 2000, 3000, 4000, 5000 nM; 24, 48, 72 h) shows antiproliferative activity in a concentration and time-dependent pattera with IC50s of 38.8 nM, 54.9 nM for MOLM-13 and MV4-11 cells, respectively[1].
FLT3/TrKA-IN-1 (500, 1000, 1500, 2000, 2500 nM) dose not elicit cytotoxic activity against GDM-1 and THP-1 AML cell lines which do not carry FLT3-ITD mutation[1].
FLT3/TrKA-IN-1 shows potent activity against colon cancer KM12 cell line with an GI50 value of 358 nM[1].
FLT3/TrKA-IN-1 (0, 10, 50, 100 nM; 24 h, 48 h) inhibits ERK1/2 (extracellular regulated kinases 1/2) and mTOR (mammalian target of rapamycin) in FLT3-ITD positive AML (acute myeloid leukemia) cell lines in a dose-dependent manner[1].
FLT3/TrKA-IN-1 (0, 10, 50, 100 nM; 72 h) induces cell cycle arrest at the G0/G1 phase as well as apoptosis and necrotic cell death of FLT3-ITD harboring AML cells[1].
FLT3/TrKA-IN-1 ( 0, 1, 10, 100, 1000 nM; 72 h) dose not elicit drastic cytotoxic effects on BNL and H9c2 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MV4-11, MOLM-13 cells
Concentration: 1000, 2000, 3000, 4000, 5000 nM
Incubation Time: 24, 48, 72 h
Result: Showed antiproliferative activity in a concentration and time-dependent pattera with IC50s of 38.8 nM, 54.9 nM for MOLM-13 and MV4-11 cells, respectively.

Western Blot Analysis[1]

Cell Line: MV4-11, MOLM-13 cells
Concentration: 0, 10, 50, 100 nM
Incubation Time: 72 h
Result: Induced cell cycle arrest at the G0/G1 phase.

Apoptosis Analysis[1]

Cell Line: MV4-11, MOLM-13 cells
Concentration: 0, 10, 50, 100 nM
Incubation Time: 72 h
Result: Induced apoptosis and necrotic cell death of FLT3-ITD harboring AML cells.

Cell Cytotoxicity Assay[1]

Cell Line: BNL, H9c2 cells
Concentration: 0, 1, 10, 100, 1000 nM
Incubation Time: 72 h
Result: Did not elicit drastic cytotoxic effects on BNL and H9c2 cells.
Molecular Weight

454.56

Formula

C28H30N4O2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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FLT3/TrKA-IN-1
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