1. Protein Tyrosine Kinase/RTK
  2. FLT3
  3. FLT3-IN-40

FLT3-IN-40 (compound 1) is a type I ATP-competitive FLT3 inhibitor with an IC50 of 16.26 nM. FLT3-IN-40 reduces the autophosphorylation level of FLT3 and the phosphorylation level of downstream ERK. FLT3-IN-40 exhibits antiproliferative, cell cycle regulatory and apoptosis-inducing activities. FLT3-IN-40 can be used in research related to acute myeloid leukemia.

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

FLT3-IN-40

FLT3-IN-40 Chemical Structure

CAS No. : 3075541-07-7

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Description

FLT3-IN-40 (compound 1) is a type I ATP-competitive FLT3 inhibitor with an IC50 of 16.26 nM. FLT3-IN-40 reduces the autophosphorylation level of FLT3 and the phosphorylation level of downstream ERK. FLT3-IN-40 exhibits antiproliferative, cell cycle regulatory and apoptosis-inducing activities. FLT3-IN-40 can be used in research related to acute myeloid leukemia[1].

In Vitro

FLT3-IN-40 (compound 1) (0.00001-100 nM; sufficient to measure antiproliferative effects) potently inhibits MV4-11 cell proliferation with an IC50 of 0.002 nM, exhibiting a gradual, biphasic dose-response profile[1].
FLT3-IN-40 (0.001-10 nM) is an ATP-competitive type-I FLT3 inhibitor, inhibiting purified FLT3 kinase with an IC50 of 16.26 nM and MV4-11 cellular FLT3 pathway signaling with an IC50 of 0.80 nM for p-ERK inhibition[1].
FLT3-IN-40 (sufficient to measure antiproliferative effects) inhibits Molm14 cell proliferation with an IC50 of 1.42 nM, and has much weaker antiproliferative activity against K562 (IC50 1583 nM) and Ba/F3 (IC50 8467 nM) cells lacking FLT3 activating mutations[1].
FLT3-IN-40 (1 pM-10 nM; 72 h) induces minimal apoptosis in MV4-11 cells at picomolar concentrations, but triggers significant early (17.3%) and late (10.3%) apoptosis at 10 nM following 72 h of treatment[1].
FLT3-IN-40 (1 pM-10 nM; 72 h) induces a moderate G1 phase stabilization in MV4-11 cells at picomolar concentrations, and a strong G1 phase cell cycle arrest at 10 nM following 72 h of treatment[1].
FLT3-IN-40 (1 nM; 10 nM) exhibits high kinase selectivity, with strong binding only to FLT3 among the 96 kinases tested at 1 nM and 10 nM concentrations[1].

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

Cell Proliferation Assay[1]

Cell Line: MV4-11 (FLT3-ITD positive acute myeloid leukemia) cells
Concentration: 0.00001-100 nM
Incubation Time: sufficient to measure antiproliferative effects
Result: Inhibited MV4-11 cell proliferation with an IC50 of 0.0021 nM (or 2.13 pM).
Achieved ~50% inhibition at 2 pM and >90% inhibition at 20 nM, with a gradual, biphasic dose-response curve.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 1 pM-10 nM
Incubation Time: 72 h
Result: Induced early apoptotic cell percentages of 2.1%, 2.3%, 3.4%, and 4.8% at 1 pM, 10 pM, 100 pM, and 1 nM respectively, with minimal late apoptosis.
Triggered early apoptotic cell percentage of 17.3% and late apoptotic cell percentage of 10.3% at 10 nM, showing a marked increase in apoptosis at nanomolar concentrations.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 1 pM-10 nM
Incubation Time: 72 h
Result: Increased G1 phase cell percentages to 52.4%, 53.5%, and 54.5% at 1 pM, 10 pM, and 100 pM respectively (compared to 47.2% for DMSO control).
Increased G1 phase percentage to 58.1% at 1 nM, and to 68.7% at 10 nM with a corresponding decrease in G2 phase from 8.93% at 1 nM to 3.01% at 10 nM.
Molecular Weight

426.47

Formula

C24H22N6O2

CAS No.
SMILES

COC1=CC(OC)=C(C=C1)NC2=CC=CC(C3=CN=C4C=C(C=CN34)C5=CN(N=C5)C)=N2

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Purity & Documentation
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FLT3-IN-40
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HY-182004
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