1. Protein Tyrosine Kinase/RTK Stem Cell/Wnt MAPK/ERK Pathway PI3K/Akt/mTOR Apoptosis
  2. FLT3 ERK Akt Apoptosis
  3. FLT3-IN-34

FLT3-IN-34 is a FLT3 inhibitor, with an IC50 value of 1.4 nM. FLT3-IN-34 blocks the phosphorylation of FLT3 and its downstream signaling molecules AKT and ERK1/2. FLT3-IN-34 induces concentration-dependent G0/G1 phase arrest and mild apoptosis in FLT3-ITD-positive MV4-11 cells. FLT3-IN-34 shows potent anti-proliferative activity against FLT3-ITD-positive MV4-11 cells (IC50 = 14.95 nM) and MOLM-13 (IC50 = 18.5 nM). FLT3-IN-34 can be used for the study of FLT3-positive acute myeloid leukemia (AML).

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FLT3-IN-34

FLT3-IN-34 Chemical Structure

CAS No. : 3020729-11-4

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Description

FLT3-IN-34 is a FLT3 inhibitor, with an IC50 value of 1.4 nM. FLT3-IN-34 blocks the phosphorylation of FLT3 and its downstream signaling molecules AKT and ERK1/2. FLT3-IN-34 induces concentration-dependent G0/G1 phase arrest and mild apoptosis in FLT3-ITD-positive MV4-11 cells. FLT3-IN-34 shows potent anti-proliferative activity against FLT3-ITD-positive MV4-11 cells (IC50 = 14.95 nM) and MOLM-13 (IC50 = 18.5 nM). FLT3-IN-34 can be used for the study of FLT3-positive acute myeloid leukemia (AML)[1].

In Vitro

FLT3-IN-34 (Compound ZY12) exhibits excellent inhibitory potency against FLT3-ITD kinase, with an IC50 value of 1.4 nM[1].
FLT3-IN-34 shows potent antiproliferative activity against FLT3-ITD-positive MV4-11 cells (IC50 = 14.95 nM) and MOLM-13 (IC50 = 18.5 nM)[1].
FLT3-IN-34 (5-20 nM, 24 h) concentration-dependently induces G0/G1 phase arrest of MV4-11 cells and induces MV4-11 cell apoptosis[1].
FLT3-IN-34 (5-20 nM) significantly blocks the phosphorylation of FLT3, AKT, and ERK1/2 in MV4-11 and MOLM-13 cells, inhibiting the FLT3 signaling pathway[1].

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

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5, 10, 20 nM
Incubation Time: 24 h
Result: Induced G0/G1 phase arrest of MV4–11 cells and decreases the percentage of cells in S and G2/M phases.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5, 10, 20 nM
Incubation Time: 24 h
Result: Induced MV4–11 cell apoptosis.
In Vivo

FLT3-IN-34 (Compound ZY12) (30 mg/kg, p.o., once daily, 10 days) fails to obviously inhibit tumor growth in 4-6 weeks old BALB/c-nu mice bearing MV4-11 subcutaneous xenografts[1].

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

Animal Model: MV4-11 cells was subcutaneously implanted into the mid-lateral axilla of 4-6 weeks old BALB/c-nu mice[1]
Dosage: 30 mg/kg
Administration: p.o., once daily, 10 days
Result: Failed to obviously inhibit tumor growth (TGI=8.55%) in mice bearing MV4-11 subcutaneous xenografts.
Molecular Weight

417.46

Formula

C23H23N5O3

CAS No.
SMILES

O=C(NC1=CC=C(C(C2=CN=C3C=C(C)C=CN32)=O)C=C1)NC4=NOC(C(C)(C)C)=C4

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FLT3-IN-34
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HY-178020
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