2. Protein Tyrosine Kinase/RTK Epigenetics Cell Cycle/DNA Damage Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. FLT3 HDAC Apoptosis Reactive Oxygen Species (ROS)
  4. FLT3/HDAC-IN-3

FLT3/HDAC-IN-3 is a dual inhibitor of FLT3 and HDAC. FLT3/HDAC-IN-3 potently inhibits FLT3 (IC50 = 14 nM), HDAC1 (IC50 = 27 nM), HDAC6 (IC50 = 20 nM), and FLT3D853Y (IC50 = 55 nM), exhibits weak activity against HDAC8, and shows no activity against HDAC4. FLT3/HDAC-IN-3 possesses kinase selectivity, plasma stability, and stability in human liver microsomes. FLT3/HDAC-IN-3 demonstrates anti-proliferative effects in a variety of hematological malignancy cell lines. FLT3/HDAC-IN-3 shows efficacy in the Jeko-1 xenograft model without observed significant toxicity. FLT3/HDAC-IN-3 can be used in the study of hematological malignancies.

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FLT3/HDAC-IN-3

FLT3/HDAC-IN-3 Chemical Structure

CAS No. : 2864394-30-7

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FLT3/HDAC-IN-3 Related Antibodies

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Description

FLT3/HDAC-IN-3 is a dual inhibitor of FLT3 and HDAC. FLT3/HDAC-IN-3 potently inhibits FLT3 (IC50 = 14 nM), HDAC1 (IC50 = 27 nM), HDAC6 (IC50 = 20 nM), and FLT3D853Y (IC50 = 55 nM), exhibits weak activity against HDAC8, and shows no activity against HDAC4. FLT3/HDAC-IN-3 possesses kinase selectivity, plasma stability, and stability in human liver microsomes. FLT3/HDAC-IN-3 demonstrates anti-proliferative effects in a variety of hematological malignancy cell lines. FLT3/HDAC-IN-3 shows efficacy in the Jeko-1 xenograft model without observed significant toxicity. FLT3/HDAC-IN-3 can be used in the study of hematological malignancies[1].

IC50 & Target

FLT3

14 nM (IC50)

HDAC6

20 nM (IC50)

HDAC1

27 nM (IC50)

FLT3D835Y

55 nM (IC50)

HDAC8

2800 nM (IC50)

HDAC4

>10000 nM (IC50)

In Vitro

FLT3/HDAC-IN-3 (compound 6s) (72 h) potently inhibits the proliferation of MV-4-11 cells (IC50 = 29 nM) and Jeko-1 cells (IC50 = 99 nM) with favorable tumor-cell selectivity (IC50 = 80 μM in HaCaT cells)[1].
FLT3/HDAC-IN-3 (0-1000 nM; 72 h) dose-dependently inhibits FLT3 and STAT5 phosphorylation, increases H3Ac levels, and upregulates Bax in MV-4-11 cells[1].
FLT3/HDAC-IN-3 (0-1000 nM; 72 h) induces dose-dependent cell death in MV-4-11 and Jeko-1 cells, and dose-dependently induces ROS accumulation, decreases mitochondrial membrane potential [1].
FLT3/HDAC-IN-3 (0-1000 nM; 48 h or 72 h) induces time- and dose-dependent apoptosis in MV-4-11 and Jeko-1 cells[1].
FLT3/HDAC-IN-3 (0-1000 nM; 72 h) dose-dependently arrests the cell cycle in the G2 phase in MV-4-11 cells[1].
FLT3/HDAC-IN-3 (200 μM; 0–72 h) exhibits good plasma stability in rat plasma, with 67.8% retention after 72 h[1].
FLT3/HDAC-IN-3 shows favorable metabolic stability in human liver microsomes with a half-life of 165 min and intrinsic clearance of 7.56 mL/min/kg[1].

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

FLT3/HDAC-IN-3 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0 nM, 50 nM, 250 nM, 1000 nM
Incubation Time: 72 h
Result: Dose-dependently inhibited phosphorylated FLT3 and p-STAT5; increased acetylated histone H3 (H3Ac) levels in a concentration-dependent manner, with higher H3Ac accumulation at 250 nM compared to SAHA at the same concentration; upregulated pro-apoptotic protein Bax in a dose-dependent manner.

Cell Cytotoxicity Assay[1]

Cell Line: MV-4-11, Jeko-1 cells
Concentration: 0 nM, 50 nM, 250 nM, 1000 nM
Incubation Time: 72 h
Result: Induced a dose-dependent increase in red fluorescence (dead cells) and decrease in green fluorescence (live cells) in both MV-4-11 and Jeko-1 cells.

Apoptosis Analysis[1]

Cell Line: MV-4-11, Jeko-1 cells
Concentration: 0 nM, 50 nM, 250 nM, 1000 nM
Incubation Time: 48 h or 72 h
Result: Induced apoptosis in a time- and dose-dependent manner; at 72 h, induced 47.7% apoptosis at 250 nM and up to 75% apoptosis at 1000 nM in MV-4-11 cells, with effects comparable to SAHA + Tandutinib combination treatment; also induced dose-dependent apoptosis in Jeko-1 cells.

Cell Cycle Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0 nM, 50 nM, 250 nM, 1000 nM
Incubation Time: 72 h
Result: Effectively arrested the cell cycle in the G2 phase in a dose-dependent manner
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ MRT0-t MRT0-∞ F
Rat[1] 5 mg/kg i.v. 0.54 h 0.083 h 86.00 ng/mL 48.70 ng·h/mL 52.20 ng·h/mL 0.48 h 0.63 h /
Rat[1] 30 mg/kg p.o. 2.21 h 0.50 h 17.80 ng/mL 33.90 ng·h/mL 60.90 ng·h/mL 1.68 h 4.49 h 19.50 %
Rat[1] 30 mg/kg i.p. 1.14 h 0.33 h 137 ng/mL 148 ng·h/mL 153 ng·h/mL 0.96 h 1.09 h 49.00 %
In Vivo

FLT3/HDAC-IN-3 (compound 6s) (15-30 mg/kg; i.p.; daily; 15 days) dose-dependently inhibits mantle cell lymphoma growth in Jeko-1 xenograft mice, achieving 53.34% tumor growth inhibition (TGI) at 30 mg/kg with no observable toxicity[1].

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

Animal Model: NOD/SCID mice injected with Jeko-1 cells[1]
Dosage: 15 mg/kg; 30 mg/kg
Administration: i.p.; daily; 15 days
Result: Achieved 37.14% TGI and 0.47 g average tumor weight at 15 mg/kg; achieved 53.34% TGI and 0.39 g average tumor weight at 30 mg/kg.
Induced more severe tumor cell necrosis than control or SAHA groups at 30 mg/kg.
Caused no significant weight loss or abnormalities in drinking, diet, or activity at 30 mg/kg.
Molecular Weight

445.53

Formula

C22H32FN7O2
CAS No.
SMILES

FC(C=N1)=C(NCCCCCCC(NO)=O)N=C1NC(C=C2)=CC=C2N3CCN(C)CC3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FLT3/HDAC-IN-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FLT3/HDAC-IN-32864394-30-7FLT3HDACApoptosisReactive Oxygen Species (ROS)Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Histone deacetylasesHDAC4xenograft modelJeko-1 cellsHDAC6FLT3D835YMV-4-11 cellshematologic malignanciesHDAC1HDAC8Inhibitorinhibitorinhibit

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