1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. JAK
    FLT3
  3. JAK2/FLT3-IN-1

JAK2/FLT3-IN-1 

Cat. No.: HY-130247
Handling Instructions

JAK2/FLT3-IN-1 is a potent and orally effective dual JAK2/FLT3 (Janus kinase 2/ FMS-like tyrosine kinase 3) inhibitors with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity.

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

JAK2/FLT3-IN-1 Chemical Structure

JAK2/FLT3-IN-1 Chemical Structure

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Description

JAK2/FLT3-IN-1 is a potent and orally effective dual JAK2/FLT3 (Janus kinase 2/ FMS-like tyrosine kinase 3) inhibitors with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity[1].

IC50 & Target

JAK2

0.7 nM (IC50)

FLT3

4 nM (IC50)

JAK1

26 nM (IC50)

JAK3

39 nM (IC50)

In Vitro

JAK2/FLT3-IN-1 (0.005-0.1 μM; for 2 hours) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cell[1].
JAK2/FLT3-IN-1 (0.005-0.1 μM; for 2 hours) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells[1].
JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) down-regulates p-FLT3 in a dose-dependent manner from 0.008 to 1 μM[1].

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.005, 0.01, 0.05, 0.1 μM
Incubation Time: For 2 hours
Result: Induced cell cycle arrest with a G1/G0 percentage of 85% at 100 nM.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.005, 0.01, 0.05, 0.1 μM
Incubation Time: For 2 hours
Result: Had a dose-dependent effect on the induction of apoptosis in the MV4-11 cells.

Western Blot Analysis[1]

Cell Line: MV4-11 and SET-2 cells
Concentration: 0.008, 0.04, 0.2, 1 μM
Incubation Time: For 2 hours
Result: Down-regulate p-FLT3 in a dose-dependent manner from 0.008 to 1 μM.
In Vivo

JAK2/FLT3-IN-1 (oral administration; 30 and 60 mg/kg/day; for 14 days) exhibits significant antitumor effects and the tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model[1].

Animal Model: NOD/SCID mouse models[1]
Dosage: 30 and 60 mg/kg
Administration: Oral administration; daily; for 14 days
Result: Exhibited significant antitumor effects and the tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model.
Molecular Weight

467.58

Formula

C₂₅H₃₄FN₇O

SMILES

OCCN(C1CCN(C2=CC=C(NC3=NC=C(C)C(C4=CN(C(C)C)N=C4)=N3)C=C2F)CC1)C

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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JAK2/FLT3-IN-1
Cat. No.:
HY-130247
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