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

JAK2/FLT3-IN-1 TFA 

Cat. No.: HY-130247A
Handling Instructions

JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor 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 (TFA) has anti-cancer activity.

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

JAK2/FLT3-IN-1 TFA Chemical Structure

JAK2/FLT3-IN-1 TFA Chemical Structure

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5 mg USD 750 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor 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 (TFA) has anti-cancer activity[1].

IC50 & Target

JAK1

26 nM (IC50)

JAK2

0.7 nM (IC50)

JAK3

39 nM (IC50)

FLT3

4 nM (IC50)

In Vitro

JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) (TFA) down-regulates p-FLT3 in a dose-dependent manner[1].
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells[1].
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells[1].

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

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-regulated p-FLT3 in a dose-dependent manner from 0.008 to 1 μM.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5, 10, 50, 100 nM
Incubation Time: For 2 hours
Result: Had a dose-dependent effect on the induction of apoptosis in the MV4-11 cells.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5, 10, 50, 100 nM
Incubation Time: For 2 hours
Result: Induced cell cycle arrest with a G1/G0 percentage of 85% at 100 nM.
In Vivo

JAK2/FLT3-IN-1 (30 and 60 mg/kg/day; p.o.; for 14 days) (TFA) exhibits significant antitumor effects[1].

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

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.
The tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model.
Molecular Weight

581.61

Formula

C₂₇H₃₅F₄N₇O₃

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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Product Name:
JAK2/FLT3-IN-1 TFA
Cat. No.:
HY-130247A
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