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

JAK2/FLT3-IN-1 TFA 

Cat. No.: HY-130247A
COA 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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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

Appearance

Solid

Formula

C27H35F4N7O3
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro: 

H2O : 33.33 mg/mL (57.31 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7194 mL 8.5968 mL 17.1937 mL
5 mM 0.3439 mL 1.7194 mL 3.4387 mL
10 mM 0.1719 mL 0.8597 mL 1.7194 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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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.

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Keywords:

JAK2/FLT3-IN-1JAKFLT3ApoptosisJanus kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3orallyanti-cancercyclearrestG1/G0MV4-11Inhibitorinhibitorinhibit

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