1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. JAK
    FLT3
  3. JAK2-IN-7

JAK2-IN-7 

Cat. No.: HY-131906 Purity: 99.42%
Handling Instructions

JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.

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

JAK2-IN-7 Chemical Structure

JAK2-IN-7 Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 455 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 800 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3800 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities[1].

IC50 & Target[1]

JAK1

42 nM (IC50)

JAK2

3 nM (IC50)

JAK3

94 nM (IC50)

Tyk2

75 nM (IC50)

FLT3

62 nM (IC50)

In Vitro

JAK2-IN-7 (compound 13ac) (0-1000 nM; 2 hours) inhibits JAK2 and STAT5 phosphorylation in a dose-dependent manner in SET-2 and Ba/F3-JAK2V617F cells[1].
JAK2-IN-7 (10-160 nM; 24 hours) induces cell arrest in the G0/G1 phase[1].
JAK2-IN-7 (0.05-1.6 μM; 2 hours) induces apoptosis in SET-2 cells[1].

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

Cell Cycle Analysis[1]

Cell Line: SET-2 cells
Concentration: 10-160 nM
Incubation Time: 24 hours
Result: Induced cell arrest in the G0/G1 phase in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: SET-2 cells
Concentration: 0.05-1.6 μM
Incubation Time: 2 hours
Result: Induced apoptosis in SET-2 cells.
In Vivo

JAK2-IN-7 (15-60 mg/kg; p.o.; daily for 16 days) shows potent in vivo antitumor efficacy with 82.3% tumor growth inhibition in the SET-2 xenograft model[1].
JAK2-IN-7 (30-60 mg/kg; p.o.; q.d. for 16 day) significantly ameliorates the disease symptoms in a Ba/F3-JAK2V617F allograft model, with 77.1% normalization of spleen weight, which was more potent than Ruxolitinib[1].

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

Animal Model: SET-2 cell-inoculated xenograft NOD/SCID mouse model[1]
Dosage: 15, 30, and 60 mg/kg
Administration: Orally daily for 16 days
Result: Exhibited a significant tumor growth inhibition of 82.3% without obvious weight change.
Molecular Weight

459.59

Formula

C₂₆H₃₃N₇O

SMILES

CC1=C(N=C(N=C1)NC2=CC=C3CN(CCC3=C2)C(/C=C/CN(C)C)=O)C4=CN(N=C4)C(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (543.96 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1759 mL 10.8793 mL 21.7585 mL
5 mM 0.4352 mL 2.1759 mL 4.3517 mL
10 mM 0.2176 mL 1.0879 mL 2.1759 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

JAK2-IN-7JAKFLT3Janus kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3V617FmutationphosphorylationantitumorSET-2xenograftmodelInhibitorinhibitorinhibit

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Product Name:
JAK2-IN-7
Cat. No.:
HY-131906
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