JAK2-IN-7

SKU: orb1304023

Description

JAK2-IN-7 is a potent and selective JAK2 inhibitor with low nanomolar IC50 values against JAK2 and relevant cell lines. It demonstrates over 14-fold selectivity against related kinases and exhibits antitumor activity by inducing G0/G1 cell cycle arrest and apoptosis in vitro.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2593402-36-7
• MW: 459.59
• Purity: 99.54% (May vary between batches)
• Formula: C₂₆H₃₃N₇O
• SMILES: C(/C=C/CN(C)C)(=O)N1CC=2C(=CC(NC=3N=C(C(C)=CN3)C4=CN(C(C)C)N=C4)=CC2)CC1
• Target: JAK,FLT,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (10.88 mM);DMSO:250 mg/mL (543.96 mM)

Bioactivity

• Target IC50:
  Tyk2:75 nM|JAK2:3 nM|JAK1:42 nM|FLT3:62 nM|JAK3:94 nM
• In Vivo:
  JAK2-IN-7, administered orally at doses ranging from 15 to 60 mg/kg daily for 16 days, demonstrated strong antitumor activity, inhibiting tumor growth by 82.3% in the SET-2 xenograft model . At doses between 30 and 60 mg/kg, it significantly reduced disease symptoms in a Ba/F3-JAK2V617F allograft model by normalizing spleen weight by 77.1%, outperforming Ruxolitinib . These findings, derived from administering JAK2-IN-7 to a NOD/SCID mouse model inoculated with SET-2 cells, highlight its potential without noticeable weight changes in the animals.
• In Vitro:
  JAK2-IN-7 (compound 13ac), in concentrations ranging from 0-1000 nM for 2 hours, dose-dependently inhibits the phosphorylation of JAK2 and STAT5 in both SET-2 and Ba/F3-JAK2 V617F cells. Additionally, at 10-160 nM over 24 hours, it promotes cell cycle arrest at the G0/G1 phase, and at 0.05-1.6 μM for 2 hours, it induces apoptosis in SET-2 cells. Both the cell cycle arrest and apoptosis induction are concentration-dependent, confirming the compound's efficacy in modulating key cellular processes related to proliferation and survival.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

JAK2 IN 7, JAK2IN7, JAK-2-IN-7, JAK2-IN-7, JAK2

Compound Identifiers

PubChem CID

155925850