| Name | JAK2-IN-7 |
| Description | JAK2-IN-7, a selective inhibitor targeting Janus Kinase 2 (JAK2), exhibits inhibitory concentrations (IC50) of 3 nM for JAK2, 11.7 nM for SET-2 cells, and 41 nM for Ba/F3 V617F cells, indicative of its potency and selectivity. This compound demonstrates more than 14-fold selectivity against JAK1, JAK3, and FLT3, underlining its specificity. JAK2-IN-7 effectively induces cell cycle arrest at the G0/G1 phase and promotes apoptosis in tumor cells, manifesting significant antitumor activities [1]. |
| 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. |
| 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 [1]. 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 [1]. 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (10.88 mM), Sonication is recommended.
DMSO : 250 mg/mL (543.96 mM), Sonication is recommended.
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| Keywords | JAK-2-IN-7 | JAK2IN7 | JAK2 IN 7 | JAK2 |
| Inhibitors Related | Stavudine | Cysteamine hydrochloride | Sodium 4-phenylbutyrate | Metronidazole | Citric Acid Triammonium | Tributyrin | L-Methionine | Sodium citrate | Cystamine dihydrochloride | L-Ascorbic acid sodium salt | Alginic acid | Dextran sulfate sodium salt (MW 5000) |
| Related Compound Libraries | Apoptosis Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Cancer Active Compound Library |
United States
