CHZ868 is a type II JAK2 inhibitor (IC50: 0.17 μM in EPOR JAK2 WT Ba/F3 cell).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | 2-3 weeks | $ 142 | |
10 mg | 2-3 weeks | $ 255 | |
20 mg | 2-3 weeks | $ 430 | |
50 mg | 2-3 weeks | $ 725 | |
100 mg | 2-3 weeks | $ 1087 |
Description | CHZ868 is a type II JAK2 inhibitor (IC50: 0.17 μM in EPOR JAK2 WT Ba/F3 cell). |
Targets&IC50 | JAK2: 110 nM |
In vitro | CHZ868 is dissolved in DMSO to make 10 mM stock solution and diluted in culture media. Cells are treated with CHZ868 (0, 0.05, 0.1, 0.2 μM) or vehicle (DMSO). After 48 hr (Ba/F3 cells) or 72 hr (MHH-CALL4 and PDX cells), CellTiter-Glo Luminescent Cell Viability Assay is added (10 μL undiluted or 25 μL of a 1:2 dilution in each well) and plates are read. |
In vivo | CHZ868 is reconstituted in 0.5% methylcellulose / 0.5% Tween-80 and administered at doses of 10 or 30 mg/kg/day by oral gavage. Pharmacokinetic/pharmacodynamic and efficacy studies in the mouse model of rhEpo-induced polycythemia are carried out essentially. Detection of STAT5 phosphorylation in spleen lysates by Meso Scale Discovery is performed. |
CAS No. | 1895895-38-1 |
Chemical Formula | C22H19F2N5O2 |
Molecular Weight | 423.424 |
Solubility | DMSO: 145 mg/mL (342.45 mM) |
Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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