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Ruxolitinib (INCB018424) is a first-in-class, potent and selective JAK1/2 inhibitor with an IC50 of 3.3 nM/2.8 nM. It is 130-fold more potent and selective for JAK1 and JAK2 compared to JAK3. In Ba/F3 and HEL cells, INCB018424 potently and selectively inhibited JAK2V617F-mediated signaling and cell proliferation.INCB018424 significantly increased apoptosis in Ba/F3 cells in a dose-dependent manner. In Ba/F3 cells, INCB018424 (64 nM) caused a doubling of mitochondrial depolarized cells.
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Application | CFU assays |
| Results | Similar to the shRNA results, both inhibitors reduced the colony-forming ability of the transformed cells in a dose-dependent manner |
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Application | MTS assay |
| Results | INCB18424 showed a significantly better inhibitory effect than TG101209 at concentrations below 1 μM. Both inhibitors also promoted apoptosis (Figure 2b) and delayed cell cycle progression (Figure 2c) of the AEtr leukemia cell line. |
| Cell Experiment | |
|---|---|
| Cell lines | Ba/F3-EpoR-JAK2V617F and HEL cell lines |
| Preparation method | Cell proliferation assay. Cells were seeded at 2000/well of white bottom 96-well plates, treated with compounds from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37°C with 5% CO2. Viability was measured by cellular ATP determination using the Cell-Titer Glo (Promega) luciferase reagent or viable cell counting. Values were transformed to percent inhibition relative to vehicle control, and IC50 curves were fitted according to nonlinear regression analysis of the data using PRISM GraphPad. |
| Concentrations | 0~10 µ M |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | myeloproliferative neoplasm mouse model |
| Formulation | 5% dimethyl acetamide, 0.5% methyl cellulose |
| Dosages | 180mg/kg began within 24 hours of cell inoculation, twice daily |
| Administration | oral gavage |
| Molecular Weight | 306.37 |
| Formula | C17H18N6 |
| CAS Number | 941678-49-5 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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