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WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation.
| Cell Experiment | |
|---|---|
| Cell lines | U87, U737 |
| Preparation method | Seeding the cells into a 96-well plate at a density of 2.5×104 cells/well and incubating for 36 h at 37 ℃ before drug exposure. On the day of treatment, culture medium is carefully aspirated from the wells and replaced with fresh medium which contains the quinazoline compounds WHI-P154 at concentrations ranging from 0.1 μM to 250 μM. Using triplicate wells for each treatment. Incubating the cells with the compound for 24 hours to 36 hours at 37 ℃ in a humidified 5% CO2 atmosphere.10 μL of MTT (final concentration for each well, 0.5 mg/mL) is added, and the plate are incubated at 37 ℃ for 4 h. Than solubilized overnight at 37 ℃ in a solution containing 10% SDS in 0.01 M HCL. Mearsuring the absorbance of each well in a microplate reader at 570 nm. |
| Concentrations | 0.1-250 μM |
| Incubation time | 24-36 h |
| Animal Experiment | |
|---|---|
| Animal models | SCID Xenograft Model of Human Glioblastoma (U737) |
| Formulation | Dissolved in PBS |
| Dosages | 0.5 mg/kg or 1 mg/kg for 10 days |
| Administration | i.p. |
| Molecular Weight | 376.2 |
| Formula | C16H14BrN3O3 |
| CAS Number | 211555-04-3 |
| 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 |
| Related JAK Products |
|---|
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| AZ 960
AZ 960 is a novel and specific inhibitor of the JAK2 kinase with a Ki of 0.45nM in vitro. |
| Momelotinib (CYT387)
Momelotinib (CYT387) is a small-molecule, ATP-competitive JAK1/JAK2 inhibitor with IC50 of 11 and 18 nM respectively. |
| TG101348
TG101348 is a selective small-molecule Janus kinase 2 (JAK2) inhibitor with IC50 of 3 nM. |
| WP1130
Degrasyn (WP1130) is a small molecular deubiquitinase (DUB) inhibitor and suppresses JAK-Stat signaling pathway. |
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