WP1066 is a novel analogue of the JAK2 inhibitor AG490. WP1066 inhibited OCIM2 cell multiplication by inducing accumulation of cells at the G(0)-G(1) phase of the cell cycle. WP1066 concentrations in the low micromolar range induced time- and dose-dependent antiproliferative and proapoptotic effects in HEL cells. In Caki-1 and 786-O renal cancer cells, 5 muM WP1066 prevented the phosphorylation of STAT3, and 2.5 muM WP1066 significantly (P<0.01) inhibited cell survival and proliferation. WP1066 suppressed the expression of Bcl-2, induced apoptosis, and inhibited the basal and hypoxia-induced expression of HIF1alpha and HIF2alpha, as well as vascular endothelial growth factor secretion into cell culture medium. Inhibition of p-STAT3 by WP1066 was enhanced with CTX in a dose-dependent manner. WP1066 is active both in vitro and ex vivo.
J Sci Food Agric. 2023 May 1.
Oxymatrine ameliorates rheumatoid arthritis by regulation of Tfr/Tfh cells balance via TLR9-MyD88-STAT3 signaling pathway
WP1066 purchased from AbMole
Graefes Arch Clin Exp Ophthalmol. 2022 May 23.
Role of the JAK/STAT pathway in a streptozotocin-induced diabetic retinopathy mouse model
WP1066 purchased from AbMole
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Source | Oncology Reports (2018). Figure 5. WP1066 |
| Method | qPCR analysis | |
| Cell Lines | U2OS and MG-63 osteosarcoma cells | |
| Concentrations | 10 μM | |
| Incubation Time | 24 h | |
| Results | Inhibition of STAT3 phosphorylation with WP1066 further suppressed the mRNA and protein expression of Snail which was induced by irisin. |
| Cell Experiment | |
|---|---|
| Cell lines | Caki-1 and 786-O cells line |
| Preparation method | Cell viability was assessed by the MTS assay using the Cell Titer96 AQueous Non-Radioactive Cell Proliferation Assay (Promega, Madison, WI, USA) according to the manufacturer's instructions. Briefly, cells were incubated overnight in 96-well plates (3 × 103 cells/well) and then treated for 48 h with the indicated concentration of WP1066 (in DMSO) or with the corresponding amount of DMSO. Two hours after adding MTS, plates were read in a microplate autoreader at a wavelength of 490 nm. The results were expressed as the mean optical density of the six-well set for each group, and the plates were measured twice with similar results. For cell counts, after being incubated overnight in six-well plates (2 × 104 cells/well in triplicate), cells were treated with 2.5 or 5 μm WP1066 or with the corresponding amount of DMSO. Total cell numbers in three independent wells in each group were counted at the indicated time by using a hemocytometer, and the mean value of four fields was recorded. |
| Concentrations | 0, 2.5 and 5 μM |
| Incubation time | 24 and 48 h |
| Animal Experiment | |
|---|---|
| Animal models | nude mice bearing Caki-1 cells xenograft model |
| Formulation | mixture of 20 parts DMSO to 80 parts polyethylene glycol 300 |
| Dosages | 40mg/kg once per day (5 days on and 2 days off) for 18 days |
| Administration | oral gavage |
| Molecular Weight | 356.22 |
| Formula | C17H14BrN3O |
| CAS Number | 857064-38-1 |
| Solubility (25°C) | DMSO 46 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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