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WP1066

Cat. No. M2125
WP1066 Structure
Size Price Availability Quantity
10mg USD 80 In stock
50mg USD 260 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 356.22
Formula C17H14BrN3O
CAS Number 857064-38-1
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
References

The tumor microenvironment expression of p-STAT3 influences the efficacy of cyclophosphamide with WP1066 in murine melanoma models.
Hatiboglu MA, et al. Int J Cancer. 2012 Jul 1;131(1):8-17. PMID: 21792892.

STAT3 inhibitor WP1066 as a novel therapeutic agent for renal cell carcinoma.
Horiguchi A, et al. Br J Cancer. 2010 May 25;102(11):1592-9. PMID: 20461084.

WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation.
Verstovsek S, et al. Clin Cancer Res. 2008 Feb 1;14(3):788-96. PMID: 18245540.

WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells.
Ferrajoli A, et al. Cancer Res. 2007 Dec 1;67(23):11291-9. PMID: 18056455.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: WP1066 supplier, JAK, inhibitors

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