WP1066

Item no.	S2796-10mM
Manufacturer	Selleckchem
CASRN	857064-38-1
Amount	10 mM/1 ml
Category	Oncology Neuroscience Neural Lineage Markers Neuroinflammation Neural Transcription Factors Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Bladder Cancer Heart & Blood Cancer
Type	Inhibitors
Specific against	other
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	857064-38-1'
Similar products	WP1066
Available
Administration	Orally administrated
Animal Models	Caki-1 xenograft mice
Cell lines	HEL cells carrying the JAK2 V617F mutant isoform, HL60, K562, Raji, PEER, CMK, TM and RHN cells
Chemical Name	(S, E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide
Concentrations	0 - 6 uM
Description	WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 uM and 2.43 uM in HEL cells .
Dosages	40 mg/kg
Features	Similar to its parent compound AG490, WP1066 inhibit the phosphorylation of JAK2, but unlike AG490, WP1066 also degraded JAK2 protein.
Formulation	DMSO:polyethylene glycol 300 (20:80)
IC50	2.3 uM [1], 2.3 uM [1], 2.3 uM [1], 2.3 uM [1], 2.3 uM [1], 2.3 uM [1]
In vitro	WP1066 markedly inhibits the growth of HEL cells carrying the JAK2 V617F mutant isoform in a dose-dependent manner with IC20, IC50 and IC80 of 0.8, 2.3 and 3.8 uM. WP1066 at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 uM inhibits the phosphorylation of JAK2, STAT3, STAT5, and ERK1/2 without affecting the phosphorylation of JAK1 and JAK3 in erythroid leukemia HEL cells that express the JAK2 V617F isoform. [1] WP1066 at concentrations ranging from 0.5 to 3.0 uM inhibits the proliferation of AML colony-forming cells obtained from patients and that of the AML cell lines OCIM2 and K562 in a dose-dependent manner. WP1066 at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 uM dose-dependently decreases JAK2 and pJAK2 protein levels as well as downstream phosphorylation levels of STAT3, STAT5, and AKT in OCIM2 and K562 cells. WP1066 at concentrations of 2 uM inhibits OCIM2 cell multiplication by inducing accumulation of cells at the G0-G1 phase of the cell cycle. WP1066 at concentrations of 1, 2, or 3 uM induces apoptosis in both OCIM2 and K562 cells in a dose-dependent fashion by activating procaspase-3 and cleaving PARP. [3] WP1066 at concentrations of 5 uM prevents the phosphorylation of STAT3, and at concentrations of 2.5uM WP1066 significantly inhibits cell survival and proliferation in Caki-1 and 786-O renal cancer cells. WP1066 at concentrations of 5 uM suppresses HIF1alpha and HIF2alpha expression and VEGF production in Caki-1 and 786-O renal cancer cells. [4]
In vivo	WP1066 orally administrated at dose of 40 mg/kg once daily for 19 days significantly inhibits the tumours growth in Caki-1 xenograft mice, with decreased immunostaining of phosphorylated STAT3 and reduced length of CD34-positive vessels. [4]
Incubation Time	72 hours
Method	The 3, [4, 5-dimethylthiazol-2-yl]-5-[3-carboxymethoxyphenyl]-2-[4-sulfophenyl]-2H-tetrazolium (MTT) assay is done using an MTT-based cell proliferation/cytotoxicity assay system. Briefly, fresh low-density peripheral blood cells and various cell lines at the logarithmic phase of their growth are washed twice in RPMI 1640 containing 10% FCS and counted in a hemocytometer. Cell viability is assessed by the trypan blue (0.1%) staining method. Equal numbers of viable cells (5 x 104 per well) are incubated in a total volume of 100 uL of RPMI 1640 supplemented with 10% FCS alone or with WP1066 at increasing concentrations, the incubations are continued for up to 72 h in 96-well flat-bottomed plates at 37 C in a humidified 5% CO2 atmosphere. Experiments for each condition are done in triplicate. After incubation, 20 uL of CellTiter96 One Solution Reagent are added to each well. The plates are then incubated for an additional 60 min at 37 C in a humidified 5% CO2 atmosphere. Immediately after incubation, absorbance is read using a 96-well plate reader at a wavelength of 490 nm.
Molecular Weight (MW)	356, 22
Picture ChemicalStructure Description	WP1066 Chemical Structure
Solubility (25C)	DMSO 72 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Storage	2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

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Amount: 10 mM/1 ml

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