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WP1066 JAK inhibitor

Name: WP1066
Brand: Selleck Chemicals
SKU: S2796
Availability: InStock
Rating: 5 (75 reviews)

Cat.No.S2796

WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. This compound induces apoptosis. Phase 1.

Chemical Structure

Molecular Weight: 356.22

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.97%

99.97

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
human MM1 cells	Function assay	24-72 h	Antitumor activity against human MM1 cells after 24 to 72 hrs by MTT assay, ic50=1.2 μM
human U266 cells	Function assay	24-72 h	Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay, IC50=1.5 μM
human OCI-My4 cells	Function assay	24-72 h	Antitumor activity against human OCI-My4 cells after 24 to 72 hrs by MTT assay, IC50=1.8 μM
human 30M cells	Cytotoxic assay	8 days	Cytotoxicity against human 30M cells assessed as cell viability after 8 days by Alamar Blue assay, IC50=1.8 μM
human 73M cells	Cytotoxic assay	8 days	Cytotoxicity against human 73M cells assessed as cell viability after 8 days by Alamar Blue assay, IC50=2.1 μM
human U373MG cells	Function assay	24-72 h	Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay, IC50=3.7 μM
human U87MG cells	Function assay	24-72 h	Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay, IC50=5.6 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	356.22	Formula	C₁₇H₁₄BrN₃O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	857064-38-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C1=CC=CC=C1)NC(=O)C(=CC2=NC(=CC=C2)Br)C#N

Solubility

In vitro
Batch:

DMSO : 71 mg/mL ( (199.31 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (11.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.590mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 11.8 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.590mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 11.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	Similar to its parent compound AG490, WP1066 inhibits the phosphorylation of JAK2, but unlike AG490, WP1066 also degraded JAK2 protein.
Targets/IC₅₀/Ki	JAK2 ^[1] (HEL cells) 2.3 μM STAT3 ^[2] (HEL cells) 2.43 μM
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 μM. This compound at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 μM 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] It at concentrations ranging from 0.5 to 3.0 μM 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. This chemical at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 μM dose-dependently decreases JAK2 and pJAK2 protein levels as well as downstream phosphorylation levels of STAT3, STAT5, and AKT in OCIM2 and K562 cells. It at concentrations of 2 μM inhibits OCIM2 cell multiplication by inducing accumulation of cells at the G0-G1 phase of the cell cycle. This compound at concentrations of 1, 2, or 3 μM induces apoptosis in both OCIM2 and K562 cells in a dose-dependent fashion by activating procaspase-3 and cleaving PARP. ^[3] It at concentrations of 5 μM prevents the phosphorylation of STAT3, and at concentrations of 2.5μM it significantly inhibits cell survival and proliferation in Caki-1 and 786-O renal cancer cells. This chemical at concentrations of 5 μM suppresses HIF1α and HIF2α 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]
References	https://pubmed.ncbi.nlm.nih.gov/18245540/ https://pubmed.ncbi.nlm.nih.gov/21792892/ https://pubmed.ncbi.nlm.nih.gov/18056455/ https://pubmed.ncbi.nlm.nih.gov/20461084/

Applications

Methods	Biomarkers	PMID
Western blot	p-STAT3 / STAT3 / p-ERK / ERK	20461084
Cell viability	Cell viability	28496056
Immunofluorescence	N-cadherin / E-cadherin / Vimentin / β-catenin	26690371