WP1066

Name: WP1066
Brand: MedChemExpress
SKU: HY-15312
Rating: 5.0 (38 reviews)

Cat. No.: HY-15312 Purity: 99.77%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3. WP1066 can cross the blood-brain barrier[1][2][3][4].

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 857064-38-1

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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고객리뷰

Based on 38 publication(s) in Google Scholar

38 Publications Citing Use of MCE WP1066

: WP1066 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2020 Feb;41(2):218-228. [Abstract]; HUVECs are pretreated with WP1066 for 1 h, followed by ZYZ-803 (1 μM) for 30 min. Protein levels are assessed by Western blot.

: WP1066 purchased from MedChemExpress. Usage Cited in: Cancer Manag Res. 2018 Nov 26:10:6339-6355. [Abstract]; Western blotting analysis: treatment with the Stat3 inhibitor WP1066 neutralizes the up-regulation of MMP2 and MMP9 and reverses the EMT progression caused by the overexpression of Uck2 in Bel-7402 cells.

: WP1066 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2017 Jul:108:542-553. [Abstract]; The role of STAT3 in SERPINB1-mediated protecting ALI in OALT is further confirmed by using STAT3 specific inhibitor WP1066. post-OALT lung STAT3 activation is significantly increased evidenced by elevated phosphorylation of STAT3 at site727 and site705 (P<0.01 vs sham), which are associated with enhanced HO-1 protein expression.

: WP1066 purchased from MedChemExpress. Usage Cited in: J Cancer. 2017 Feb 25;8(5):816-824. [Abstract]; The protein expression levels of p-Akt, t-Akt, p-STAT3, t-STAT3, MMP2 and MMP9 are determined via western blotting 48 h after knockdown of B7-H3 and blockade of the PI3K/Akt pathway using LY294002 or the STAT3 pathway using WP1066.

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JAK1 JAK2 JAK3 Tyk2 JAK

Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3. WP1066 can cross the blood-brain barrier[1][2][3][4].

IC₅₀ & Target^[1]^[2]

JAK2

STAT3

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	4.2 3 Compound: WP1066	Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay	[PMID: 34055214]
HeLa	IC₅₀	4.2 3 Compound: WP1066	Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay	[PMID: 34055214]
U-266	IC₅₀	1.5 3 Compound: WP1066	Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay	[PMID: 22036213]
U-266	IC₅₀	1.5 3 Compound: WP1066	Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay	[PMID: 22036213]
U-373MG ATCC	IC₅₀	3.7 3 Compound: WP1066	Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay	[PMID: 22036213]
U-373MG ATCC	IC₅₀	3.7 3 Compound: WP1066	Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay	[PMID: 22036213]
U-87MG ATCC	IC₅₀	5.6 3 Compound: WP1066	Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay	[PMID: 22036213]
U-87MG ATCC	IC₅₀	5.6 3 Compound: WP1066	Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay	[PMID: 22036213]
HeLa	IC₅₀	4.2 3 Compound: WP1066	Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay	[PMID: 34055214]
U-266	IC₅₀	1.5 3 Compound: WP1066	Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay	[PMID: 22036213]
U-373MG ATCC	IC₅₀	3.7 3 Compound: WP1066	Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay	[PMID: 22036213]
U-87MG ATCC	IC₅₀	5.6 3 Compound: WP1066	Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay	[PMID: 22036213]

In Vitro

WP1066 markedly inhibits the growth of HEL cells in a dose-dependent manner. The IC₅₀ value for inhibition of the proliferation of HEL cells is 2.3 μM. WP1066 inhibits the growth of human HEL cells carrying the JAK2 V617F mutant isoform^[1]. Blockade of p-STAT3 with WP1066 enhances the cytotoxic effects of CTX on the tumor. The IC₅₀ doses of WP1066 for B16 cells is 2.43 μM (0.865 μg/mL)^[2]. WP1066 inhibits AML blast colony-forming cell proliferation, suppresses normal BM progenitor proliferation at increased concentrations, and inhibits AML colony-forming cell proliferation^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

WP1066 (30 mg/kg, o.g.) exerts an additive effect to CTX inhibition of the p-STAT3 pathway within the tumor microenvironment^[2].
WP1066 shows excellent CNS penetration provided compelling rationale for testing WP1066 against a variety cancer^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

분자량

356.22

화학식

C₁₇H₁₄BrN₃O

CAS No.

857064-38-1

Appearance

Solid

Color

White to light yellow

SMILES

O=C(N[C@H](C1=CC=CC=C1)C)/C(C#N)=C/C2=NC(Br)=CC=C2

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

DMSO : ≥ 44 mg/mL (123.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 16.67 mg/mL (46.80 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8073 mL	14.0363 mL	28.0725 mL
5 mM	0.5615 mL	2.8073 mL	5.6145 mL
10 mM	0.2807 mL	1.4036 mL	2.8073 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기
농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (14.04 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.77%

Select Batch:

Data Sheet (280 KB) SDS (396 KB)

COA (249 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Verstovsek S, et al. WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation. Clin Cancer Res, 2008, (3), 788-796. [Content Brief]

[2]. Hatiboglu MA, et al. The tumor microenvironment expression of p-STAT3 influences the efficacy of WP1066 in murine melanoma models. Int J Cancer, 2012, 131(1), 8-17 [Content Brief]

[3]. Ferrajoli A, et al. WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells. Cancer Res, 2007, 67(23), 11291-11299. [Content Brief]

[4]. Kong L Y, et al. A novel inhibitor of STAT3 activation is efficacious against established central nervous system melanoma and inhibits regulatory T cells[J]. Clinical cancer research: an official journal of the American Association for Cancer Research, 2008, 14(18): 5759.

Cell Assay ^[1]	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 (5×10⁴ per well) are incubated in a total volume of 100 μL 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 μL 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. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
Animal Administration ^[2]	To ascertain the inhibition of the immune populations within the spleen and peripheral blood compartments, tumor-bearing mice are treated with CTX, WP1066, or CTX in combination with WP1066, for 14 days. Single-cell suspensions are prepared from spleens and the peripheral blood of mice and single cells are surface-stained with FITC-conjugated anti-CD4 (L3T4) or PE-conjugated anti-CD8 (53-6.7) and are intracellularly stained with APC-conjugated-FoxP3 (clone FJK-16s). The cell number of CD4⁺ and CD8⁺ T cells in the peripheral blood is counted based on positive surface staining of the respective markers relative to the total cell count of PBMCs. The percentage of FoxP3+ Tregs is calculated within the peripheral blood and within the CD4 compartment. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
References	[1]. Verstovsek S, et al. WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation. Clin Cancer Res, 2008, (3), 788-796. [Content Brief] [2]. Hatiboglu MA, et al. The tumor microenvironment expression of p-STAT3 influences the efficacy of WP1066 in murine melanoma models. Int J Cancer, 2012, 131(1), 8-17 [Content Brief] [3]. Ferrajoli A, et al. WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells. Cancer Res, 2007, 67(23), 11291-11299. [Content Brief] [4]. Kong L Y, et al. A novel inhibitor of STAT3 activation is efficacious against established central nervous system melanoma and inhibits regulatory T cells[J]. Clinical cancer research: an official journal of the American Association for Cancer Research, 2008, 14(18): 5759.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

Ethanol / DMSO	1 mM	2.8073 mL	14.0363 mL	28.0725 mL	70.1813 mL
	5 mM	0.5615 mL	2.8073 mL	5.6145 mL	14.0363 mL
	10 mM	0.2807 mL	1.4036 mL	2.8073 mL	7.0181 mL
	15 mM	0.1872 mL	0.9358 mL	1.8715 mL	4.6788 mL
	20 mM	0.1404 mL	0.7018 mL	1.4036 mL	3.5091 mL
	25 mM	0.1123 mL	0.5615 mL	1.1229 mL	2.8073 mL
	30 mM	0.0936 mL	0.4679 mL	0.9358 mL	2.3394 mL
	40 mM	0.0702 mL	0.3509 mL	0.7018 mL	1.7545 mL
DMSO	50 mM	0.0561 mL	0.2807 mL	0.5615 mL	1.4036 mL
	60 mM	0.0468 mL	0.2339 mL	0.4679 mL	1.1697 mL
	80 mM	0.0351 mL	0.1755 mL	0.3509 mL	0.8773 mL
	100 mM	0.0281 mL	0.1404 mL	0.2807 mL	0.7018 mL

WP1066 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WP1066857064-38-1WP 1066WP-1066STATJAKApoptosisJanus kinaseInhibitorinhibitorinhibit

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WP1066

고객리뷰

WP1066 Related Antibodies

38 Publications Citing Use of MCE WP1066

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•Related Screening Libraries:

•Related Small Molecules:

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View All STAT Isoform Specific Products:

View All JAK Isoform Specific Products:

Biological Activity

Protocol

순도&문서

References

고객리뷰

WP1066 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

WP1066 Related Classifications

Keywords:

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고객리뷰

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