WEHI-539 hydrochloride

Name: WEHI-539 hydrochloride
Brand: MedChemExpress
SKU: HY-15607A
Rating: 5.0 (31 reviews)

Cat. No.: HY-15607A Purity: 99.72%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL with an IC₅₀ of 1.1 nM.

For research use only. We do not sell to patients.

WEHI-539 hydrochloride Chemical Structure

CAS No. : 2070018-33-4

Size	Stock	Quantity

Free Sample (0.1 - 0.5 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 31 publication(s) in Google Scholar

Other Forms of WEHI-539 hydrochloride:

WEHI-539 Get quote

27 Publications Citing Use of MCE WEHI-539 hydrochloride

Proliferation Assay

: WEHI-539 hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2018 Feb 1;142(3):584-596. [Abstract]; Evaluation of PARP protein cleavage in Mneo and MXL90 cells after treatment for 24h with 20 μM NSC 119875, in presence of increasing doses of the specific Bcl-xL inhibitor WEHI-539.

: WEHI-539 hydrochloride purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 May 25;9(40):26046-26063. [Abstract]; Representative images of Hoechst/PI merged channels for WEHI-539 treatment in MCF7-pSFFV cell line.

: WEHI-539 hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2017 Jan;24(1):111-119. [Abstract]; BCL-XL-BIK complexes can be dissociated using the BCL-XL-inhibitor WEHI-539.

: WEHI-539 hydrochloride purchased from MedChemExpress. Usage Cited in: Blood. 2014 Dec 4;124(24):3587-96. [Abstract]; CD41⁺ or CD41⁻ cells are treated with DMSO as a vehicle control or a BCL-xL inhibitor (WEHI-539; 0.2, 0.4, and 0.8 μM) on OP9 stromal cells in the presence of THPO for 7 days. The number of viable cells is counted.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL with an IC₅₀ of 1.1 nM.

IC₅₀ & Target^[1]

Bcl-xL

1.1 nM (IC₅₀)

In Vitro

WEHI-539 hydrochloride is a selective inhibitor of Bcl-X_L. WEHI-539 augments NSC 241240 induced caspase 3/7 activity, PARP cleavage and annexin V labelling. WEHI-539 as a single agent causes noticeable PARP cleavage in Ovcar-4 (5 μM in Ovcar-4.) and Ovsaho (1 μM in Ovsaho) cells^[2].

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

Molecular Weight

620.18

Formula

C₃₁H₃₀ClN₅O₃S₂

CAS No.

2070018-33-4

Appearance

Solid

Color

Light yellow to light brown

SMILES

OC(C1=C(CCCOC2=CC=C(CN)C=C2)SC(C3=CC4=C(CCC/C4=N\NC5=NC(C=CC=C6)=C6S5)C=C3)=N1)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 16.67 mg/mL (26.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6124 mL	8.0622 mL	16.1244 mL
5 mM	0.3225 mL	1.6124 mL	3.2249 mL
10 mM	0.1612 mL	0.8062 mL	1.6124 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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: ≥ 2.5 mg/mL (4.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.03 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.

Purity & Documentation

Purity: 99.72%

Select Batch:

Data Sheet (279 KB) SDS (252 KB)

COA (255 KB) HNMR (420 KB) RP-HPLC (270 KB) LCMS (106 KB)

Handling Instructions (2659 KB)

References

[1]. Lessene G, et al. Structure-guided design of a selective BCL-X(L) inhibitor. Nat Chem Biol. 2013 Jun;9(6):390-7. [Content Brief]

[2]. Abed MN, et al. Antagonism of Bcl-XL is necessary for synergy between NSC 241240 and BH3 mimetics in ovarian cancer cells. J Ovarian Res. 2016 Apr 14;9:25. [Content Brief]

Cell Assay
^[2]

Ovcar-8, Ovcar-3, Ovcar-4 and Ovsaho cells are grown in the RPMI, Igrov-1, Cov-362 and Cov-318 cells are grown in DMEM and Fuov-1 cells are grown in DMEM/F-12 nutrient mixture. ABT-737, ABT-199 and WEHI-539 (Medchem Express, NJ, USA), are prepared as a 20 mM solution in DMSO. For cell growth assays, cells are plated in 96 wells plate (5,000 cells/well for all cell lines except Ovcar-8 which is plated at a density of 2,500 cells/well). The next day, cells are treated with drugs. After 72 h the culture medium is removed and the cells are fixed with 100 μL of cold 10 % Trichloroacetic acid (TCA), incubated on ice for 30 min and stained with 0.4 % sulforhodamine B (SRB). The data are analysed by using Graphpad Prism 4 software. Non-linear regression is used to fit a four parameters Hill equation. For drug combinations studies the cells are exposed simultaneously to a range of concentrations of NSC 241240 combined with fixed concentration of BH3 mimetics that is expected from the single agent studies to cause 5 % growth inhibition: ABT-737, 1 μM in Ovcar-8, Ovcar-3 and Igrov-1, 2 μM in Ovcar-4 and Ovsaho and 6 μM in Cov-362; ABT-199, 1 μM in Ovcar-4, 2 μM in Ovcar-3, Igrov-1, Cov-362 and Ovsaho and 3 μM in Ovcar-8; WEHI-539, 0.2 μM in Igrov-1, 0.3 μM in Ovcar-8, 1 μM in Ovcar-3 and Ovsaho, 3.1 μM in Cov-362 and 5 μM in Ovcar-4. Surviving cell number is assessed by SRB staining. A combination index (CI) is calculated^[2].

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

References

[1]. Lessene G, et al. Structure-guided design of a selective BCL-X(L) inhibitor. Nat Chem Biol. 2013 Jun;9(6):390-7. [Content Brief]

[2]. Abed MN, et al. Antagonism of Bcl-XL is necessary for synergy between NSC 241240 and BH3 mimetics in ovarian cancer cells. J Ovarian Res. 2016 Apr 14;9:25. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.6124 mL	8.0622 mL	16.1244 mL	40.3109 mL
	5 mM	0.3225 mL	1.6124 mL	3.2249 mL	8.0622 mL
	10 mM	0.1612 mL	0.8062 mL	1.6124 mL	4.0311 mL
	15 mM	0.1075 mL	0.5375 mL	1.0750 mL	2.6874 mL
	20 mM	0.0806 mL	0.4031 mL	0.8062 mL	2.0155 mL
	25 mM	0.0645 mL	0.3225 mL	0.6450 mL	1.6124 mL