GW806742X hydrochloride

Name: GW806742X hydrochloride
Brand: MedChemExpress
SKU: HY-112292A
Rating: 5.0 (23 reviews)

Cat. No.: HY-112292A Purity: 98.30%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a K_d of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC₅₀=2 nM). GW806742X hydrochloride retards MLKL membrane translocation and inhibits necroptosis.

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

CAS No. : 2930350-95-9

Size	Stock	Quantity
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 23 publication(s) in Google Scholar

Other Forms of GW806742X hydrochloride:

GW806742X In-stock

23 Publications Citing Use of MCE GW806742X hydrochloride

Cell Proliferation/Viability Assay

IHC

In Vivo Imaging

: GW806742X hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 18;15(1):6043. [Abstract]; WB analysis of necroptosis markers after 48 h treatment with different necroptosis inhibitors. The inhibitors used were Nec-1 (50 µM, a RIPK1 inhibitor), GSK-872 (3 µM, a RIPK3 inhibitor), and GW806742X (1 µM, an MLKL inhibitor).

: GW806742X hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 18;15(1):6043. [Abstract]; WB analysis of PCNA in cells untreated/treated with GW806742X (1 µM) for 48 h.

: GW806742X hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 18;15(1):6043. [Abstract]; CD47 IHC staining of primary tumours from C57BL/6 orthotopic model received different treatments: saline, anti-mouse IL6 (200 µg, iv., 3×/week), or GW806742X (100 µM in 50 µl, iv., 3×/week); mice were euthanized 4 weeks after injection.

: GW806742X hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 18;15(1):6043. [Abstract]; Bioluminescence of total tumour burden in C57BL/6 orthotopic model received different treatments: saline, GW806742X (100 µM in 50 µl, iv., 3×/week), anti-mCD47 (400 µg, ip., 3×/week) or both since day 7 after injection (106 KPC OE-MLKL cells); Images were collected at four weeks after injection; (8 mice per group).

: GW806742X hydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2023 Mar;615(7950):158-167. [Abstract]; Cell viability assessment in Tbk1-null B16 cells pre-treated with RIPK3 inhibitor (HS-1371, 2 μM) or MLKL inhibitor (GW806742X, 5 μM) and the pan-caspase inhibitor Q-VD-Oph (20 μM) +/− TNFα/IFNγ for 9 days (n=6, 2 independent experiments: 2-way ANOVA, Dunnett’s multiple comparisons test).

: GW806742X hydrochloride purchased from MedChemExpress. Usage Cited in: Autophagy. 2022 Apr;18(4):726-744. [Abstract]; Western blots for levels of p-MLKL and MLKL in wild type (WT) L929 cells untreated or treated with either TSZ for 6 h or ECS for 3 h. GW806742X (GW, 1 µM) was included in some samples as indicated 0.5 h before and during the treatment.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]

MLKL

9.3 μM (Kd)

VEGFR2

2 nM (IC₅₀)

In Vitro

GW806742X (0.1-10000 nM) inhibits necroptotic death of wild-type mouse dermal fibroblasts (MDFs) stimulated with TSQ (1 ng/mL TNF, 500 nM compound A (Smac mimetic), 10 μM Q-VD-OPh) in a dose-dependent manner^[1].
GW806742X shows inhibition of VEGF induced proliferation of HUVECs with an IC50 of 5 nM^[2].

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

Molecular Weight

610.01

Formula

C₂₅H₂₃ClF₃N₇O₄S

CAS No.

2930350-95-9

Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=CC(NC2=NC=CC(N(C)C3=CC=C(NC(NC4=CC=C(OC(F)(F)F)C=C4)=O)C=C3)=N2)=C1)(N)=O.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 : 100 mg/mL (163.93 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	1.6393 mL	8.1966 mL	16.3932 mL
5 mM	0.3279 mL	1.6393 mL	3.2786 mL
10 mM	0.1639 mL	0.8197 mL	1.6393 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.10 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 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 98.30%

Select Batch:

Data Sheet (272 KB) SDS (252 KB)

COA (245 KB) HNMR (314 KB) LCMS (107 KB)

Handling Instructions (2659 KB)

References

[1]. Hildebrand JM, et al. Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death. Proc Natl Acad Sci U S A. 2014;111(42):15072-15077. [Content Brief]

[2]. Sammond DM, et al. Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase. Bioorg Med Chem Lett. 2005;15(15):3519-3523. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.6393 mL	8.1966 mL	16.3932 mL	40.9829 mL
	5 mM	0.3279 mL	1.6393 mL	3.2786 mL	8.1966 mL
	10 mM	0.1639 mL	0.8197 mL	1.6393 mL	4.0983 mL
	15 mM	0.1093 mL	0.5464 mL	1.0929 mL	2.7322 mL
	20 mM	0.0820 mL	0.4098 mL	0.8197 mL	2.0491 mL
	25 mM	0.0656 mL	0.3279 mL	0.6557 mL	1.6393 mL
	30 mM	0.0546 mL	0.2732 mL	0.5464 mL	1.3661 mL
	40 mM	0.0410 mL	0.2049 mL	0.4098 mL	1.0246 mL
	50 mM	0.0328 mL	0.1639 mL	0.3279 mL	0.8197 mL
	60 mM	0.0273 mL	0.1366 mL	0.2732 mL	0.6830 mL
	80 mM	0.0205 mL	0.1025 mL	0.2049 mL	0.5123 mL
	100 mM	0.0164 mL	0.0820 mL	0.1639 mL	0.4098 mL