Selumetinib sulfate (Synonyms: AZD6244 sulfate; ARRY-142886 sulfate)

Name: Selumetinib sulfate
Brand: MedChemExpress
SKU: HY-50706A
Rating: 5.0 (66 reviews)

Cat. No.: HY-50706A Purity: 99.58%: FAQs
Data Sheet SDS COA Handling Instructions

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Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC₅₀ of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.

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

Selumetinib sulfate Chemical Structure

CAS No. : 943332-08-9

Size	Price	Stock	Quantity

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 79	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 79	In-stock	Estimated Time of Arrival: December 31
Solid
50 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 156	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
1 g	USD 468	In-stock	Estimated Time of Arrival: December 31
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Based on 66 publication(s) in Google Scholar

Other Forms of Selumetinib sulfate:

Selumetinib In-stock

61 Publications Citing Use of MCE Selumetinib sulfate

: Selumetinib sulfate purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2018 Apr 19;12:911-920. [Abstract]; Immunoblotting demonstrates that AZD6244 can effectively restore upregulation of LC3-II/I and downregulation of p62 induced by RAD001 in 786-O and A498 cells.

: Selumetinib sulfate purchased from MedChemExpress. Usage Cited in: PLoS One. 2018 Jul 5;13(7):e0200014. [Abstract]; Representative immunoblots of control and NHA^RAS treated with Selumetinib for 24 h.

: Selumetinib sulfate purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Feb;16(2):334-343. [Abstract]; Selumetinib treatment results in decreased phosphorylation of ERK1/2. Effect of Selumetinib on the expression and phosphorylation of ERK and AKT in the gastrocnemius muscle of cancer cachexia model.

: Selumetinib sulfate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Feb 28;8(9):14835-14846. [Abstract]; MEK inhibition results in reduced ERK phosphorylation.A. Western blot analysis of SEM and KOPN8 exposed to 500 nM of MEK inhibitor or vehicle control (DMSO) for 6, 24 and 48 hours. Both cell lines almost completely lose ERK phosphorylation (p-ERK), while total ERK (t-ERK) levels remain unaffected. B. Analysis of MEK phosphorylation (p-MEK) suggests exposure to MEK162 and Selumetinib results in enhanced MEK phosphorylation in both cell lines, whereas total MEK (t-MEK) levels remain constant.

: Selumetinib sulfate purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2014 Nov 1;20(21):5483-95. [Abstract]; Effects of AZD6244 as single agents, respectively, on mediators of IGF-1R- and ERK1/ERK2-signaling pathways.Effect of AZD6244 on IGF-1R protein expression levels, and phosphorylation of Erk1/Erk2.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC₅₀ of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.

In Vitro

Selumetinib (AZD6244) causes a time- and dose-dependent reduction in DNA synthesis and cell viability in primary, induces growth arrest and apoptosis associated with the inactivation of ERK in primary 2-1318 cells^[1].
Selumetinib (AZD6244) (1µM) shows anti-proliferative effects through G0/G1 arrest on H-441, H-1437 cells^[2].
Selumetinib (AZD6244) results in the growth inhibition of several cell lines containing B-Raf and Ras mutations but has no effect on a normal fibroblast cell line^[3].

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

In Vivo

Selumetinib (AZD6244, 50 and 100 mg/kg, p.o.) decreases the growth rate of 4-1318 xenografts in a dose-dependent manner; AZD6244 when given at the dose of 50 mg/kg also significantly suppresses the growth of the 5-1318, 2-1318, 26-1004, and 29-1104 xenografts^[1].
Selumetinib (ARRY-142886, 10, 25, 50, or 100 mg/kg, p.o.) is capable of inhibiting both ERK1/2 phosphorylation and growth of HT-29 xenograft tumors in nude mice. Tumor regressions are also seen in a BxPC3 xenograft model^[3].

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

Clinical Trial

Molecular Weight

555.76

Formula

C₁₇H₁₇BrClFN₄O₇S

CAS No.

943332-08-9

Appearance

Solid

Color

Light yellow to yellow

SMILES

OCCONC(C(C=C1C(N=CN1C)=C2F)=C2NC3=C(C=C(Br)C=C3)Cl)=O.O=S(O)(O)=O

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 : 50 mg/mL (89.97 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	1.7993 mL	8.9967 mL	17.9934 mL
5 mM	0.3599 mL	1.7993 mL	3.5987 mL
10 mM	0.1799 mL	0.8997 mL	1.7993 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 (4.50 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 (4.50 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.50 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 10 mg/mL (17.99 mM); Suspended solution; Need ultrasonic

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: 99.58%

Select Batch:

Data Sheet (278 KB) SDS (701 KB)

COA (253 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. [1].Huynh H, et al, Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma. Mol Cancer Therapy, 2007, 6 (1), 138-146 [Content Brief]

[2]. [2].Garon EB, et al. Identification of common predictive markers of in vitro response to the Mek inhibitor selumetinib (AZD6244; ARRY-142886) in human breast cancer and non-small cell lung cancer cell lines. Mol Cancer Thera, 2010, 9 (7), 1985-1994. [Content Brief]

[3]. [3].Yeh TC, et al. Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clin Cancer Res, 2007, 13 (5), 1576-1583. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.7993 mL	8.9967 mL	17.9934 mL	44.9834 mL
	5 mM	0.3599 mL	1.7993 mL	3.5987 mL	8.9967 mL
	10 mM	0.1799 mL	0.8997 mL	1.7993 mL	4.4983 mL
	15 mM	0.1200 mL	0.5998 mL	1.1996 mL	2.9989 mL
	20 mM	0.0900 mL	0.4498 mL	0.8997 mL	2.2492 mL
	25 mM	0.0720 mL	0.3599 mL	0.7197 mL	1.7993 mL
	30 mM	0.0600 mL	0.2999 mL	0.5998 mL	1.4994 mL
	40 mM	0.0450 mL	0.2249 mL	0.4498 mL	1.1246 mL
	50 mM	0.0360 mL	0.1799 mL	0.3599 mL	0.8997 mL
	60 mM	0.0300 mL	0.1499 mL	0.2999 mL	0.7497 mL
	80 mM	0.0225 mL	0.1125 mL	0.2249 mL	0.5623 mL

Selumetinib sulfate 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:

Selumetinib943332-08-9AZD6244ARRY-142886AZD 6244AZD-6244ARRY142886ARRY 142886MEKApoptosisMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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Selumetinib sulfate (Synonyms: AZD6244 sulfate; ARRY-142886 sulfate)

Customer Review

Other Forms of Selumetinib sulfate:

Selumetinib sulfate Related Antibodies

61 Publications Citing Use of MCE Selumetinib sulfate

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

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View All MEK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Selumetinib sulfate Related Antibodies

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Complete Stock Solution Preparation Table

Selumetinib sulfate Related Classifications

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