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Selumetinib (sulfate)

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.

Product Specifications

CAS Number

[943332-08-9]

Product Name Alternative

AZD6244 (sulfate) ; ARRY-142886 (sulfate)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; MEK

Type

Reference compound

Related Pathways

Apoptosis; MAPK/ERK Pathway

Applications

Neuroscience-Neurodegeneration

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/selumetinib-sulfate.html

Purity

99.58

Solubility

DMSO : 50 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL

Smiles

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

Molecular Formula

C17H17BrClFN4O7S

Molecular Weight

555.76

Precautions

H302, H315, H319, H335

References & Citations

[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|[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.|[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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Launched

Citation 01

OMICS. 2025 Sep;29 (9) :458-472.|ACS Comb Sci. 2019 Dec 9;21 (12) :805-816.|Adv Sci (Weinh) . 2025 Nov 21:e11943.|Allegheny College. 2017-5-2.|Anal Chem. 2025 Jun 3;97 (21) :11099-11109.|Biochem Genet. 2024 Feb;62 (1) :242-253.|Biochem Pharmacol. 2025 Jan 9:116744.|Bioengineering (Basel) . 2025 Oct 19;12 (10) :1121.|Biomolecules. 2021 Mar 30;11 (4) :518.|bioRxiv. 2019 Sep.|bioRxiv. 2023 Jan 17.|bioRxiv. 2024 Nov 6:2024.11.04.621884.|bioRxiv. 2025 Apr 26:2025.04.24.650512.|bioRxiv. 2025 Jan 1.|bioRxiv. 2025 January 31.|bioRxiv. 2025 March 02.|bioRxiv. 2025 Sep 16:2025.09.10.675396.|bioRxiv. 2025 Sep 21.|Br J Cancer. 2023 Feb;128 (4) :678-690.|Cancer Cell. 2020 Mar 16;37 (3) :387-402.e7. |Cancer Res. 2024 Sep 16;84 (18) :2985-3003.|Cancer Sci. 2024 Feb;115 (2) :412-426.|Cell Death Discov. 2023 Sep 19;9 (1) :347.|Cell Rep Med. 2025 Feb 6:101970.|Cell Res. 2018 Dec;28 (12) :1171-1185. |Cell Syst. 2018 Apr 25;6 (4) :424-443.e7.|Cell Syst. 2020 Nov 18;11 (5) :478-494.e9.|Chemotherapy. 2021;66 (5-6) :169-178.|Clin Cancer Res. 2014 Dec 1;20 (23) :6034-44. |Clin Cancer Res. 2014 Nov 1;20 (21) :5483-95. |Clin Cancer Res. 2020 Apr 15;26 (8) :2011-2021. |Comput Struct Biotechnol J. 2019 Feb 8:17:352-361.|Drug Des Devel Ther. 2018 Apr 19:12:911-920.|Drug Resist Updat. 2024 May:74:101079.|Epigenetics. 2023 Dec;18 (1) :2254976.|Eur J Haematol. 2023 Apr;110 (4) :435-443.|Eur J Nucl Med Mol Imaging. 2022 Nov;49 (13) :4312-4324.|Exp Cell Res. 2025 Jan 15;444 (2) :114377.|Front Med. 2021 Mar 23;8:625130.|Gastroenterologie, Hepatologie und Endokrinologie. 2020 Oct.|Genome Med. 2016 Oct 31;8 (1) :116.|Glia. 2019 Jul;67 (7) :1320-1332. |Gynecol Oncol. 2020 Dec;159 (3) :827-838.|Harvard Medical School LINCS LIBRARY|Hepatol Commun. 2019 Feb 5;3 (3) :423-436.|J Cell Mol Med. 2020 Mar;24 (6) :3336-3345.|J Exp Clin Cancer Res. 2021 Jan 9;40 (1) :25.|J Hematol Oncol. 2020 Feb 22;13 (1) :13.|J Invest Dermatol. 2022 Mar;142 (3 Pt A) :613-623.e7.|J Neuroinflammation. 2022 Mar 14;19 (1) :67.|J Pathol. 2023 Jun;260 (2) :203-221.|J Transl Med. 2023 Jan 9;21 (1) :9.|Lipids. 2019 Oct;54 (10) :603-616.|Mol Cancer Ther. 2015 Oct;14 (10) :2249-59.|Mol Cancer Ther. 2017 Feb;16 (2) :334-343.|Mol Carcinog. 2024 Apr 17|Mol Carcinog. 2024 Jul;63 (7) :1235-1247.|Mol Oncol. 2020 Nov;14 (11) :2894-2919.|Mol Pharmacol. 2019 Dec;96 (6) :862-870.|Mol Syst Biol. 2015 Mar 26;11 (3) :797. |Mol Ther Oncolytics. 2019 Feb 5;12:235-245.|Nat Commun. 2025 Feb 1;16 (1) :1237.|Neuro Oncol. 2019 Mar 18;21 (4) :486-497. |Oncogenesis. 2019 Nov 4;8 (11) :65. |Oncol Res. 2024 Mar 20;32 (4) :753-768.|Oncotarget. 2017 Feb 28;8 (9) :14835-14846. |Oncotarget. 2020 Nov 3;11 (44) :3921-3932.|Patent. US20170020964A1.|Patent. US20170326205A1.|Patent. US20210299273A1.|Patent. US9724393B2.|PLoS One. 2018 Jul 5;13 (7) :e0200014.|Res Sq. 2025 May 16:rs.3.rs-6590535.|Res Sq. 2025 Sep 23.|Research (Wash D C) . 2025 Apr 3:8:0649.|Research Square Preprint. 2024 Nov 06.|Research Square Print. September 27th, 2022.|Sci Data. 2024 Sep 19;11 (1) :1024.|Sci Signal. 2018 Oct 30;11 (554) :eaar6795.|Signal Transduct Target Ther. 2025 Oct 3;10 (1) :326.|Universitat Autònoma de Barcelona. Biologia Molecular i Biomedicina. 2022 Aug.|University of Düsseldorf. 2024.

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