Selumetinib sulfate
Based on 98 publication(s) in Google Scholar
Selumetinib (AZD6244) sulfate is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) sulfate inhibits ERK1/2 phosphorylation. Selumetinib sulfate can penetrate the blood brain barrier (BBB).
For research use only. We do not sell to patients.
- Purity: 99.58%
- CAS No.: 943332-08-9
- Formula: C17H17BrClFN4O7S
- Molecular Weight:555.76
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Selumetinib sulfate
More- Signal Transduct Target Ther. 2025 Oct 3;10(1):326. [Abstract]
- Cancer Cell. 2020 Mar 16;37(3):387-402.e7. [Abstract]
- J Hematol Oncol. 2020 Feb 22;13(1):13. [Abstract]
- Cell Res. 2018 Dec;28(12):1171-1185. [Abstract]
- Nat Cancer. 2026 Jan;7(1):116-130. [Abstract]
- Cell Host Microbe. 2026 Feb 11;34(2):245-262.e8. [Abstract]
- Cancer Res. 2024 Sep 16;84(18):2985-3003. [Abstract]
- Drug Resist Updat. 2024 May:74:101079. [Abstract]
- Nat Commun. 2026 Jun 17;17(1):5361. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2025 Feb 1;16(1):1237. [Abstract]
- Acta Pharm Sin B. 2026 Jun 8.
- J Exp Clin Cancer Res. 2021 Jan 9;40(1):25. [Abstract]
- Adv Sci (Weinh). 2025 Nov 21:e11943. [Abstract]
- Cell Rep Med. 2025 Feb 6:101970. [Abstract]
- Sci Adv. 2026 Jan 30;12(5):eady8382. [Abstract]
- Neuro Oncol. 2019 Mar 18;21(4):486-497. [Abstract]
- Research (Wash D C). 2025 Apr 3:8:0649. [Abstract]
- J Immunother Cancer. 2025 Dec 1;13(12):e012800. [Abstract]
- J Neuroinflammation. 2022 Mar 14;19(1):67. [Abstract]
- Clin Cancer Res. 2020 Apr 15;26(8):2011-2021. [Abstract]
- Clin Cancer Res. 2014 Dec 1;20(23):6034-44. [Abstract]
- Clin Cancer Res. 2014 Nov 1;20(21):5483-95. [Abstract]
- Genome Med. 2016 Oct 31;8(1):116. [Abstract]
- Cell Death Discov. 2023 Sep 19;9(1):347. [Abstract]
- J Transl Med. 2026 Feb 4;24(1):385. [Abstract]
- J Transl Med. 2023 Jan 9;21(1):9. [Abstract]
- Apoptosis. 2026 May 24;31(6):150. [Abstract]
- Leukemia. 2026 Mar 25. [Abstract]
- Mol Ther Oncolytics. 2019 Feb 5;12:235-245. [Abstract]
- Br J Cancer. 2023 Feb;128(4):678-690. [Abstract]
- Cell Rep. 2026 Jun 18;45(7):117576. [Abstract]
- Eur J Nucl Med Mol Imaging. 2022 Nov;49(13):4312-4324. [Abstract]
- Cell Syst. 2020 Nov 18;11(5):478-494.e9. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- J Invest Dermatol. 2022 Mar;142(3 Pt A):613-623.e7. [Abstract]
- Sci Signal. 2018 Oct 30;11(554):eaar6795. [Abstract]
- Mol Cancer Ther. 2017 Feb;16(2):334-343. [Abstract]
- Mol Cancer Ther. 2015 Oct;14(10):2249-59. [Abstract]
- Mol Syst Biol. 2015 Mar 26;11(3):797. [Abstract]
- Biochem Pharmacol. 2025 Jan 9:116744. [Abstract]
- Drug Des Devel Ther. 2018 Apr 19:12:911-920. [Abstract]
- Oncogenesis. 2019 Nov 4;8(11):65. [Abstract]
- Hepatol Commun. 2019 Feb 5;3(3):423-436. [Abstract]
- Cell Rep Methods. 2026 Jun 15;6(6):101339. [Abstract]
- Biomolecules. 2021 Mar 30;11(4):518. [Abstract]
- Glia. 2019 Jul;67(7):1320-1332. [Abstract]
- J Pathol. 2023 Jun;260(2):203-221. [Abstract]
- Cancer Sci. 2024 Feb;115(2):412-426. [Abstract]
- Comput Struct Biotechnol J. 2019 Feb 8:17:352-361. [Abstract]
- J Cell Mol Med. 2020 Mar;24(6):3336-3345. [Abstract]
- Oncol Res. 2024 Mar 20;32(4):753-768. [Abstract]
- Mol Oncol. 2020 Nov;14(11):2894-2919. [Abstract]
- Gynecol Oncol. 2020 Dec;159(3):827-838. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- J Virol. 2026 Mar 24;100(3):e0195225. [Abstract]
- Epigenetics. 2023 Dec;18(1):2254976. [Abstract]
- Exp Cell Res. 2025 Jan 15;444(2):114377. [Abstract]
- Mol Carcinog. 2024 Jul;63(7):1334-1348. [Abstract]
- Mol Carcinog. 2024 Jul;63(7):1235-1247. [Abstract]
- Mol Pharmacol. 2019 Dec;96(6):862-870. [Abstract]
- PLoS One. 2018 Jul 5;13(7):e0200014. [Abstract]
- Eur J Haematol. 2023 Apr;110(4):435-443. [Abstract]
- OMICS. 2025 Sep;29(9):458-472. [Abstract]
- Biochem Genet. 2024 Feb;62(1):242-253. [Abstract]
- Lipids. 2019 Oct;54(10):603-616. [Abstract]
- Chemotherapy. 2021;66(5-6):169-178. [Abstract]
- Res Sq. 2026 May 20.
- bioRxiv. 2026 Apr 21:2026.04.16.719008. [Abstract]
- Res Sq. 2026 Feb 18.
- Charles University. 2026.
- bioRxiv. 2025 Sep 21.
- Res Sq. 2025 Sep 23.
- bioRxiv. 2025 Sep 16:2025.09.10.675396. [Abstract]
- bioRxiv. 2025 Jan 1.
- Res Sq. 2025 May 16:rs.3.rs-6590535. [Abstract]
- bioRxiv. 2025 Apr 26:2025.04.24.650512. [Abstract]
- bioRxiv. 2025 March 02.
- bioRxiv. 2025 January 31.
- bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
- University of Düsseldorf. 2024.
- Research Square Preprint. 2024 Nov 06.
- bioRxiv. 2023 Jan 17.
- Research Square Print. September 27th, 2022.
- Universitat Autònoma de Barcelona. 2022 Aug.
- Patent. US20210299273A1.
- Front Med. 2021 Mar 23;8:625130. [Abstract]
- Oncotarget. 2020 Nov 3;11(44):3921-3932. [Abstract]
- Medizinische Hochschule Hannover. 2020 Oct.
- ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]
- bioRxiv. 2019 Sep.
- Patent. US20170326205A1.
- Patent. US9724393B2.
- Allegheny College. 2017 May 2.
- Oncotarget. 2017 Feb 28;8(9):14835-14846. [Abstract]
- Patent. US20170020964A1.
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All MEK Isoforms
More
Biological Activity
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 943332-08-9
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Appearance Solid
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Molecular Weight 555.76
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Formula C17H17BrClFN4O7S
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Color Light yellow to yellow
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SMILES
OCCONC(C(C=C1C(N=CN1C)=C2F)=C2NC3=C(C=C(Br)C=C3)Cl)=O.O=S(O)(O)=O
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Synonyms
AZD6244 sulfate; ARRY-142886 sulfate
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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)
Publications (98)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Retinol Binding Protein 4 reactivates latent HIV-1 by triggering canonical NF-κB, JAK/STAT5 and JNK signalling. [Abstract]2025 Oct 3;10(1):326. PMID: 41038866 -
Cancer Cell
2020 Mar 16;37(3):387-402.e7. PMID: 32142667
Selumetinib sulfate purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2020 Mar 16;37(3):387-402.e7. [Abstract]
MCF-7 cells were seeded in 10-11 M E2 to which fulvestrant (F), dabrafenib (D), trametinib (T) or selumetinib (S) were subsequently added at 10-9, 10-6, 10-7 or 10-6 M, respectively. After 6 days, proteins were measured by immunoblotting, and phosphorylation levels (as defined by the levels of the phosphorylated form over total protein) relative to the vehicle-treated cells were set to 1.
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J Hematol Oncol
Combination of PI3K and MEK inhibitors yields durable remission in PDX models of PIK3CA-mutated metaplastic breast cancers. [Abstract]2020 Feb 22;13(1):13. PMID: 32087759 -
Cell Res
2018 Dec;28(12):1171-1185. PMID: 30287942 -
Nat Cancer
The MEK-RAF molecular glue IK-595 has potent antitumor activity across RAS/MAPK pathway-altered cancers. [Abstract]2026 Jan;7(1):116-130. PMID: 41482524 -
Cell Host Microbe
Enterococcus faecalis-derived lactic acid suppresses macrophage activation to facilitate persistent and polymicrobial wound infections. [Abstract]2026 Feb 11;34(2):245-262.e8. PMID: 41605216 -
Cancer Res
Oncogenic Calreticulin Induces Immune Escape by Stimulating TGF-β Expression and Regulatory T Cell Expansion in the Bone Marrow Microenvironment. [Abstract]2024 Sep 16;84(18):2985-3003. PMID: 38885318 -
Drug Resist Updat
TRIM29 facilitates gemcitabine resistance via MEK/ERK pathway and is modulated by circRPS29/miR-770-5p axis in PDAC. [Abstract]2024 May:74:101079. PMID: 38518727 -
Nat Commun
Induced pluripotent stem cell-derived models of malignant nerve sheath tumor progression mimic glial to neuro-mesenchymal transition and uncover therapeutic opportunities. [Abstract]2026 Jun 17;17(1):5361. PMID: 42310314 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
PPARα-mediated lipid metabolism reprogramming supports anti-EGFR therapy resistance in head and neck squamous cell carcinoma. [Abstract]2025 Feb 1;16(1):1237. PMID: 39890801 -
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J Exp Clin Cancer Res
2021 Jan 9;40(1):25. PMID: 33422093 -
Adv Sci (Weinh)
Lipid-Driven OLR1/FOXM1/FGF19 Axis Orchestrates Crosstalk in an Epithelial-Fibroblast Positive Feedback Promoting Progesterone Resistance in Endometrial Cancer. [Abstract]2025 Nov 21:e11943. PMID: 41270216 -
Cell Rep Med
2025 Feb 6:101970. PMID: 39938523 -
Sci Adv
Inhibition of focal adhesion kinase impairs tumor formation and preserves hearing in a murine model of NF2-related schwannomatosis. [Abstract]2026 Jan 30;12(5):eady8382. PMID: 41616055 -
Neuro Oncol
Preclinical assessment of MEK1/2 inhibitors for neurofibromatosis type 2-associated schwannomas reveals differences in efficacy and drug resistance development. [Abstract]2019 Mar 18;21(4):486-497. PMID: 30615146 -
Research (Wash D C)
EGF-Upregulated lncRNA ESSENCE Promotes Colorectal Cancer Growth through Stabilizing CAD and Ferroptosis Defense. [Abstract]2025 Apr 3:8:0649. PMID: 40190348 -
J Immunother Cancer
Tempered signal strength via low-dose MEK inhibition optimizes therapeutic performance of engineered T cells. [Abstract]2025 Dec 1;13(12):e012800. PMID: 41330614 -
J Neuroinflammation
Homer1 promotes the conversion of A1 astrocytes to A2 astrocytes and improves the recovery of transgenic mice after intracerebral hemorrhage. [Abstract]2022 Mar 14;19(1):67. PMID: 35287697 -
Clin Cancer Res
Gene Expression Signatures Identify Novel Therapeutics for Metastatic Pancreatic Neuroendocrine Tumors. [Abstract]2020 Apr 15;26(8):2011-2021. PMID: 31937620 -
Clin Cancer Res
MHC class I loss is a frequent mechanism of immune escape in papillary thyroid cancer that is reversed by interferon and selumetinib treatment in vitro. [Abstract]2014 Dec 1;20(23):6034-44. PMID: 25294906 -
Clin Cancer Res
Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R. [Abstract]2014 Nov 1;20(21):5483-95. PMID: 25186968
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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Genome Med
A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma. [Abstract]2016 Oct 31;8(1):116. PMID: 27799065 -
Cell Death Discov
Cross-species analysis of SHH medulloblastoma models reveals significant inhibitory effects of trametinib on tumor progression. [Abstract]2023 Sep 19;9(1):347. PMID: 37726268 -
J Transl Med
Personalized medicine strategy for MPNSTs: using precision oncology on PDOX models to inform tumor boards. [Abstract]2026 Feb 4;24(1):385. PMID: 41639724 -
J Transl Med
Papillary thyroid cancer organoids harboring BRAFV600E mutation reveal potentially beneficial effects of BRAF inhibitor-based combination therapies. [Abstract]2023 Jan 9;21(1):9. PMID: 36624452 -
Apoptosis
A pH-responsive silver nanoparticle platform overcomes MEK inhibitor resistance in neurofibroma via triacsin C-mediated lipid metabolic reprogramming. [Abstract]2026 May 24;31(6):150. PMID: 42177691 -
Leukemia
A Perturb-seq map of a differentiation hub reveals synergistic vulnerabilities in KMT2A-rearranged acute myeloid leukemia. [Abstract]2026 Mar 25. PMID: 41882099 -
Mol Ther Oncolytics
MAPK Inhibitors Enhance HDAC Inhibitor-Induced Redifferentiation in Papillary Thyroid Cancer Cells Harboring BRAF V600E: An In Vitro Study. [Abstract]2019 Feb 5;12:235-245. PMID: 30847387 -
Br J Cancer
Drug response profiles in patient-derived cancer cells across histological subtypes of ovarian cancer: real-time therapy tailoring for a patient with low-grade serous carcinoma. [Abstract]2023 Feb;128(4):678-690. PMID: 36476658 -
Cell Rep
2026 Jun 18;45(7):117576. PMID: 42313565 -
Eur J Nucl Med Mol Imaging
Preclinical and first-in-human evaluation of 18F-labeled D-peptide antagonist for PD-L1 status imaging with PET. [Abstract]2022 Nov;49(13):4312-4324. PMID: 35831714 -
Cell Syst
Receptor-Driven ERK Pulses Reconfigure MAPK Signaling and Enable Persistence of Drug-Adapted BRAF-Mutant Melanoma Cells. [Abstract]2020 Nov 18;11(5):478-494.e9. PMID: 33113355 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
J Invest Dermatol
Combined Cyclin-Dependent Kinase Inhibition Overcomes MAPK/Extracellular Signal-Regulated Kinase Kinase Inhibitor Resistance in Plexiform Neurofibroma of Neurofibromatosis Type I. [Abstract]2022 Mar;142(3 Pt A):613-623.e7. PMID: 34534577 -
Sci Signal
2018 Oct 30;11(554):eaar6795. PMID: 30377225 -
Mol Cancer Ther
Selumetinib Attenuates Skeletal Muscle Wasting in Murine Cachexia Model through ERK Inhibition and AKT Activation. [Abstract]2017 Feb;16(2):334-343. PMID: 27599525
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.
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Mol Cancer Ther
Inhibition of Wild-Type p53-Expressing AML by the Novel Small Molecule HDM2 Inhibitor CGM097. [Abstract]2015 Oct;14(10):2249-59. PMID: 26206331 -
Mol Syst Biol
Systematic analysis of BRAF(V600E) melanomas reveals a role for JNK/c-Jun pathway in adaptive resistance to drug-induced apoptosis. [Abstract]2015 Mar 26;11(3):797. PMID: 25814555 -
Biochem Pharmacol
Direct reprogramming of human fibroblasts into hair-inducing dermal papilla cell-like cells by a single small molecule. [Abstract]2025 Jan 9:116744. PMID: 39798934 -
Drug Des Devel Ther
Attenuation of everolimus-induced cytotoxicity by a protective autophagic pathway involving ERK activation in renal cell carcinoma cells. [Abstract]2018 Apr 19:12:911-920. PMID: 29719377
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.
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Oncogenesis
A novel small-molecule inhibitor of trefoil factor 3 (TFF3) potentiates MEK1/2 inhibition in lung adenocarcinoma. [Abstract]2019 Nov 4;8(11):65. PMID: 31685806 -
Hepatol Commun
Murine Liver Organoids as a Genetically Flexible System to Study Liver Cancer In Vivo and In Vitro. [Abstract]2019 Feb 5;3(3):423-436. PMID: 30859153 -
Cell Rep Methods
Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. [Abstract]2026 Jun 15;6(6):101339. PMID: 42134319 -
Biomolecules
Allosteric Kinase Inhibitors Reshape MEK1 Kinase Activity Conformations in Cells and In Silico. [Abstract]2021 Mar 30;11(4):518. PMID: 33808483 -
Glia
Inhibition of MAPK/ERK pathway promotes oligodendrocytes generation and recovery of demyelinating diseases. [Abstract]2019 Jul;67(7):1320-1332. PMID: 30815939 -
J Pathol
Novel prognostication biomarker adipophilin reveals a metabolic shift in uveal melanoma and new therapeutic opportunities. [Abstract]2023 Jun;260(2):203-221. PMID: 36825655 -
Cancer Sci
NOTCH3 promotes docetaxel resistance of prostate cancer cells through regulating TUBB3 and MAPK signaling pathway. [Abstract]2024 Feb;115(2):412-426. PMID: 38115797 -
Comput Struct Biotechnol J
Unveiling the Kinomes of Leishmania infantum and L. braziliensis Empowers the Discovery of New Kinase Targets and Antileishmanial Compounds. [Abstract]2019 Feb 8:17:352-361. PMID: 30949306 -
J Cell Mol Med
Combined tazemetostat and MAPKi enhances differentiation of papillary thyroid cancer cells harbouring BRAFV600E by synergistically decreasing global trimethylation of H3K27. [Abstract]2020 Mar;24(6):3336-3345. PMID: 31970877 -
Oncol Res
Development of a cell adhesion-based prognostic model for multiple myeloma: Insights into chemotherapy response and potential reversal of adhesion effects. [Abstract]2024 Mar 20;32(4):753-768. PMID: 38560563 -
Mol Oncol
Optimized low-dose combinatorial drug treatment boosts selectivity and efficacy of colorectal carcinoma treatment. [Abstract]2020 Nov;14(11):2894-2919. PMID: 33021054 -
Gynecol Oncol
A first-in-class CDK4 inhibitor demonstrates in vitro, ex-vivo and in vivo efficacy against ovarian cancer. [Abstract]2020 Dec;159(3):827-838. PMID: 32958271 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
J Virol
The ASFV CD2v protein inhibits apoptosis by inducing proteasomal degradation of BimEL via activation of the TPL2-MEK-ERK signaling pathway. [Abstract]2026 Mar 24;100(3):e0195225. PMID: 41631827 -
Epigenetics
DNMT1 expression partially dictates 5-Azacytidine sensitivity and correlates with RAS/MEK/ERK activity in gastric cancer cells. [Abstract]2023 Dec;18(1):2254976. PMID: 37691391 -
Exp Cell Res
The aberrantly activated AURKB supports and complements the function of AURKA in CALR mutated cells through regulating the cell growth and differentiation. [Abstract]2025 Jan 15;444(2):114377. PMID: 39706286 -
Mol Carcinog
Four and a half LIM domains 2 (FHL2) attenuates tumorigenesis of gastrointestinal stromal tumors (GISTs) by negatively regulating KIT signaling. [Abstract]2024 Jul;63(7):1334-1348. PMID: 38629424 -
Mol Carcinog
Loss of PTPRS elicits potent metastatic capability and resistance to temozolomide in glioblastoma. [Abstract]2024 Jul;63(7):1235-1247. PMID: 38517048 -
Mol Pharmacol
Functional RNAi Screens Define Distinct Protein Kinase Vulnerabilities in EGFR-Dependent HNSCC Cell Lines. [Abstract]2019 Dec;96(6):862-870. PMID: 31554698 -
PLoS One
PIK3CA missense mutations promote glioblastoma pathogenesis, but do not enhance targeted PI3K inhibition. [Abstract]2018 Jul 5;13(7):e0200014. PMID: 29975751
Selumetinib sulfate purchased from MedChemExpress. Usage Cited in: PLoS One. 2018 Jul 5;13(7):e0200014. [Abstract]
Representative immunoblots of control and NHARAS treated with Selumetinib for 24 h.
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Eur J Haematol
Interferon gamma regulates a complex pro-survival signal network in chronic lymphocytic leukemia. [Abstract]2023 Apr;110(4):435-443. PMID: 36576398 -
OMICS
Integrative Genomic and Immune Profiling to Identify and Characterize High-Risk Subgroups in Acute Myeloid Leukemia: Development of a 20-Gene Predictive Signature and Its Clinical Implications. [Abstract]2025 Sep;29(9):458-472. PMID: 40844427 -
Biochem Genet
GABRP Promotes the Metastasis of Pancreatic Cancer by Activation of the MEK/ERK Signaling Pathway. [Abstract]2024 Feb;62(1):242-253. PMID: 37326897 -
Lipids
Activated PPARβ/δ Protects Pancreatic β Cells in Type 2 Diabetic Goto-Kakizaki Rats from Lipoapoptosis via GPR40. [Abstract]2019 Oct;54(10):603-616. PMID: 31364177 -
Chemotherapy
The Synergistic Inhibitory Effect of Combining MK-2206 and AZD 6244 in MARIMO Cells Harboring a Calreticulin Gene Mutation. [Abstract]2021;66(5-6):169-178. PMID: 34666331 -
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bioRxiv
Acquired resistance to the PRMT5 inhibitor confers collateral sensitivity to MEK inhibition in MTAP-null non-small cell lung cancer. [Abstract]2026 Apr 21:2026.04.16.719008. PMID: 42079286 -
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bioRxiv
A Human Neuronal Co-Culture System Reveals Early Tumor-Neuron Communication and Targetable Pathways in Glioblastoma. [Abstract]2025 Sep 16:2025.09.10.675396. PMID: 41000938 -
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Res Sq
Novel mixed cancer-cell models designed to capture inter-patient tumor heterogeneity for accurate evaluation of drug combinations. [Abstract]2025 May 16:rs.3.rs-6590535. PMID: 40470249 -
bioRxiv
Capacity for compensatory cyclin D2 response confers trametinib resistance in canine mucosal melanoma. [Abstract]2025 Apr 26:2025.04.24.650512. PMID: 40568110 -
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bioRxiv
PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]2024 Nov 6:2024.11.04.621884. PMID: 39574568 -
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Front Med
Acitretin Promotes the Differentiation of Myeloid-Derived Suppressor Cells in the Treatment of Psoriasis. [Abstract]2021 Mar 23;8:625130. PMID: 33834031 -
Oncotarget
2020 Nov 3;11(44):3921-3932. PMID: 33216841 -
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ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077 -
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Oncotarget
MEK inhibition is a promising therapeutic strategy for MLL-rearranged infant acute lymphoblastic leukemia patients carrying RAS mutations. [Abstract]2017 Feb 28;8(9):14835-14846. PMID: 27588400
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.
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (17.99 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (276 KB)
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SDS (702 KB)
- English - EN (702 KB)
- Français - FR (702 KB)
- Deutsch - DE (702 KB)
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- Italian - IT (702 KB)
- Korean - KR (702 KB)
- Portuguese - PT (702 KB)
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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]
[4]. Sara H Osum, et al. Selumetinib normalizes Ras/MAPK signaling in clinically relevant neurofibromatosis type 1 minipig tissues in vivo. Neurooncol Adv. 2021 Feb 10;3(1):vdab020. [Content Brief]
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.
| 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 |