Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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S125580-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $44.90 | |
S125580-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $76.90 | |
S125580-500mg | 500mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $325.90 | |
S125580-1g | 1g | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $508.90 |
Potent, selective MEK1/2 inhibitor
Synonyms | 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy -ethoxy)-amide | AZD6244 (Selumetinib) | BCPP000367 | EX-A020 | HMS3244G03 | 5-[(4-BROMO-2-CHLOROPHENYL)AMINO]-4-FLUORO-N-(2-HYDROXYETHOXY)-1-METHYL-1H-BENZI |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | Selumetinib is a non-ATP competitive inhibitor of MEK-1 (IC50 = 14 nM). This compound inactivates the phosphorylation of ERK1/2 (IC50 < 40 nM). Selumetinib has little effect on p38, c-Jun-NH2-kinase, or the MEK/ERK5 pathways.Potent, selective, non-ATP com |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | ALLOSTERIC MODULATOR, INHIBITOR |
Mechanism of action | Dual specificity mitogen-activated protein kinase kinase 2 inhibitor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3. |
ALogP | 3.6 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide |
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INCHI | InChI=1S/C17H15BrClFN4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26) |
InChi Key | CYOHGALHFOKKQC-UHFFFAOYSA-N |
Canonical SMILES | CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO |
Isomeric SMILES | CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO |
PubChem CID | 10127622 |
Molecular Weight | 457.69 |
Wikipedia | Selumetinib |
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DiscoveRx TREEspot | AZD-6244/ARRY-886| |
PubChem CID | 10127622 |
ChEMBL Ligand | CHEMBL1614701 |
RCSB PDB Ligand | 3EW |
Reactome Reaction | R-HSA-9657606 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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E1529129 | Certificate of Analysis | Oct 18, 2024 | S125580 |
C2409113 | Certificate of Analysis | Feb 28, 2024 | S125580 |
C2409114 | Certificate of Analysis | Feb 28, 2024 | S125580 |
C2409116 | Certificate of Analysis | Feb 28, 2024 | S125580 |
H1815140 | Certificate of Analysis | Feb 26, 2024 | S125580 |
H1815139 | Certificate of Analysis | Feb 26, 2024 | S125580 |
J2326187 | Certificate of Analysis | Oct 21, 2023 | S125580 |
J2326188 | Certificate of Analysis | Oct 21, 2023 | S125580 |
J2326189 | Certificate of Analysis | Oct 21, 2023 | S125580 |
J2326190 | Certificate of Analysis | Oct 21, 2023 | S125580 |
Solubility | Soluble in DMSO (92 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C). |
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Pictogram(s) | GHS08, GHS09, GHS05, GHS07 |
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Signal | Danger |
Hazard Statements | H373:Causes damage to organs through prolonged or repeated exposure H411:Toxic to aquatic life with long lasting effects H318:Causes serious eye damage H317:May cause an allergic skin reaction H361:Suspected of damaging fertility or the unborn child |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P260:Do not breathe dust/fume/gas/mist/vapors/spray. P272:Contaminated work clothing should not be allowed out of the workplace. P333+P313:IF SKIN irritation or rash occurs: Get medical advice/attention. P362+P364:Take off contaminated clothing and wash it before reuse. P391:Collect spillage. P203:Obtain, read and follow all safety instructions before use. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P305+P354+P338:IF IN EYES: Immediately rinse with water for several minutes. Remove contact lenses if present and easy to do. Continue rinsing. P318:if exposed or concerned, get medical advice. P317:Get emergency medical help. P319:Get medical help if you feel unwell. |
1. Davies H, Bignell GR, Cox C, Stephens P, Edkins S, Clegg S, Teague J, Woffendin H, Garnett MJ, Bottomley W et al.. (2002) Mutations of the BRAF gene in human cancer.. Nature, 417 (6892): (949-54). [PMID:12068308] [10.1021/op500134e] |
2. Huynh H, Soo KC, Chow PK, Tran E. (2007) Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma.. Mol Cancer Ther, 6 (1): (138-46). [PMID:17237274] [10.1021/op500134e] |
3. Troiani T, Vecchione L, Martinelli E, Capasso A, Costantino S, Ciuffreda LP, Morgillo F, Vitagliano D, D'Aiuto E, De Palma R et al.. (2012) Intrinsic resistance to selumetinib, a selective inhibitor of MEK1/2, by cAMP-dependent protein kinase A activation in human lung and colorectal cancer cells.. Br J Cancer, 106 (10): (1648-59). [PMID:22569000] [10.1021/op500134e] |
4. Dombi E, Baldwin A, Marcus LJ, Fisher MJ, Weiss B, Kim A, Whitcomb P, Martin S, Aschbacher-Smith LE, Rizvi TA et al.. (2016) Activity of Selumetinib in Neurofibromatosis Type 1-Related Plexiform Neurofibromas.. N Engl J Med, 375 (26): (2550-2560). [PMID:28029918] [10.1021/op500134e] |