Selumetinib
Code | Size | Price |
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TAR-T6218-1mL | 1 mL * 10 mM (in DMSO) | £107.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
TAR-T6218-25mg | 25mg | £108.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
TAR-T6218-50mg | 50mg | £121.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
TAR-T6218-100mg | 100mg | £136.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
TAR-T6218-200mg | 200mg | £172.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
Images
Documents
Further Information
Bioactivity:
Selumetinib (AZD6244) is an effective, specific inhibitor of MEK1 and ERK1/2 phosphorylation (IC50: 14/10 nM).
CAS:
606143-52-6
Formula:
C17H15BrClFN4O3
Molecular Weight:
457.68
Pathway:
Apoptosis; MAPK
Purity:
0.99
SMILES:
Cn1cnc2c(F)c(Nc3ccc(Br)cc3Cl)c(cc12)C(=O)NOCCO
Target:
Apoptosis; ERK; MEK
References
Yang N, Fan Z, Sun S, et al.Discovery of highly potent and selective KRASG12C degraders by VHL-recruiting PROTACs for the treatment of tumors with KRASG12C-Mutation.European Journal of Medicinal Chemistry.2023: 115857.
Meng Y, Lv T, Zhang J, et al.Temporospatial inhibition of Erk signaling is required for lymphatic valve formation.Signal Transduction and Targeted Therapy.2023, 8(1): 342.
Huynh H, et al. AZD6244 and doxorubicin induce growth suppression and apoptosis in mouse models of hepatocellular carcinoma. Mol Cancer Ther. 2007 Sep;6(9):2468-76.
Boos S L, Loevenich L P, Vosberg S, et al Disease Modeling on Tumor Organoids Implicates AURKA as a Therapeutic Target in Liver Metastatic Colorectal Cancer. Cellular and Molecular Gastroenterology and Hepatology. 2021
Zhang Q, Le K, Xu M, et al. Combined MEK inhibition and tumor-associated macrophages depletion suppresses tumor growth in a triple-negative breast cancer mouse model[J]. International Immunopharmacology. 2019, 76: 105864.
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 Mar 1;13(5):1576-83.
Zhang Q, Le K, Xu M, et al. Combined MEK inhibition and tumor-associated macrophages depletion suppresses tumor growth in a triple-negative breast cancer mouse model. International Immunopharmacology. 2019, 76: 105864.
Zhang G M, Huang S S, Ye L X, et al. Reciprocal positive regulation between BRD4 and YAP in GNAQ-mutant uveal melanoma cells confers sensitivity to BET inhibitors. Pharmacological Research. 2022: 106464.
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.
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.