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Selumetinib (AZD6244)

(CAS No:606143-52-6)
Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM in cell-free assays, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3.
CAS No:606143-52-6
Molecular Weight(MW):457.68
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 606143-52-6
Molecular formula(MF) C17H15BrClFN4O3
Molecular Weight(MW): 457.68
Alias 5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide
Solubility
In vitro DMSO 91 mg/mL warmed (198.82 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL
Biological Activity
Description Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM in cell-free assays, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3.
Features First MEK inhibitor being tested in Phase II clinical trials.
Targets
MEK1 [1]
(Cell-free assay)
14 nM
In vitro

AZD6244 is not competitive with ATP and inactivates the ERK1/2 phosphorylation with IC50 concentrations below 40 nM. AZD6244 also inhibits the growth of primary HCC cells through inhibition of ERK1/2 and p90RSK phosphorylation, accompanied with elevation of the cleavage of caspase-3 and caspase-7, and cleaved poly(ADP)ribose polymerase. AZD6244 has little effects on the p38, c-Jun-NH2-kinase, phosphatidylinositol 3-kinase, and MEK5/ERK5 pathways. [1] AZD6244 is sensitive to Raf mutations in breast cancer cell lines and Ras mutations in NSCLC cell lines. [2]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CHP-212 cell Growth inhibition assay Inhibition of human CHP-212 cell growth in a cell viability assay, IC50=3.15 nM. SANGER
human H9 cell Growth inhibition assay Inhibition of human H9 cell growth in a cell viability assay, IC50=22.88 nM. SANGER
human HL-60 cell Growth inhibition assay Inhibition of human HL-60 cell growth in a cell viability assay, IC50=24.59 nM. SANGER
human A375 cells Proliferation assay 72 h Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by Cell titer-glo assay, IC50=31 nM. 23474388
human NOMO-1 cell Growth inhibition assay Inhibition of human NOMO-1 cell growth in a cell viability assay, IC50=31.97 nM. SANGER
human DU-4475 cell Growth inhibition assay Inhibition of human DU-4475 cell growth in a cell viability assay, IC50=33.67 nM. SANGER
human M14 cell Growth inhibition assay Inhibition of human M14 cell growth in a cell viability assay, IC50=36.89 nM. SANGER
human HT-144 cell Growth inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay, IC50=89.05 nM. SANGER
human SK-N-AS cell Growth inhibition assay Inhibition of human SK-N-AS cell growth in a cell viability assay, IC50=92.83 nM. SANGER
human LB2518-MEL cell Growth inhibition assay Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=93.82 nM. SANGER
human C32 cell Growth inhibition assay Inhibition of human C32 cell growth in a cell viability assay, IC50=98.23 nM. SANGER
human BHT-101 cell Growth inhibition assay Inhibition of human BHT-101 cell growth in a cell viability assay, IC50=106.93 nM. SANGER
human KY821 cell Growth inhibition assay Inhibition of human KY821 cell growth in a cell viability assay, IC50=107.18 nM. SANGER
human CP50-MEL-B cell Growth inhibition assay Inhibition of human CP50-MEL-B cell growth in a cell viability assay, IC50=127.94 nM. SANGER
human MEL-HO cell Growth inhibition assay Inhibition of human MEL-HO cell growth in a cell viability assay, IC50=138.84 nM. SANGER
human MIAPaCa2 cells Proliferation assay Antiproliferative activity against human MIAPaCa2 cells, IC50=142 nM. 23474388
human EoL-1-cell cell Growth inhibition assay Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=144.76 nM. SANGER
human DOK cell Growth inhibition assay Inhibition of human DOK cell growth in a cell viability assay, IC50=147.08 nM. SANGER
human SH-4 cell Growth inhibition assay Inhibition of human SH-4 cell growth in a cell viability assay, IC50=166.48 nM. SANGER
human BPH-1 cell Growth inhibition assay Inhibition of human BPH-1 cell growth in a cell viability assay, IC50=182.31 nM. SANGER
human HuP-T4 cell Growth inhibition assay Inhibition of human HuP-T4 cell growth in a cell viability assay, IC50=195.32 nM. SANGER
human KU812 cell Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50=211.68 nM. SANGER
human A549 cell Growth inhibition assay Inhibition of human A549 cell growth in a cell viability assay, IC50=214.13 nM. SANGER
human HTC-C3 cell Growth inhibition assay Inhibition of human HTC-C3 cell growth in a cell viability assay, IC50=214.61 nM. SANGER
human A101D cell Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50=240.33 nM. SANGER
human ONS-76 cell Growth inhibition assay Inhibition of human ONS-76 cell growth in a cell viability assay, IC50=244.53 nM. SANGER
human RKO cell Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50=248.38 nM. SANGER
human WM-115 cell Growth inhibition assay Inhibition of human WM-115 cell growth in a cell viability assay, IC50=267.54 nM. SANGER
human HCC2998 cell Growth inhibition assay Inhibition of human HCC2998 cell growth in a cell viability assay, IC50=269.07 nM. SANGER
human C2BBe1 cell Growth inhibition assay Inhibition of human C2BBe1 cell growth in a cell viability assay, IC50=272.59 nM. SANGER
human RVH-421 cell Growth inhibition assay Inhibition of human RVH-421 cell growth in a cell viability assay, IC50=279.39 nM. SANGER
human H-EMC-SS cell Growth inhibition assay Inhibition of human H-EMC-SS cell growth in a cell viability assay, IC50=290.99 nM. SANGER
human ML-2 cell Growth inhibition assay Inhibition of human ML-2 cell growth in a cell viability assay, IC50=293.63 nM. SANGER
human SW620 cell Growth inhibition assay Inhibition of human SW620 cell growth in a cell viability assay, IC50=302.2 nM. SANGER
human UACC-257 cell Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=321.84 nM. SANGER
human AsPC-1 cell Growth inhibition assay Inhibition of human AsPC-1 cell growth in a cell viability assay, IC50=324.39 nM. SANGER
human CAL-39 cell Growth inhibition assay Inhibition of human CAL-39 cell growth in a cell viability assay, IC50=332.26 nM. SANGER
human COLO-679 cell Growth inhibition assay Inhibition of human COLO-679 cell growth in a cell viability assay, IC50=341.19 nM. SANGER
human NCI-H747 cell Growth inhibition assay Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=350.98 nM. SANGER
human NCI-H1437 cell Growth inhibition assay Inhibition of human NCI-H1437 cell growth in a cell viability assay, IC50=352.85 nM. SANGER
human PSN1 cell Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50=366.09 nM. SANGER
human NKM-1 cell Growth inhibition assay Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=385.8 nM SANGER
human MZ2-MEL cell Growth inhibition assay Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50=394.37 nM. SANGER
human SK-MEL-2 cell Growth inhibition assay Inhibition of human SK-MEL-2 cell growth in a cell viability assay, IC50=405.06 nM. SANGER
human LAMA-84 cell Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=456.22 nM. SANGER
human U-266 cell Growth inhibition assay Inhibition of human U-266 cell growth in a cell viability assay, IC50=487.74 nM. SANGER
human RCM-1 cell Growth inhibition assay Inhibition of human RCM-1 cell growth in a cell viability assay, IC50=493.85 nM. SANGER

... Click to View More Cell Line Experimental Data
In vivo AZD6244 significantly inhibits phosphorylation of ERK1/2 in 2-1318, 5-1318, 26-1004 and 4-1318 xenografts and induces apoptosis in primary 2-1318 cells by activating the caspase pathway. [1] AZD6244 could inhibit the tumor growth in HT-29 xenograft, which is a colorectal tumor model carrying a B-Raf mutation, at a dose of 100 mg/kg and the tumor growth inhibition of AZD6244 is better than it of Gemcitabine. [3] Otherwise AZD6244 could inhibit HCC xenografts tumor growth, which associated with increased apoptosis and down-regulation of cell cycle regulators, including cyclin D1, Cdc-2, CDK2 and 4, cyclin B1, and c-Myc. [4]
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