For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>ML 264 is a potent Krüppel-like factor 5 (KLF5) inhibitor. ML264 inhibits the MAPK pathway by reducing EGR1 and KLF5 levels. ML 264 decreases proliferation of colorectal cancer cell lines, and inhibits the growth of xenografts in a mouse model of primary tumor development. [1]<br>target : KLF5<br>IC50: ML264 is highly active (IC50 = 29 nM is a cell-based assay for proliferation of DLD-1 cells, IC50 = 81 nM in a cell-based luciferase assay) [2].<br>in vitro[1]: ML264, potently inhibits proliferation of colorectal cancer cells in vitro through modifications of the cell-cycle profile. In an established xenograft mouse model of colon cancer, we demonstrate that ML264 efficiently inhibits growth of the tumor within 5 days of treatment. For in vitro experiments, ML264 was dissolved in DMSO<br>In vivo[1]: ML264 was dissolved in the vehicle solution: 80% dH2O, 10% DMSO, and 10% Tween 80. Our in vivo DMPK studies demonstrated that ML264 has 2-hour half-life in mice. Interestingly, ML264 also displays 47% oral bioavailability in mice, a very promising feature for compound development with potential therapeutic advantages.</p>
| Catalog Number | I001958 |
| CAS Number | 1550008-55-3 |
| Synonyms | (2E)-3-(3-chlorophenyl)-N-[2-[methyl(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)amino]-2-oxoethyl]-2-propenamide |
| Molecular Formula | C17H21ClN2O4S |
| Purity | ≥95% |
| Target | KLF |
| Solubility | Soluble in DMSO, not in water |
| Storage | Store at -20°C |
| InChI | InChI=1S/C17H21ClN2O4S/c1-20(15-7-9-25(23,24)10-8-15)17(22)12-19-16(21)6-5-13-3-2-4-14(18)11-13/h2-6,11,15H,7-10,12H2,1H3,(H,19,21)/b6-5+ |
| InChIKey | AJCDZIDKYKCOMZ-AATRIKPKSA-N |
| SMILES | ClC1=CC=CC(/C=C/C(NCC(N(C)C2CCS(CC2)(=O)=O)=O)=O)=C1 |
| Reference | </br>1:ML264, A Novel Small-Molecule Compound That Potently Inhibits Growth of Colorectal Cancer. Ruiz de Sabando A, Wang C, He Y, García-Barros M, Kim J, Shroyer KR, Bannister TD, Yang VW, Bialkowska AB.Mol Cancer Ther. 2016 Jan;15(1):72-83. doi: 10.1158/1535-7163.MCT-15-0600. Epub 2015 Nov 30. PMID: 26621868 Free PMC Article</br>2:ML264: An Antitumor Agent that Potently and Selectively Inhibits Krüppel-like Factor Five (KLF5) Expression: A Probe for Studying Colon Cancer Development and Progression. Bialkowska A, Crisp M, Madoux F, Spicer T, Knapinska A, Mercer B, Bannister TD, He Y, Chowdhury S, Cameron M, Yang VW, Hodder P.Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.2011 Oct 31 [updated 2013 Mar 7]. PMID: 23762940 Free Books & Documents |
