Chemical Structure : TMX-2172
CAS No.:
2488892-09-5
TMX-2172
(TMX2172)
Catalog No.: PC-21526Not For Human Use, Lab Use Only.
TMX-2172 is a potent, selective CDK2 and CDK5 dual PROTAC degrader with IC50 of 6.5 nM and 6.8 nM for CDK2/cyclin A and CDK5/p25, respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TMX-2172 is a potent, selective CDK2 and CDK5 dual PROTAC degrader with IC50 of 6.5 nM and 6.8 nM for CDK2/cyclin A and CDK5/p25, respectively.
TMX-2172 shows high degradation selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9).
TMX-2172 exhibits antiproliferative activity against OVCAR8 with IC50 of 33.1 nM, an ovarian cancer cell line that overexpresses CCNE1 (a well-established activator of CDK2).
TMX-2172 exhibits an IC50 of 46.9 nM in cellular CRBN engagement assays.
TMX-2172 induced CDK2 degradation at a concentration of 250 nM in Jurkat cells with no effect against other cell cycle CDKs.
Physicochemical Properties
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M.Wt
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970.83
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Formula
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C41H45BrFN9O11S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-((5-bromo-2-((4-(N-(14-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12-tetraoxatetradecyl)sulfamoyl)-2-methylphenyl)amino)pyrimidin-4-yl)amino)-6-fluorobenzamide
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References
1. Teng M, et al. Angew Chem Int Ed Engl. 2020 Aug 10;59(33):13865-13870.
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