TMX-2172 | CDK2/5 PROTAC | Probechem Biochemicals

Chemical Structure : TMX-2172

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TMX-2172 (TMX2172)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	970.83
分子式	C41H45BrFN9O11S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Teng M, et al. Angew Chem Int Ed Engl. 2020 Aug 10;59(33):13865-13870.

TMX-2172 (TMX2172)

生物&药学活性

物理化学性质&存储条件

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TMX-2172 (TMX2172)

生物&药学活性

物理化学性质&存储条件

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