2488892-09-5
Chemical Structure
TMX-2172
- CAS No.: 2488892-09-5
- Formula:C41H45BrFN9O11S
- Molecular Weight:970.82
InChIKey: ZOJWMCDSTRTTOW-UHFFFAOYSA-N
SMILES: O=C(C1=C(NC2=NC(NC3=CC=C(S(=O)(NCCOCCOCCOCCOCCNC4=CC=CC(C(N5C6C(NC(CC6)=O)=O)=O)=C4C5=O)=O)C=C3C)=NC=C2Br)C=CC=C1F)N
Biological Activity: TMX-2172 is a selective bivalent cereblon-recruiting PROTAC-based dual CDK2 and CDK5 degrader with IC50 values of 6.5 nM and 6.8 nM, respectively. TMX-2172 shows selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9). TMX-2172 inhibits CDK2/CDK5 enzymatic activity, induces their proteasomal degradation, reduces ASCL1 protein levels and half-life, induces cancer cell death, and exerts antiproliferative effects. TMX-2172 can be used for the research of ovarian cancer and small cell lung cancer[1][2][3][4][5].
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TMX-2172 | 99.38% | TMX-2172 is a selective bivalent cereblon-recruiting PROTAC-based dual CDK2 and CDK5 degrader with IC50 values of 6.5 nM and 6.8 nM, respectively. TMX-2172 shows selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9). TMX-2172 inhibits CDK2/CDK5 enzymatic activity, induces their proteasomal degradation, reduces ASCL1 protein levels and half-life, induces cancer cell death, and exerts antiproliferative effects. TMX-2172 can be used for the research of ovarian cancer and small cell lung cancer. | ||||||||||||||||||||
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- [1]. Giarolla J, et al. Targeting cyclin-dependent kinase 2 (CDK2) interactions with cyclins and Speedy 1 (Spy1) for cancer and male contraception. Future Med Chem. 2025;17(5):607-627. [Content Brief]
- [2]. Teng M, et al. Exploring Ligand-Directed N-Acyl-N-alkylsulfonamide-Based Acylation Chemistry for Potential Targeted Degrader Development. ACS Med Chem Lett. 2021 Jul 21;12(8):1302-1307. [Content Brief]
- [3]. Koduri V, et al. Targeting oncoproteins with a positive selection assay for protein degraders. Sci Adv. 2021 Feb 5;7(6):eabd6263. [Content Brief]
- [4]. Zeng Y, et al. Inhibitors and PROTACs of CDK2: challenges and opportunities. Expert Opin Drug Discov. 2024;19(9):1125-1148. [Content Brief]
- [5]. Teng M, et al. Development of CDK2 and CDK5 Dual Degrader TMX-2172. Angew Chem Int Ed Engl. 2020;59(33):13865-13870. [Content Brief]
Keywords
