2489241-16-7
Chemical Structure
CST651
Synonym(s): PROTAC CDK4/6 degrader 34
- CAS No.: 2489241-16-7
- Formula:C56H72FN11O9S
- Molecular Weight:1094.30
IUPAC Name: (2S,4R)-N-(2-(2-(2-(2-(4-(6-((6-acetyl-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazin-1-yl)ethoxy)ethoxy)ethoxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide
InChIKey: WYPMPGWHIPETEB-VZUPZQALSA-N
SMILES: O=C1C(C(C)=O)=C(C2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(N5CCN(CCOCCOCCOC6=CC(C7=C(C)N=CS7)=CC=C6CNC([C@H]8N(C([C@H](C(C)(C)C)NC(C9(CC9)F)=O)=O)C[C@H](O)C8)=O)CC5)C=N4)C
Biological Activity: CST651 (PROTAC CDK4/6 degrader 34) is a selective cyclin-dependent kinase CDK4/6 PROTAC degrader with DC50 values of 20 nM and 5.1 nM, respectively. CST651 recruits the VHL E3 ubiquitin ligase to mediate the ubiquitination and proteasomal degradation of CDK4/6. CST651 inhibits cancer cell proliferation and migration. CST651 can be used in research related to breast cancer, multiple myeloma, acute myeloid leukemia, and acute lymphoblastic leukemia[1][2].
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CST651 | CST651 (PROTAC CDK4/6 degrader 34) is a selective cyclin-dependent kinase CDK4/6 PROTAC degrader with DC50 values of 20 nM and 5.1 nM, respectively. CST651 recruits the VHL E3 ubiquitin ligase to mediate the ubiquitination and proteasomal degradation of CDK4/6. CST651 inhibits cancer cell proliferation and migration. CST651 can be used in research related to breast cancer, multiple myeloma, acute myeloid leukemia, and acute lymphoblastic leukemia. | |||||||||||||||||||||
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- [1]. Kossakowski K, et al. FDA-approved kinase inhibitors in PROTAC design, development and synthesis. Journal of enzyme inhibition and medicinal chemistry. 2025 Dec;40(1):2542357. [Content Brief]
- [2]. Steinebach C, et al. Systematic exploration of different E3 ubiquitin ligases: an approach towards potent and selective CDK6 degraders. Chemical science. 2020 Apr 07;11(13):3474-3486. [Content Brief]
Keywords
