3064485-73-7
Chemical Structure
CIRc-014
- CAS No.: 3064485-73-7
- Formula:C45H62ClF6N7O7
- Molecular Weight:962.46
InChIKey: PTZDPNNZZODMBT-FIIVPKDJSA-N
SMILES: O=C([C@H]1N(C(C2(C(F)(F)F)CC(F)(F)C2)=O)C[C@H](F)C1)N[C@@H](C3CC3)C(N([C@@H]4C(N[C@@H](CC(C)C)C(N(C)[C@@H](CC5=CC(Cl)=CN=C5OC6CC6)C(N(C)CCCCCCC4)=O)=O)=O)C)=O
Biological Activity: CIRc-014 is an orally active Cyclin A/B inhibitor with a Cyclin A IC50 of 0.05 μM, Cyclin A Kd of 2.7 nM, Cyclin B IC50 of less than 0.02 μM and Cyclin B Kd of 1.0 nM. CIRc-014 activates the spindle assembly checkpoint and promotes the formation of a complex between Cyclin B and CDK2 by blocking the RxL interaction of Cyclin A/B. CIRc-014 can induce replication stress, DNA damage, mitotic arrest and apoptosis in tumor cells. CIRc-014 showed tumor growth inhibition and regression in NCI-H69 and NCI-H446 small cell lung cancer xenograft models. CIRc-014 can be used for the research of small-cell lung cancer[1][2].
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CIRc-014 | CIRc-014 is an orally active Cyclin A/B inhibitor with a Cyclin A IC50 of 0.05 μM, Cyclin A Kd of 2.7 nM, Cyclin B IC50 of less than 0.02 μM and Cyclin B Kd of 1.0 nM. CIRc-014 activates the spindle assembly checkpoint and promotes the formation of a complex between Cyclin B and CDK2 by blocking the RxL interaction of Cyclin A/B. CIRc-014 can induce replication stress, DNA damage, mitotic arrest and apoptosis in tumor cells. CIRc-014 showed tumor growth inhibition and regression in NCI-H69 and NCI-H446 small cell lung cancer xenograft models. CIRc-014 can be used for the research of small-cell lung cancer. | |||||||||||||||||||||
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References
- [1]. Shapiro JA, et al. Orally Bioavailable Cyclin A/B RxL Inhibitors: Optimization of a Novel Class of Macrocyclic Peptides That Target E2F-High and G1-S-Checkpoint-Compromised Cancers. J Med Chem. 2026;69(5):5441-5460. [Content Brief]
- [2]. Singh S, et al. Targeting G1-S-checkpoint-compromised cancers with cyclin A/B RxL inhibitors. Nature. 2025;646(8085):734-745. [Content Brief]
