3064485-16-8
Chemical Structure
CID-078
- CAS 番号: 3064485-16-8
- Formula:C47H63ClF6N8O6
- Molecular Weight:985.50
InChIKey: LSUMJDILBCWSIG-ZFLRSTEBSA-N
SMILES: ClC1=CC=C(C2=CN(C)N=C2)C(C[C@H](N(C([C@H](CC(C)C)NC3=O)=O)C)C(N(CCCCCCC[C@@H]3N(C([C@H](C4CC4)NC([C@@H]5C[C@@H](F)CN5C(C6(C(F)(F)F)CC(F)(F)C6)=O)=O)=O)C)C)=O)=C1
Biological Activity: CID-078 is an orally active macrocyclic cyclin A and cyclin B inhibitor. CID-078 binds cyclin hydrophobic patches, disrupting interactions of cyclin A-Cdk2 with E2F1 and cyclin B-Cdk1 with Myt1, and selectively targets RxL binding motifs to block complex-substrate interactions. CID-078 induces DNA damage, G2/M cell cycle arrest, apoptosis, mitotic catastrophe, spindle assembly checkpoint activation, and neomorphic cyclin B-CDK2 complex formation, driving synthetic lethality in E2F-driven cancer cells. CID-078 can be used for the research of small cell lung cancer, non-small cell lung cancer, triple negative breast cancer, advanced solid tumors, luminal HR+/HER2- breast cancer, RB1-altered solid tumors, and neuroblastoma[1][2][3][4].
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CID-078 | CID-078 is an orally active macrocyclic cyclin A and cyclin B inhibitor. CID-078 binds cyclin hydrophobic patches, disrupting interactions of cyclin A-Cdk2 with E2F1 and cyclin B-Cdk1 with Myt1, and selectively targets RxL binding motifs to block complex-substrate interactions. CID-078 induces DNA damage, G2/M cell cycle arrest, apoptosis, mitotic catastrophe, spindle assembly checkpoint activation, and neomorphic cyclin B-CDK2 complex formation, driving synthetic lethality in E2F-driven cancer cells. CID-078 can be used for the research of small cell lung cancer, non-small cell lung cancer, triple negative breast cancer, advanced solid tumors, luminal HR+/HER2- breast cancer, RB1-altered solid tumors, and neuroblastoma. | |||||||||||||||||||||
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- [1]. B. Levin, et al. EP.03F.03 Orally Bioavailable Cyclin A/B Rxl Macrocycle has Antitumor Effect in SCLC & NSCLC Cell Line Derived (CDX) & Patient Derived Xenograft (PDX) Models. S455October 2024.
- [2]. Afshin Dowlati, et al. Abstract CT023: Early clinical activity from the phase 1 evaluation of CID-078, a novel Cyclin A/B-RxL inhibitor, in patients with advanced solid tumors. Cancer Res (2026) 86 (8_Supplement): CT023.
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[3]. Nehal J. Lakhani, et al. A Phase 1 study to evaluate the safety, pharmacokinetics, and
efficacy of the first-in-class Cyclin A/B RxL inhibitor CID-078, an
orally bioavailable, cell-permeable macrocycle. - [4]. Dylan M.M. Jongerius, et al. CID-078, an orally bioavailable cyclin A/B-RxL inhibitor elicits anti-tumor activity in neuroblastoma models.
Keywords
