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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⁺/HER^2- breast cancer, RB1-altered solid tumors, and neuroblastoma.

For research use only. We do not sell to patients.

CAS No.: 3064485-16-8
Formula: C₄₇H₆₃ClF₆N₈O₆
Molecular Weight:985.50

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

CID-078 Chemical Structure

CAS No.: 3064485-16-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

All CDK Isoforms :

In Vitro

CID-078 induces antiproliferation in 46 SCLC and 104 NSCLC cell lines, with enhanced activity observed in cells with high E2F and G2M hallmark pathway scores and/or elevated cyclin B1 and separase expression^[1].
CID-078 (4-8 days) inhibits proliferation of a broad panel of solid tumor cell lines, with significantly greater potency (lower GI₅₀ values) in RB1-altered cell lines, and heightened sensitivity correlated with high E2F targets and G₂/M checkpoint pathway scores in SCLC, TNBC, and NSCLC cell lines^[3].
CID-078 binds to the hydrophobic patch/RxL binding site of cyclin-CDK complexes, inhibits E2F1-cyclin A-CDK2 and MYT1-cyclin B-CDK1 interactions, and induces replication stress, DNA damage, and mitotic catastrophe in E2F1-high tumor cells^[3].
CID-078 (72 h) inhibits growth of established neuroblastoma cell lines with GI₅₀ values ranging from 0.001 μM (SKNSH) to 10 μM (SY5Y WT, GIMEN, TR14, SKNAS)^[4].
CID-078 (72 h) sensitizes CDKN2A-inactivated SH-SY5Y neuroblastoma cells, resulting in GI₅₀ values of 55 nM (C7.3 clone) and 6 nM (C8.10 clone) compared to >10 μM in wild-type SH-SY5Y cells^[4].
CID-078 (120 h) inhibits growth of patient-derived neuroblastoma organoid models with GI₅₀ values ranging from 0.01 μM to 1 μM^[4].
CID-078 (100 nM; 24 h) induces G₂/M-phase cell cycle arrest in neuroblastoma cell lines, with percentage increases in G₂/M population ranging from 52% (SY5Y C7.3) to 632% (SKNSH) compared to DMSO control^[4].
CID-078 (3-200 nM; 24 h) induces spindle assembly checkpoint activation (phospho-BUBR1), DNA damage (phospho-γH₂AX), and G2/M phase marker expression (phospho-FoxM1) in neuroblastoma cell lines and hTERT-RPE1 healthy control cells^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[4]

Cell Line:

SY5Y C7.3, TR14, SY5Y C8.10, SY5Y WT, SHEP2, HDN33, SKNAS, GIMEN, NGP, SJNB6, NMB, SKNSH
Concentration:

100 nM
Incubation Time:

24 h
Result:

Increased the G2/M-phase population compared to DMSO control, with percentage increases ranging from 52% (SY5Y C7.3) to 632% (SKNSH).

Western Blot Analysis^[4]

Cell Line:

SY5Y WT, SY5Y C7.3, SY5Y C8.10, SJNB6, SKNSH, TR14, HDN33, GIMEN, SKNAS, hTERT-RPE1
Concentration:

20 nM, 200 nM
Incubation Time:

24 h
Result:

Induced phosphorylation of BUBR1 (SAC activation) in SY5Y WT, SY5Y C7.3, SY5Y C8.10, SJNB6, and hTERT-RPE1 cells at 20 nM and 200 nM.
Induced phosphorylation of γH2AX (DNA damage) in SY5Y WT, SY5Y C7.3, SY5Y C8.10, SJNB6, and SKNSH cells at 20 nM and 200 nM; in TR14 and HDN33 cells at 3 nM, 30 nM, and 100 nM.
Induced phosphorylation of FoxM1 (G2/M phase marker) in SY5Y WT, SY5Y C7.3, SY5Y C8.10, GIMEN, and SKNAS cells at 3 nM and 100 nM.

In Vivo

CID-078 (100 mg/kg; p.o.; twice daily) shows robust single-agent activity in a TNBC RB1 mutant PDX model and a Luminal HR+/HER2- post-CDK4/6 inhibitor PDX model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 3064485-16-8
Molecular Weight 985.50
Formula C₄₇H₆₃ClF₆N₈O₆
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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.

[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.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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