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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-CIRc-004
CIRc-004

Chemical Structure : CIRc-004

CAS No.: 3036232-05-7

CIRc-004 (CIRc004)

货号: PC-25358Not For Human Use, Lab Use Only.

CIRc-004 is a potent, cell-permeable dual cyclin A/B RxL inhibitor with IC50 of 0.13 and <0.02 uM for cyclin A1-CDK2 and cyclin B-CDK1, does not inhibit cyclin E1-CDK2, inhibits cyclin A/B-RxL interactions and induces apoptosis in cancer cells with high E2F activity.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CIRc-004 is a potent, cell-permeable dual cyclin A/B RxL inhibitor with IC50 of 0.13 and <0.02 uM for cyclin A1-CDK2 and cyclin B-CDK1, does not inhibit cyclin E1-CDK2, inhibits cyclin A/B-RxL interactions and induces apoptosis in cancer cells with high E2F activity.
Non-transformed WI-38 fibroblasts is insensitive to cyclin A/B inhibition.
CIRc-004 induces apoptosis and mitotic arrest in sensitive SCLC (NCI-H1048, H446 and H69).
CIRc-004 blocks anaphase initiation, consistent with SAC activation causing mitotic cell death.
CIRc-004 disrupts an interaction between cyclin B and an RxL-containing substrate that normally functions as a negative regulator of cyclin B–CDK1 activity.
CIRc-004 induces E2F1 hyperactivation and sensitizes cells to cyclin A/B RxL inhibitors.

物理化学性质&存储条件

分子量 994.90
分子式 C45H59Cl2F6N7O7
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S,4R)-N-((S)-3-cyclobutyl-1-(((6S,9S,12S)-6-(2,5-dichlorobenzyl)-9-isobutyl-7-methyl-5,8,11,18-tetraoxo-4,7,10,17-tetraazaspiro[2.15]octadecan-12-yl)(methyl)amino)-1-oxopropan-2-yl)-1-(3,3-difluoro-1-(trifluoromethyl)cyclobutane-1-carbonyl)-4-fluoropyrrolidine-2-carboxamide

参考文献

1. Singh S, et al. Nature. 2025 Aug 20. doi: 10.1038/s41586-025-09433-w.

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