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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-CID-078
CID-078

Chemical Structure : CID-078

CAS No.: 3064485-16-8

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CID-078 (CID078)

货号: PC-27526Not For Human Use, Lab Use Only.

CID-078 is a highly potent, first-in-class, oral macrocycle cyclin A/B-RxL inhibitor with IC50 of <0.02 uM for both cyclin A and cyclin B in FP assays, Kd of 1.1 nM and 0.83 nM for cyclin A and cyclin B respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CID-078 is a highly potent, first-in-class, oral macrocycle cyclin A/B-RxL inhibitor with IC50 of <0.02 uM for both cyclin A and cyclin B in FP assays, Kd of 1.1 nM and 0.83 nM for cyclin A and cyclin B respectively.
CID-078 drives replication stress and mitotic catastrophe, leading to tumor cell death.
CID-078 (50-100 mg/kg PO BID) inhibits tumor growth inhibition in a SCLC CDX model. CID-078 demonstrates greater activity in an Rb-deficient vs Rb-proficient lung PDX model.

物理化学性质&存储条件

分子量 985.51
分子式 C47H63ClF6N8O6
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

L-Phenylalanine, (4R)-1-[[3,3-difluoro-1-(trifluoromethyl)cyclobutyl]carbonyl]-4-fluoro-L-prolyl-(2S)-2-cyclopropylglycyl-2,9-bis(methylamino)nonanoyl-L-leucyl-5-chloro-2-(1-methyl-1H-pyrazol-4-yl)-N-methyl-, (5→3)-lactam

参考文献

1. Patent WO2024243010 A1 2024-11-28.

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