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首页-抗体药物偶连体和PROTACs-PROTAC-CP5V
CP5V

Chemical Structure : CP5V

CAS No.: 2509359-75-3

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CP5V (apcin-A-PEG5-VHL Ligand 1)

货号: PC-20565Not For Human Use, Lab Use Only.

CP5V (apcin-A-PEG5-VHL Ligand 1) is an efficient, selective Cdc20 PROTAC with DC50 of 1.6 uM in both MCF7 and MDA-MB-231 cells, induces mitotic inhibition and suppresses cancer cell proliferation.

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5 mg ￥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CP5V (apcin-A-PEG5-VHL Ligand 1) is an efficient, selective Cdc20 PROTAC with DC50 of 1.6 uM in both MCF7 and MDA-MB-231 cells, induces mitotic inhibition and suppresses cancer cell proliferation.
CP5V-induced degradation of Cdc20 is mediated through the ubiquitin-proteasome pathway.
CP5V-induced Cdc20 degradation is sensitive to neddylation inhibitor MLN4924.
CP5V efficiently binds onto Cdc20 (SOR KD=11.2 uM) to help stabilize Cdc20-PROTACS-VHL-ElonginC-ElonginB complex.
CP5V significantly inhibits mitotic progression and induces breast cancer cell death.
CP5V restores Taxol-induced cytotoxic response in Taxol-resistant cells.
CP5V is a potent inhibitor that suppresses breast tumor progression with no toxicity in 4T1 xenograft model.

物理化学性质&存储条件

分子量 1075.49
分子式 C46H66Cl3N9O12S
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

(S)-25-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidine-1-carbonyl)-26,26-dimethyl-5,23-dioxo-8,11,14,17,20-pentaoxa-4,24-diazaheptacosyl (2,2,2-trichloro-1-(pyrimidin-2-ylamino)ethyl)carbamate

参考文献

1. Junlong Jack Chi, et al. EBioMedicine. 2019 Nov;49:40-54.

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