Chemical Structure : Linker-free PROTAC Pro-BA
CAS No.:
Linker-free PROTAC Pro-BA
(Proline-Brigatinib analog)
货号: PC-24674Not For Human Use, Lab Use Only.
Linker-free PROTAC Pro-BA is a linker-free PROTAC degarder of EML4-ALK protein with DC50 of 74 nM and achieves an 82% reduction at 500 nM in H3122 cells, shows cell growth IC50 of 34 nM.
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
Linker-free PROTAC Pro-BA is a linker-free PROTAC degarder of EML4-ALK protein with DC50 of 74 nM and achieves an 82% reduction at 500 nM in H3122 cells, shows cell growth IC50 of 34 nM.
Pro-BA induces reduction of EML4-ALK protein levels in H3122 cells starting at 100 nM.
Pro-BA outperforms the linker-containing degraders in vitro.
Pro-BA induces a strong interaction between the target and the E3 ubiquitin ligase.
Pro-BA is a water-soluble, orally administered degrader that significantly inhibits the tumor growth in a xenograft mouse model.
Pro-BA facilitates EML4-ALK degradation through the ubiquitin-proteasome system.
Pro-BA introduced a new interaction between EML4-ALK and GID4 and subsequently promoted EML4-ALK ubiquitylation.
. GID4, serving as the substrate receptor for the CTLH E3 ligase complex, is responsible for recognizing substrates featuring an N-terminal proline.
物理化学性质&存储条件
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分子量
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667.19
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分子式
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C33H44ClN8O3P
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(S)-(4-(1-(4-((5-chloro-4-((2-(dimethylphosphoryl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)piperidin-4-yl)piperazin-1-yl)(pyrrolidin-2-yl)methanone
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参考文献
1. Jianchao Zhang, et al. Nature Communications volume 16, Article number: 4794 (2025).
