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首页-抗体药物偶连体和PROTACs-PROTAC-Helios degrader ALV2
Helios degrader ALV2

Chemical Structure : Helios degrader ALV2

CAS No.: 2438124-95-7

Helios degrader ALV2 (ALV-04-019-01)

货号: PC-38303Not For Human Use, Lab Use Only.

Helios degrader ALV2 (ALV-04-019-01) is a potent and selective Helios degrader with IC50 of 0.57 uM in CRBN-binding TR-FRET assay.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Helios degrader ALV2 (ALV-04-019-01) is a potent and selective Helios degrader with IC50 of 0.57 uM in CRBN-binding TR-FRET assay.
ALV2 recruited the E3 ubiquitin ligase substrate receptor cereblon to Helios.
ALV2 bound CRBN in vitro with greater potency than lenalidomide but less than CC-885.
ALV2 also induced CRBN-Helios dimerization in the TR-FRET assay, with greater activity than either CC-885.
ALV2 exhibited relative selectivity for Helios, but not ALV1, exhibited potent degradation of ZNF692 and ZNF653.

物理化学性质&存储条件

分子量 523.974
分子式 C26H26ClN5O5
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

1-(3-chloro-4-methylphenyl)-3-(2-(3-((1-(2,6-dioxopiperidin-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl)amino)phenyl)propan-2-yl)urea

参考文献

1. Eric S Wang, et al. Nat Chem Biol. 2021 Jun;17(6):711-717.

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