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首页-抗体药物偶连体和PROTACs-PROTAC-BETd-260
BETd-260

Chemical Structure : BETd-260

CAS No.: 2093388-62-4

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BETd-260 (ZBC 260, ZBC260, BETd260)

货号: PC-60102Not For Human Use, Lab Use Only.

BETd-260 (ZBC260, BETd260) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.

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1 mg ￥1880 In stock
5 mg ￥3580 In stock
10 mg ￥5880 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

BETd-260 (ZBC260, BETd260) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.
BETd-260 effectively degrades BRD4 protein at 30 pM in the RS4;11 leukemia cell line, achieves an IC50 of 51 pM in inhibition of RS4;11 cell growth.
BETd-260 induces rapid tumor regression in vivo against RS4;11 xenograft tumors.

物理化学性质&存储条件

分子量 798.905
分子式 C43H46N10O6
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

4-((3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino)-7-(3,5-dimethylisoxazol-4-yl)-N-(5-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)pentyl)-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide

参考文献

1. Zhou B, et al. J Med Chem. 2017 Mar 24. doi: 10.1021/acs.jmedchem.6b01816.

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