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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-RAR/RXR-BPA-B9
BPA-B9

Chemical Structure : BPA-B9

CAS No.:

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BPA-B9 (Bipyridine amide B9)

货号: PC-20840Not For Human Use, Lab Use Only.

BPA-B9 (Bipyridine amide B9) is a small molecule RXRα-targeted anti-mitotic agent, binds to RXRα (Kd=39 nM) and selectively inhibits the p-RXRα/PLK1 interaction to induce mitotic arrest and catastrophe in cancer cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BPA-B9 (Bipyridine amide B9) is a small molecule RXRα-targeted anti-mitotic agent, binds to RXRα (Kd=39 nM) and selectively inhibits the p-RXRα/PLK1 interaction to induce mitotic arrest and catastrophe in cancer cells.
BPA-B9 showed better activity than XS-060, with excellent RXRα-binding affinity and anti-proliferative activity against MDA-MB-231 (IC50=16 nM).
BPA-B9 displayed better pharmacokinetics than the lead XS-060.
BPA-B9 had significant anticancer efficacy in vivo with no considerable side effects.

物理化学性质&存储条件

分子量 414.51
分子式 C25H26N4O2
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

O=C(NC1=NC=CC(C2=CC(N3CCC(CO)CC3)=NC=C2)=C1)/C=C/C4=CC=CC=C4

参考文献

1. Jun Chen, et al. Eur J Med Chem. 2023 Jun 5;254:115341.

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