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BPA-B9

Chemical Structure : BPA-B9

CAS No.:

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BPA-B9 (Bipyridine amide B9)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 414.51
Formula C25H26N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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