| Bioactivity | BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction. BPA-B9 has excellent RXRα-binding affinity (KD=39.29 ± 1.12 nM). BPA-B9 inhibits the proliferation of cancer cells by inducing mitotic arrest and cell apoptosis[1]. |
| Invitro | BPA-B9 (0-250 nM, 24 h) 在 MDA-MB-231 细胞中诱导细胞凋亡[1]。BPA-B9 (0-125 nM, 12 h) 在G2/M期抑制A549细胞周期[1]。BPA-B9 (0-500 nM, 0-24 h) 诱导裂解 PARP 表达的剂量和时间依赖性增加，抗凋亡蛋白 Bcl-2 和 Mcl-1 剂量依赖性降低 [1].BPA-B9 对 TNBC 细胞系 MDA-MB-231 表现出优异的抗增殖活性 (IC50=16 ± 3 nM，SI > 3)，并对 HCC1937、A549、H460、 HepG2 和 HeLa 细胞的 IC50 值分别为 0.561 μM、0.201 μM、0.253 μM、0.128 μM 和 0.077 μM[1]。 Apoptosis Analysis[1] Cell Line: |
| In Vivo | BPA-B9 (0-25 mg/kg，腹腔注射，每天一次，连续15天）在体内具有显着的抗癌功效，且无明显副作用[1]。BPA-B9 (25 mg/kg，腹腔注射或口服，一次)显示出比 XS-060 (HY-149085) 更好的药代动力学[1]。 Animal Model: |
| Name | BPA-B9 |
| Formula | C25H26N4O2 |
| Molar Mass | 414.50 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Chen J, et al. Discovery of bipyridine amide derivatives targeting pRXRα-PLK1 interaction for anticancer therapy. Eur J Med Chem. 2023 Apr 6;254:115341. |