| Description |
XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction[1].
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| Related Catalog |
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| Target |
RXRα (Retinoid X receptor alpha)[1]
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| In Vitro |
XS-060 靶向 RXRα' 的共激活因子结合位点可抑制 pRXRα-PLK1 相互作用，作为抗有丝分裂剂表现出良好的抗肿瘤活性[1]。 XS-060 对 MDA-MB 231 癌细胞具有抗增殖活性，IC50 为 6.880 ± 0.059 μM[1]。 Cell Proliferation Assay[1] Cell Line: MDA-MB 231, A549, and HepG2 Concentration: 5 μM Incubation Time: Result: Showed anti-proliferative activity at 5 μM against cancer cells (MDA-MB 231, A549, and HepG2), with cell viability rate (%) of 51.93 ± 4.32, 82.65 ± 2.84, and 48.65 ± 6.45, respectively.
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| In Vivo |
XS-060 (25 mg/kg, IP or PO, once) 腹腔注射吸收良好，但口服吸收很差[1]。 Animal Model: Sprague-Dawley rats (10-14 weeks, 200-220g)[1] Dosage: 25 mg/kg Administration: Oral absorption (p.o.) and intraperitoneal injection (i.p.), once, (Pharmacokinetic Analysis) Result: The oral absorption of XS-060 is very poor, while intraperitoneal injection displayed good absorption[1]. Pharmacokinetic Parameters of XS-060 in Sprague-Dawley rats[1]. XS060 25 mg/kg (i.p.) Tmax (h) 2.67 ± 1.12 Cmax (μg/L) 1061.50 ± 399.20 AUC0-∞ (μg⋅h/L) 7040.30 ± 1593.52 T1/2 (h) 2.13 ± 0.05 CLz/F (L/(h⋅kg)) 3.67 ± 0.81 Vd, z/F (L/kg) 11.31 ± 2.71
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| References |
[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.
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