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编 号：F762315
分子式：C20H18N2O3
分子量：334.37
分子式：C20H18N2O3
分子量：334.37
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CAS No: 346721-50-4
产品详情
生物活性：
XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction. XS-060 inhibits p-RXRα interaction with PLK1 but has no effect on RXRα heterodimerization with RARγ. XS-060 inhibits the in situ interaction between p-RXRα and PLK1 at the centrosome.
体内研究：
XS-060 (25 mg/kg, IP or PO, once) 腹腔注射吸收良好，但口服吸收很差。Animal Model:Sprague-Dawley rats (10-14 weeks, 200-220g)
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. Pharmacokinetic Parameters of XS-060 in Sprague-Dawley rats. 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
体外研究：
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。XS-060 对 MDA-MB 231 癌细胞具有抗增殖活性，IC50 为 6.880 ± 0.059 μM。
XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction. XS-060 inhibits p-RXRα interaction with PLK1 but has no effect on RXRα heterodimerization with RARγ. XS-060 inhibits the in situ interaction between p-RXRα and PLK1 at the centrosome.
体内研究：
XS-060 (25 mg/kg, IP or PO, once) 腹腔注射吸收良好，但口服吸收很差。Animal Model:Sprague-Dawley rats (10-14 weeks, 200-220g)
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. Pharmacokinetic Parameters of XS-060 in Sprague-Dawley rats. 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
体外研究：
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。XS-060 对 MDA-MB 231 癌细胞具有抗增殖活性，IC50 为 6.880 ± 0.059 μM。
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