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编 号:F655503
分子式:C27H37N3O6
分子量:499.6
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生物活性:
Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC).

体内研究:
Onalespib lactate (30 mg/kg;i.v.;一次) 可穿过血脑屏障 (BBB) 并在 6 周龄 ICR 小鼠中引起 HSP90 的持续抑制。Onalespib lactate (0.5 μM;移植后 5 至 10 天) 和 TMZ (HY-17364) (10 μM) 可减少斑马鱼胚胎中的肿瘤生长并延长存活期。Onalespib lactate (5、10 mg/kg 用于 HCT116 异种移植物,20 mg/kg 用于 A431 异种移植物;i.p.;每天一次,持续 3 天) 在 HCT116 和 A431 异种移植物中显示出抗肿瘤活性。Animal Model:Female nu/nu Balb/c mice (HCT116 and A431 xenografts)
Dosage:5, 10 mg/kg for HCT116 xenografts, 20 mg/kg for A431 xenografts
Administration:I.p.; on day 1, 2, and 3 days
Result:Inhibited tumor growth and had a median survival of 9.5 days and the maximum survival was 14 days in HCT116 xenografts, reduced the tumor size significantly by 32% in A431 xenografts.

体外研究:
Onalespib lactate (0-0.4 μM; 72 h, 48 h) 抑制神经胶质瘤细胞的增殖、存活和迁移。Onalespib lactate (0-0.4 μM; 48 h) 以剂量依赖性方式降低 EGFR、p-EGFR、AKT、P-AKT、ERK1/2、P-ERK1/2、S6、P-S6 蛋白的表达。
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