Nodinitib-1
| CAS号 | 799264-47-4 | 货号 | BCP20383 |
| 中文名 | Nodinitib-1 | ||
| 英文名 | Nodinitib-1 | ||
| 中文别名 | |||
| 英文别名 | ML-130;ML130;ML 130; | ||
| 分子式 | C14H13N3O2S | 分子量 | 287.34 |
| 生物活性 | Afuresertib (GSK2110183) shows concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3β, PRAS40, FOXO and Caspase 9 in both BT474 and LNCaP cell lines. GSK2110183 consistently has potent anti-proliferative effects on a variety of hematological malignancies. Overall 65% of the hematological cell lines are sensitive to GSK2110183 (EC50<1 μM). Among solid tumor cell lines, 21% have EC50<1 μM in response to GSK2110183. In Vivo Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which results in 8, 37 and 61% tumor growth inhibition (TGI), respectively. Mice tolerates GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recovers over the course of the study. Other tumor xenograft models which possess an activation of the AKT pathway are explored to further demonstrate compound efficacy. Mice bearing SKOV3 ovarian tumor xenografts with 10, 20 | ||
| 信号通路 | Others Pathway | ||
| 靶 点 | NLR | ||
结构式
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