型号:
产品价格:电议      采购度:1595      原产地:美洲
发布时间:2021/8/2 17:16:55 所属地区:上海 上海市
简要描述:
NSC781406是高效的 PI3K 和 mTOR 抑制剂,对PI3Kα的 IC50 值为2 nM。
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CAS No. : 1676893-24-5
MCE 站:NSC781406
产品活性:NSC781406是高效的 PI3K 和 mTOR 抑制剂,对PI3Kα的 IC50 值为2 nM。
研究领域:PI3K/Akt/mTOR
In Vitro: NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC50=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20 nM). NSC781406 displays reasonable liver microsome stability. NSC781406 demonstrates cytotoxic activities against leukemia, non-small cell, lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. It is potent against 60 cancer cell lines with a mean GI50 value of 65 nM, and with a GI50 value less than 10 nM against four cancer cell lines.
In Vivo: In the xenograft models, treatment with 30 mg/kg of NSC781406 results in statistically significant antitumor activity, with a mean reduction in relative tumor volume ratio of 52%. Sorafenib displays an inhibition ratio of 44% at 50 mg/kg. NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight.
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更新时间:2024/1/2 10:17:29
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