NSC781406CAS号: 1676893-24-5分子式: C29H27F2N6O6S2分子量: 627.68描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα. |
纯度 |
98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
NSC-781406;NSC 781406
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外观 |
Powder
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可溶性/溶解性 |
DMSO : ≥ 150 mg/mL (238.98 mM)
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生物活性 | |
靶点 |
PI3Kα,PI3Kγ,PI3Kβ,PI3Kδ,mTOR
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In vitro(体外研究) |
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.
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In vivo(体内研究) |
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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分子结构图