CAS NO: | 881375-00-4 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | KU-0060648 is a dual inhibitor ofPI3KandDNA-PKwithIC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM forPI3Kα,PI3Kβ,PI3Kγ,PI3KδandDNA-PK, respectively[1]. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | KU-0060648 inhibits cellular DNA-PK auto-phosphorylation with IC50values of 0.019 μM (MCF7 cells) and 0.17 μM (SW620 cells), and PI-3K-mediated AKT phosphorylation with IC50values of 0.039 μM (MCF7 cells) and >10 μM (SW620 cells)[1].KU-0060648 (30-500 nM; 72 hours) dose-dependently inhibits HepG2 cell proliferation, IC50=134.32nM[2].KU-0060648 (0.1-1 μM;5 days) inhibits cell lines growth with GI50s of 0.95 μM, 0.21 μM, 0.27 μM, 0.41 μM and 1 μM in SW620, LoVo, MCF7, T47D and MDA-MB-231 cells[1].KU-0060648 (100-300 nM;12 hours) significantly inhibits activation of PI3K (p85 phosphorylation), AKT (Ser-473 and Thr-308 phosphorylations) and mTOR (p70S6K1 Thr-389 phosphorylation) in HepG2/Huh-7 lines and primary human HCC cells[2]. Cell Proliferation Assay[1]
Western Blot Analysis[2]
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体内研究 (In Vivo) | KU-0060648 (intraperitoneal injection; 10 and 50 mg/kg; once daily; daily for 21 days) dramatically inhibits HepG2 xenograft growth in nude mice, the tumor weights (at week 5) of KU-0060648 group mice are dramatically lighter than that of vehicle control mice and exert a dose-dependent effect in vivo[1].
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分子量 | 582.71 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C33H34N4O4S | ||||||||||||||||
CAS 号 | 881375-00-4 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 2.78 mg/mL(4.77 mM;ultrasonic and warming and heat to 60℃) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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