KU-0060648|cas:881375-00-4|西域试剂

KU-0060648,99.39%

产品编号：Bellancom-13431| CAS NO：881375-00-4| 分子式：C₃₃H₃₄N₄O₄S| 分子量：582.71

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货号	价格	库存与货期
Bellancom-13431	￥1750.00	杭州北京（现货）
Bellancom-13431	￥3000.00	杭州北京（现货）
Bellancom-13431	￥6500.00	杭州北京（现货）

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KU-0060648

产品介绍

KU-0060648 是 PI3K 和 DNA-PK 的双重抑制剂，抑制 PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ 和 DNA-PK 的 IC₅₀ 值分别为 4 nM，0.5 nM，0.1 nM，0.594 nM 和 8.6 nM。

生物活性

KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC₅₀s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively.

体外研究

KU-0060648 inhibits cellular DNA-PK auto-phosphorylation with IC₅₀ values of 0.019 μM (MCF7 cells) and 0.17 μM (SW620 cells), and PI-3K-mediated AKT phosphorylation with IC₅₀ values of 0.039 μM (MCF7 cells) and >10 μM (SW620 cells).
KU-0060648 (30-500 nM; 72 hours) dose-dependently inhibits HepG2 cell proliferation, IC₅₀=134.32nM.
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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	Human breast (MCF7, T47D and MDA-MB-231) and colon (LoVo and SW620) cancer cells
Concentration:	0.1-1 μM
Incubation Time:	5 days
Result:	Resulted in> 50% inhibition of cell growth in all cell lines.

Western Blot Analysis

Cell Line:	HCC cells; HepG2/Huh-7 cells
Concentration:	100-300 nM
Incubation Time:	12 hours
Result:	Inhibited phosphatidylinositol 3-kinase (PI3K) and in-activates AKT-mTOR signaling.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	HepG2 xenograft nude mice model
Dosage:	10 and 50 mg/kg
Administration:	Intraperitoneal injection; 10 and 50 mg/kg; once daily; daily for 21 days
Result:	Suppressed HepG2 xenograft growth in nude mice.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	HepG2 xenograft nude mice model
Dosage:	10 and 50 mg/kg
Administration:	Intraperitoneal injection; 10 and 50 mg/kg; once daily; daily for 21 days
Result:	Suppressed HepG2 xenograft growth in nude mice.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	HepG2 xenograft nude mice model
Dosage:	10 and 50 mg/kg
Administration:	Intraperitoneal injection; 10 and 50 mg/kg; once daily; daily for 21 days
Result:	Suppressed HepG2 xenograft growth in nude mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 2.78 mg/mL (4.77 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7161 mL	8.5806 mL	17.1612 mL
5 mM	---	---	---
10 mM	---	---	---

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.28 mg/mL (0.48 mM); Clear solution

此方案可获得 ≥ 0.28 mg/mL (0.48 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 2.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.28 mg/mL (0.48 mM); Clear solution

此方案可获得 ≥ 0.28 mg/mL (0.48 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 2.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 0.28 mg/mL (0.48 mM); Clear solution

此方案可获得 ≥ 0.28 mg/mL (0.48 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 2.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。