KU-60019|cas:925701-46-8|西域试剂

KU-60019,99.0%

产品编号：Bellancom-12061| CAS NO：925701-46-8| 分子式：C₃₀H₃₃N₃O₅S| 分子量：547.67

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货号	价格	库存与货期
Bellancom-12061	￥780.00	杭州北京（现货）
Bellancom-12061	￥1100.00	杭州北京（现货）
Bellancom-12061	￥3950.00	杭州北京（现货）
Bellancom-12061	￥6500.00	杭州北京（现货）

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KU-60019

产品介绍

KU-60019 是一种 ATM 激酶特异性的抑制剂，IC₅₀ 为 6.3 nM。

生物活性

KU-60019 is an improved ATM kinase-specific inhibitor with IC₅₀ of 6.3 nM.

体外研究

KU-60019 is an improved analogue of KU-55933. KU-55933 has an IC₅₀ of 13 nM and K_i of 2.2 nM in vitro and is highly specific for the ATM kinase using a panel of 60 protein kinases. KU-60019 is an improved inhibitor of the ATM kinase with an IC₅₀ of 6.3 nM, approximately half that of KU-55933. The IC₅₀ values for DNA-PKcs and ATR are 1.7 and >10 μM, respectively, almost 270-and 1600-fold higher than for ATM. KU-60019 is 10-fold more effective than KU-55933 at blocking radiation-induced phosphorylation of key ATM targets in human glioma cells. In human U87 glioma cells, KU-55933 completely inhibits phosphorylation of p53 (S15) at 10 μM but not at 3 μM, whereas γ-H2AX levels are only partly reduced with 10 μM 1 h after irradiation. By comparison, 3 μM KU-60019 completely inhibits p53 phosphorylation and partial inhibits at 1 μM.

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

体内研究

Despite PTEN-deficient control tumors reaching a 4-fold increase in size before PTEN wild-type controls, KU-60019-treated PTEN-deficient tumors display a statistically significant slowing in growth. This growth inhibition is especially evident at the start of the experiment (days 5-12) just after KU-60019 is administered (days 1-5).

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (182.59 mM; Need ultrasonic)

Ethanol : 10 mg/mL (18.26 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8259 mL	9.1296 mL	18.2592 mL
5 mM	0.3652 mL	1.8259 mL	3.6518 mL
10 mM	0.1826 mL	0.9130 mL	1.8259 mL

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: ≥ 2.5 mg/mL (4.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.56 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (4.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.56 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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