1. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  2. ATM/ATR
  3. KU 59403

KU 59403 是 ATM 的一个有效抑制剂,其对 ATM、DNA-PK 和 PI3KIC50 值分别为 3 nM、9.1 μM 和 10 μM。

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KU 59403 Chemical Structure

KU 59403 Chemical Structure

CAS No. : 845932-30-1

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
1 mg ¥1590
In-stock
5 mg ¥3500
In-stock
10 mg ¥5500
In-stock
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100 mg   询价  

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Customer Review

查看 ATM/ATR 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KU 59403 is a potent ATM inhibitor, with IC50 values of 3 nM, 9.1 μM and 10 μM for ATM, DNA-PK and PI3K, respectively[1].

IC50 & Target

IC50: 3 nM (ATM)[1].

体外研究
(In Vitro)

KU 59403 (1 μM) 在 HCT116 和 HCT116-N7 细胞中增强 VP-16 (1 μM) 细胞毒性至相似程度,在 p53 突变体 SW620 细胞和人乳腺癌细胞系 MDAMB-231 中,致敏作用为 11.9±4.7和 3.8±1.8 倍。KU 59403 (1 μM) 对 IR 诱导的 ATM 活性的抑制作用在 MDA-MB231 细胞中约为 50%,在 ATM 表达和活性较低的 HCT116 细胞中约为 50%[1]

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

Cell Viability Assay[1]

Cell Line: LoVo, HCT116 and SW620 (human colon cancer), and U2OS (human osteosarcoma) and MDA-MB-231 (human breast cancer) cells.
Concentration: 1 μM.
Incubation Time: 16 hours.
Result: Had at least 1000 times greater specificity for ATM over other members of the PI3K family tested.
Enhanced camptothecin cytotoxicity in both cell lines with greater enhancement being observed in the LoVo compared to the SW620 cells.
Significantly enhanced the cytotoxicity of fixed concentrations of VP-16 (0.1 and 1 μM) or NSC 123127 (10 or 100 nM) in these cell lines, with greater enhancement of VP-16 in SW620 cells and of NSC 123127 in LoVo cells.
体内研究
(In Vivo)

KU59403 每日单次剂量为 12.5 mg/kg 会引起显著的致敏作用[1]
将 KU59403 的剂量增加至 25 mg/kg,每天两次会导致最大的化学致敏作用,在 SW620 和 HCT116-N7 异种移植物中, BMY-40481 诱导的肿瘤生长延迟增加了 3 倍,而没有显著的化疗敏感性和毒性增加[1]

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

Animal Model: CD-1 nude mice implanted with SW620 or HCT116-N7 human cancer cell lines at 1×107 cells per animal s.c. (n=5 per group)[1].
Dosage: 6, 12.5 and 25 mg/kg.
Administration: I.P. twice daily (0 and 4 hours) and 12.5 mg/kg once daily.
Result: Treatment with BMY-40481 alone causes a modest tumour growth delay of 4 days (time to RTV4=10.5 days). This delay is extended to 8.5 days when given with KU 59403 at 12.5 mg/kg i.p. twice daily for 5 days and 11.5 days (time to RTV4=18 days) when given with KU 59403 at 25 mg/kg i.p. twice daily for 5 days.
分子量

564.72

Formula

C29H32N4O4S2

CAS 号
性状

固体

颜色

White to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 10 mg/mL (17.71 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7708 mL 8.8539 mL 17.7079 mL
5 mM 0.3542 mL 1.7708 mL 3.5416 mL
查看完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.23%

参考文献

完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7708 mL 8.8539 mL 17.7079 mL 44.2697 mL
5 mM 0.3542 mL 1.7708 mL 3.5416 mL 8.8539 mL
10 mM 0.1771 mL 0.8854 mL 1.7708 mL 4.4270 mL
15 mM 0.1181 mL 0.5903 mL 1.1805 mL 2.9513 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

产品名称:
KU 59403
目录号:
HY-18650
需求量: