KU 59403 - CAS:845932-30-1

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KU 59403

目录号 : KM19348 CAS No. : 845932-30-1 纯度 : 98%

Data Sheet 产品使用指南

KU 59403 是 ATM 的一个有效抑制剂，其对 ATM、DNA-PK 和 PI3K 的 IC₅₀ 值分别为 3 nM、9.1 μM 和 10 μM。

规格	价格	是否有货
1mg		In-stock
5mg	询价	In-stock
10mg	询价	In-stock

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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.

体外研究

KU 59403 (1 μM) enhances VP-16 (1 μM) cytotoxicity to a similar extent in HCT116 and HCT116-N7 cells, and in the p53 mutant SW620 cells and human breast cancer cell line, MDAMB-231, sensitisation is 11.9±4.7 and 3.8±1.8-fold respectively. Inhibition of IR-induced ATM activity by KU 59403 (1 μM) is approximately 50% in MDA-MB231 cells and >50% in HCT116 cells that have low ATM expression and activity.

Cell Viability Assay

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

KU59403 with a single daily dose of 12.5 mg/kg causes a significant sensitization.
Increasing the dose of KU59403 to 25 mg/kg given twice daily results in the greatest chemo-sensitisation with a 3-fold increase in BMY-40481-induced tumour growth delay in both SW620 and HCT116-N7 xenografts, in the absence of a significantly increased toxicity.

Animal Model:	CD-1 nude mice implanted with SW620 or HCT116-N7 human cancer cell lines at 1×10 cells per animal s.c. (n=5 per group).
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.

分子式

C₂₉H₃₂N₄O₄S₂

分子量

564.72

CAS号

845932-30-1

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)

纯度： 98%

Data Sheet

产品使用指南

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The molarity calculator equation

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

质量

浓度

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

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浓度

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动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

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第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

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计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器