KU-0060648 - CAS:881375-00-4

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KU-0060648

目录号 : KM11304 CAS No. : 881375-00-4 纯度 : 98%

Data Sheet SDS 产品使用指南

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 。

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5mg		In-stock
10mg	询价	In-stock
50mg	询价	In-stock

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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.

IC₅₀&Target

PI3Kα

4 nM (IC₅₀)

PI3Kβ

0.5 nM (IC₅₀)

PI3Kγ

0.594 μM (IC₅₀)

PI3Kδ

0.1 nM (IC₅₀)

DNA-PK

8.6 nM (IC₅₀)

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.

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

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.

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.

分子式

C₃₃H₃₇Cl₃N₄O₄S

分子量

582.71

CAS号

881375-00-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

纯度： 98%

Data Sheet

SDS

产品使用指南

暂无相关参考文献

The molarity calculator equation

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

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

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

浓度

体积

浓度

体积

重置计算

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

只

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

% DMSO

计算重置

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:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器