LYN-1604 - CAS:2088939-99-3

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LYN-1604

目录号 : KCM12492 CAS No. : 2088939-99-3 纯度 : ≥98%

Data Sheet 产品使用指南

LYN-1604 是一种有效的 UNC-51 样激酶 1 (ULK1) 激活剂，EC50 值为 18.94 nM。LYN-1604 可用于三阴性乳腺癌 (TNBC) 的研究。

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock

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生物活性

LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).

IC₅₀&Target

ULK1

18.94 nM (EC₅₀)

体外研究

LYN-1604 is a potential ULK1 agonist (enzymatic activity=195.7% at 100 nM and IC₅₀=1.66 μM against MDA-MB-231 cells).
LYN-1604 binds to wild-type ULK1 with a binding affinity in the nanomole range (K_D=291.4 nM) .
LYN-1604 (0.5, 1.0 and 2.0 μM) induces cell death via the ULK complex in MDA-MB-231 cells.
LYN-1604 (0.5-2 μM, 24 hours) induces remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II in MDA-MB-231 cells.
LYN-1604 induces ATG5-dependent autophagy via the ULK complex.
LYN-1604 can also increase cleavage of caspase3 and induce apoptosis.

Cell Viability Assay

Cell Line:	MDA-MB-231 cells
Concentration:	0.5, 1.0 and 2.0 μM
Incubation Time:
Result:	Induced cell death. Autophagy ratio was increased in a dose-dependent manner.

Western Blot Analysis

Cell Line:	MDA-MB-231 cells
Concentration:	0, 0.5, 1, and 2 μM
Incubation Time:	24 hours
Result:	Induced remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II.

体内研究

LYN-1604 (low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg; intragastric administration once a day for 14 days) inhibits the growth of xenograft TNBC by targeting ULK1-modulated cell death.

Animal Model:	24 female nude mice (BALB/c, 6-8 weeks, 20-22 g)
Dosage:	Low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg
Administration:	Intragastric administration; once a day for 14 days
Result:	Significantly inhibited the growth of xenograft MDA-MB-231 cells. The body weights of mice were stable. By the end of the experiment, the liver and spleen weight indexes of mice were slightly increased in parts of the groups, while the kidney weight index was not affected in all dose groups.

分子式

C₃₃H₄₃Cl₂N₃O₂

分子量

584.62

CAS号

2088939-99-3

中文名称

2-[双(2-甲基丙基)氨基]-1-[4-[2-(2,4-二氯苯基)-2-(2-萘基甲氧基)乙基]-1-哌嗪基]乙酮

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

溶解性数据

In Vitro:

DMSO: 100 mg/mL (171.05 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7105 mL	8.5526 mL	17.1051 mL
5 mM	0.3421 mL	1.7105 mL	3.4210 mL
10 mM	0.1711 mL	0.8553 mL	1.7105 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。

纯度： ≥98%

Data Sheet

产品使用指南

Zhang L, et al. Discovery of a small molecule targeting ULK1-modulated cell death of triple negative breast cancer in vitro and in vivo. Chem Sci. 2017 Apr 1;8(4):2687-2701.

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。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器