LYN-1604 dihydrochloride

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LYN-1604 dihydrochloride  纯度: 98.73%

LYN-1604 dihydrochloride 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。

LYN-1604 dihydrochloride

LYN-1604 dihydrochloride Chemical Structure

CAS No. : 2310109-38-5

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥2100 In-stock
5 mg ¥1450 In-stock
10 mg ¥2550 In-stock
25 mg ¥4500 In-stock
50 mg ¥7500 In-stock
100 mg ¥11500 In-stock
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LYN-1604 dihydrochloride 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Breast Cancer Compound Library
  • Targeted Diversity Library

生物活性

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

IC50 & Target[1]

ULK1

18.94 nM (EC50)

体外研究
(In Vitro)

LYN-1604 is a potential ULK1 agonist (enzymatic activity=195.7% at 100 nM and IC50=1.66 μM against MDA-MB-231 cells) [1].
LYN-1604 binds to wild-type ULK1 with a binding affinity in the nanomole range (KD=291.4 nM) [1].
LYN-1604 (0.5, 1.0 and 2.0 μM) induces cell death via the ULK complex in MDA-MB-231 cells[1].
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[1].
LYN-1604 induces ATG5-dependent autophagy via the ULK complex[1].
LYN-1604 can also increase cleavage of caspase3 and induce apoptosis[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

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
(In Vivo)

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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 24 female nude mice (BALB/c, 6-8 weeks, 20-22 g)[1]
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.

分子量

657.54

Formula

C33H45Cl4N3O2

CAS 号

2310109-38-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°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
In Vitro: 

H2O : 50 mg/mL (76.04 mM; Need ultrasonic)

DMSO : 50 mg/mL (76.04 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5208 mL 7.6041 mL 15.2082 mL
5 mM 0.3042 mL 1.5208 mL 3.0416 mL
10 mM 0.1521 mL 0.7604 mL 1.5208 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 (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。

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 (3.80 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.80 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% corn oil

    Solubility: ≥ 2.5 mg/mL (3.80 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.80 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. 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.

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