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LYN-1604 hydrochloride

产品编号 T39687 CAS 2216753-86-3

LYN-1604 hydrochloride, a powerful activator of UNC-51-like kinase 1 (ULK1) with an EC50 value of 18.94 nM, has significant implications in the study of triple-negative breast cancer (TNBC).

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LYN-1604 hydrochloride Chemical Structure

LYN-1604 hydrochloride, CAS 2216753-86-3

规格	价格/CNY	货期
25 mg	￥ 6,210	6-8周
50 mg	￥ 8,067	6-8周
100 mg	￥ 14,817	6-8周

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LYN-1604 hydrochloride 的其他形式现货产品:

LYN-1604 dihydrochloride

其他形式的 LYN-1604 hydrochloride:

LYN-1604 dihydrochloride
现货
LYN-1604
询价

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	LYN-1604 hydrochloride, a powerful activator of UNC-51-like kinase 1 (ULK1) with an EC50 value of 18.94 nM, has significant implications in the study of triple-negative breast cancer (TNBC).
靶点活性	ULK1:18.94 nM (EC50)
体外活性	LYN-1604 is a potential ULK1 agonist (enzymatic activity=195.7% at 100 nM and IC 50 =1.66 μM against MDA-MB-231 cells)[1]. LYN-1604 binds to wild-type ULK1 with a binding affinity in the nanomole range (K D =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]. 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.
体内活性	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]. 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	621.08
分子式	C33H44Cl3N3O2
CAS No.	2216753-86-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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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.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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