| Identification | Back Directory | [Name]
LYN-1604 | [CAS]
2088939-99-3 | [Synonyms]
CS-2610
CS-2635
LYN-1604
LYN-1604 Hcl
LYN-1604 2HCl
LYN1604;LYN 1604
LYN-1604;LYN 1604;LYN1604
Ethanone, 2-[bis(2-methylpropyl)amino]-1-[4-[2-(2,4-dichlorophenyl)-2-(2-naphthalenylmethoxy)ethyl]-1-piperazinyl]- | [Molecular Formula]
C33H43Cl2N3O2 | [MDL Number]
MFCD31619235 | [MOL File]
2088939-99-3.mol | [Molecular Weight]
584.62 |
| Chemical Properties | Back Directory | [Boiling point ]
670.9±55.0 °C(Predicted) | [density ]
1.168±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/ml; DMSO: 20 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml | [form ]
A crystalline solid | [pka]
8.03±0.50(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Description]
LYN-1604 is an activator of unc-51-like kinase 1 (ULK1; EC50 = 18.94 nM). It increases Beclin 1, LC3-II, and total LC3 protein levels and reduces levels of p62 in human MDA-MB-231 triple-negative breast cancer (TNBC) cells in a concentration-dependent manner, indicating an increase in autophagy. It also increases the cleavage of the pro-apoptotic protein caspase-3. LYN-1604 decreases the viability of MDA-MB-231 cells in vitro (IC50 = 1.66 μM), an effect that can be reversed by the autophagy inhibitor 3-methyladenine (3-MA; ). LYN-1604 (25, 50, and 100 mg/kg) reduces tumor growth in an MDA-MB-231 mouse xenograft model. | [Uses]
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)[1]. | [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]. | 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. |
| [IC 50]
ULK1: 18.94 nM (EC50) | [References]
[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. DOI:10.1039/c6sc05368h |
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| Company Name: |
Twochem Co.Ltd.
|
| Telephone: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
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